TW202114999A - 異惡唑啉化合物及其作為害蟲防治劑的用途 - Google Patents
異惡唑啉化合物及其作為害蟲防治劑的用途 Download PDFInfo
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- TW202114999A TW202114999A TW109129661A TW109129661A TW202114999A TW 202114999 A TW202114999 A TW 202114999A TW 109129661 A TW109129661 A TW 109129661A TW 109129661 A TW109129661 A TW 109129661A TW 202114999 A TW202114999 A TW 202114999A
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- Prior art keywords
- trifluoromethyl
- dihydroisoxazol
- methyl
- sulfinyl
- dichlorophenyl
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- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/04—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/72—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
- A01N43/80—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,2
Landscapes
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Dentistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
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- Wood Science & Technology (AREA)
- Zoology (AREA)
- Environmental Sciences (AREA)
- Pest Control & Pesticides (AREA)
- Agronomy & Crop Science (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Description
本發明涉及式(I)化合物。更具體地,本發明涉及式(I)的異惡唑啉化合物及其製備方法。本發明進一步涉及式(I)的異惡唑啉化合物作為害蟲防治劑的用途。
無脊椎動物害蟲,尤其是節肢動物和線蟲會破壞正在生長和已收穫的農作物,並進一步侵襲木製房屋和商業結構,從而給糧食供應和財產造成巨大的經濟損失。因此,持續需要用於對抗無脊椎動物害蟲例如昆蟲、蜘蛛和線蟲的新試劑。當前可獲得的現代殺蟲劑和殺蟎劑必須滿足在有效量、殘留活性、活性譜和效果以及它們的可能用途等諸多方面的要求。在過去的幾十年裡,人們努力開發能發揮生物化學作用模式(目前只在昆蟲或蟎蟲體內出現)的,而且還顯示出比已知殺蟲劑更優越的特性的針對性的殺蟲劑。
具有殺蟲活性的異惡唑啉化合物是已知的,例如在WO2008122375, WO2011157748, WO2009002809, JP2011037817, JP2011178673, WO2016077158, WO2008130651, WO2012120135, WO2011092287, WO2010032437和WO2013026939A1中有所描述。
但是,通過長期使用這種殺蟲劑,許多害蟲獲得了抗藥性,不能進行有效的控制,並且這種現象在最近幾年越來越嚴重。此外,這些現有殺蟲劑中的某些具有高毒性,或由於其殘留特性而在環境中保留很長時間,這可能會造成生態系統的破壞,成為一個日益嚴重的問題。
因此,持續需要更有效、毒性更低、對環境更安全和/或具有不同作用方式的新化合物。
鑒於上述情況,本發明設想了滿足或克服與現有技術有關的缺點的此類化合物。令人驚訝的是,現已發現某些含硫取代基的新型殺蟲活性的異惡唑啉化合物具有理想的殺蟲性能。
因此,本發明提供了式(I)的異惡唑啉化合物或其農業上可接受的鹽、異構體/結構異構體、立體異構體、非對映異構體、對映異構體、互變異構體、金屬絡合物、多晶型物或N-氧化物。
式(I)
其中,R1
、R2a
、R2b
、R2c
、A、T和Z如詳細描述中所定義。
在一個實施方案中,本發明提供了一種製備式(I)化合物或其農業上可接受的鹽的方法。
在另一個實施方案中,本發明提供了用於控制或預防無脊椎動物害蟲的組合物,其包含生物學有效量的式(I)化合物或其農業上可接受的鹽、異構體/結構異構體、立體異構體、非對映異構體、對映異構體、互變異構體、金屬絡合物、多晶型物或N-氧化物以及至少一種選自表面活性劑和助劑的其他組分。
在另一個實施方案中,組合物還包含至少一種選自殺真菌劑、殺蟲劑、殺線蟲劑、殺蟎劑、生物農藥、除草劑、植物生長調節劑、抗生素、肥料或營養素的至少一種生物活性和相容性化合物。
在另一實施方案中,本發明提供了式(I)化合物或其農業上可接受的鹽、異構體/結構異構體、立體異構體、非對映體、對映體、互變異構體、金屬絡合物、多晶型物或N-氧化物、其組合物或組合用於防治農作物和/或園藝作物中的無脊椎動物害蟲或動物寄生蟲的用途。
在又一實施方案中,本發明提供了一種防治無脊椎動物害蟲的方法,包括使用生物有效量的式(I)化合物或其農業上可接受的鹽、異構體/結構異構體、立體異構體、非對映體、對映體、互變異構體、金屬絡合物、多晶型物或N-氧化物、其組合物或組合接觸無脊椎動物害蟲、其棲息地、繁殖地、食物、植物、種子、土壤、無脊椎動物害蟲生長或可能生長的區域、材料或環境,或希望免受蟲害或侵擾的材料、植物、種子、土壤、表面或空間。
本發明詳細描述
定義
本發明中所提供的術語定義僅用於說明目的,絕不限制本發明公開的本發明的範圍。
本文所用的“包含”、“包括”、“具有”、“擁有”、“以...為特徵”或其任何其他變體旨在涵蓋非排他性包含,但須受明確指明的除外。例如,組合、混合、過程或方法包含的要素表的不一定局限於這些要素,但可以包括沒有明確列出的該組合、混合、步驟或方法固有的其他要素。
過渡詞“由...組成”排除任何未指定的元素、步驟或成分。如果在請求項中(除了通常與之相關的雜項之外),這樣的請求項將包含除所述材料之外的材料。當“由…組成”一詞出現在請求項正文的一個條款中,而不是緊接在序言之後時,它只限制該條款所規定的要素;其他因素也未從整個請求項中排除。
過渡詞“基本上由...組成”用於定義包括材料、步驟、特徵、成分或要素的組合物或方法,條件是這些附加材料、步驟、特徵、成分或要素不實質上影響請求項保護的發明的基本要素和新穎特徵。術語“基本上由......組成”佔據“包含”和“由......組成”之間的中間地帶。
此外,除非有相反的明確說明,否則“或”是指包含性的“或”而不是排他性的“或”。例如,條件A“或”B滿足以下任何一個:A為真(或存在)且B為假(或不存在),A為假(或不存在)且B為真(或現在),A和B都為真(或存在)。
此外,在本發明的要素或成分之前的不定冠詞“a”和“an”不限制該要素或成分的實例(即出現次數)的數量。因此,“a”或“an”應該被理解為包括一個或至少一個,並且要素或成分的單數單詞形式也包括複數,除非該數明顯是單數的。
如本發明所述,術語“無脊椎動物害蟲”包括作為具有經濟重要性害蟲的節肢動物、腹足動物和線蟲。術語“節肢動物”包括昆蟲、蟎蟲、蜘蛛、蠍子、蜈蚣、千足蟲、藥蟲和甲蟲。術語“腹足類”一詞包括蝸牛、蛞蝓和其他莖突蟲。“線蟲”一詞是指線蟲門的活生物體。術語“蠕蟲”包括蛔蟲、犬絲蟲、植食性線蟲、吸蟲、棘頭蟲和絛蟲。
術語“農業學的”一詞是指農作物如食物和纖維的生產,包括種植玉米、大豆和其他豆類、大米、穀物(如小麥、燕麥、大麥、黑麥、水稻、玉米)、綠葉蔬菜(如生菜、捲心菜和其他油菜作物)、果實蔬菜(如番茄、胡椒、茄子、十字花科植物和葫蘆)、土豆、紅薯、葡萄、棉花、樹木果實(如梨果和柑橘),小水果(草莓、櫻桃)和其他特種作物(如油菜、向日葵、橄欖)。
術語“非農學的”一詞指的非農作物,例如園藝作物(例如,花房、苗圃或不在田間生長的觀賞植物)、住宅、農業、商業和工業結構、草皮(例如,草皮農場、牧場、高爾夫球場、草坪、運動場等)、木製品、儲藏物、農林業和植被管理、公共衛生(即人類)和動物健康(例如寵物、牲畜和家禽等馴養動物,野生動物等非馴養動物)應用。
非農學應用包括通過向要保護的動物施用殺寄生蟲有效量(即生物學上有效)的本發明化合物(通常以配製用於獸醫用途的組合物形式)來保護動物免受無脊椎寄生蟲的侵害。本公開和請求項中所提及的術語“殺寄生蟲的”和“寄生殺蟲地”是指為保護動物免受害蟲的侵害對無脊椎寄生蟲害的可觀察到的效果。寄生殺蟲效果通常與減少目標無脊椎動物寄生蟲的出現或活動有關。對害蟲的這種效果包括壞死、死亡、生長遲緩、活動性降低或在宿主動物身體或身上的寄宿能力降低、進食減少和對繁殖的抑制。這些對無脊椎動物寄生蟲的影響可防治(包括預防、減少或消除)動物免受寄生蟲的侵擾或感染。
本發明的化合物可以以純的形式或作為不同可能的異構形式的混合物存在,例如立體異構體或結構異構體。各種立體異構體包括對映異構體、非對映異構體、手性異構體、阻轉異構體、構象異構體、旋轉異構體、互變異構體、光學異構體、多晶型物和幾何異構體。這些異構體的任何所需混合物都屬於本發明的請求項的範圍。本領域技術人員將理解,當相對於其他異構體富集時或當與其他異構體分離時,一種立體異構體可以更具活性和/或可以表現出有益效果。另外,本領域技術人員知道分離、富集和/或選擇性製備所述異構體的過程或方法或技術。
現就本說明中使用的各種術語的含義給予說明:
本文中使用的術語“脂肪族化合物”或“脂肪族基團”是其碳原子以直鏈、支鏈或非芳香環連接的有機化合物。
術語“烷基”(獨立使用或在“烷基硫”或“鹵代烷基”或-N(烷基)或烷基羰基烷基或烷基磺醯胺基等複合詞中使用),包括直鏈或支鏈C1
到C24
烷基,優選C1
到C15
烷基,優選C1
到C10
烷基,更優選C1
到C6
烷基。烷基的非限制性例子包括甲基、乙基、丙基、1-甲基乙基、1-甲基乙基、戊基、1-甲基丁基、1-甲基丁基、2-甲基丁基、2-甲基丙基、1-甲基戊基、1-甲基戊基、1-甲基戊基、2-甲基戊基、3-甲基戊基、4-甲基戊基、1,1-二甲基丁基、1,2-二甲基丁基、2,3-二甲基丁基、3,3-二甲基丁基、1-乙基丁基、2-乙基丁基、1,1,2-三甲基丙基、1,2,2-三甲基丙基,1-乙基1-甲基丙基和l-乙基2-甲基丙基或不同異構體。如果烷基在複合取代基的末端,例如,在烷基環烷基中,起始的複合取代基的部分,例如環烷基,可以以相同或不同方式且獨立地被烷基單取代或多取代。這同樣適用於其他自由基如烯基、烷基、羥基、鹵素、羰基、羰基氧基等位於末端的複合取代基。
術語“烯基”(獨立使用或在複合詞中使用),包括直鏈或C2
到C24
烯烴、優選C2
到C15
烯烴、更優選C2
到C10
烯烴、更優選C2
到C6
烯烴的支鏈。烯烴的非限制性例子包括乙烯基、1-丙烯基、2-丙烯基、1-丁烯基、2-丁烯基、1-甲基-1-丙烯基、2-甲基-2-丙烯基、2-甲基-1-丁烯基、1-甲基-1-丁烯基、2-甲基-1-丁烯基、3-甲基-2-丁烯基、3-甲基-3-丁烯基、2-甲基-3-丁烯基、3-甲基-3-丁烯基、1-1-二甲-2-丁烯基、1,2-二甲基-2-丙烯、1-乙基-1-丙烯、1-乙基-2-丙烯、1-乙基-2-戊烯、3-甲基-1-戊烯、2-甲基-1-戊烯、3-甲基-2-戊烯、3-甲基-2-戊烯、3-甲基-3-戊烯、3-甲基-3-戊烯、4-甲基-4-戊烯、3-甲基-4-戊烯、3-甲基-4-戊烯、1,1-二甲基-2-丁烯基、l,l-二甲基-3-丁烯基、1,2-二甲基-2-丁烯基、1,2-二甲基-3-丁烯基、1,3-二甲基-3-丁烯基、2,3-二甲基-3-丁烯基、2,3-二甲基-3-丁烯基、2,3-二甲基-3-丁烯基、3,3-二甲基-3-丁烯基、1-乙基-1-丁烯基、1-乙基-2-丁烯基、2-乙基-2-丁烯基、2-乙基-2-丁烯基、2-乙基-2-丁烯基、2-乙基-2-丁烯基、2-乙基-2-丁烯基、1-乙基-2-丁烯基、l-乙基-2-甲基-l-丙烯和l-乙基-2-甲基-2-丙烯及其異構體。烯烴也包括多烯,如1,2-丙二烯和2,4-己二烯。除非在其他地方有明確的定義,這個定義也適用於烯烴作為複合取代基的一部分,例如鹵代烯烴等。
術語“炔基”(單獨使用或在複合詞中使用)包括支鏈或直鏈C2
到C24
炔烴、優選C2
到C15
炔烴、更優選C2
到C10
炔烴、最優選C2
到C6
炔烴。炔的非限制性例子包括乙炔基、1-丙炔基、2-丙炔基、1-丁炔基、2-丁炔基、3-丁炔基、1-甲基-2-丙炔基、1-戊炔基、2-戊炔基、3-戊炔基,4-戊炔基、1-甲基-2-丁炔基、1-甲基-3-丁炔基、2-甲基-3-丁炔基、3-甲基-1-丁炔基、1,1-二甲基-2-丙炔基、1-乙基-2-丙炔基、1-己炔基、2-己炔基、3-己炔基、4-己炔基、5-己炔基、1-甲基-2-戊炔基、1-甲基-3-戊炔基、1-甲基-4-戊炔基、2-甲基-3-戊炔基、2-甲基-4-戊炔基、3-甲基-1-戊炔基、3-甲基-4-戊炔基、4-甲基-1-戊炔基、4-甲基-2-戊炔基、1,1-二甲基-2-丁炔基、1,1-二甲基-3-丁炔基、1,2-二甲基-3-丁炔基、2,2-二甲基-3-丁炔基、3,3-二甲基-1-丁炔基、1-乙基-2-丁炔基、1-乙基-3-丁炔基、2-乙基-3-丁炔基和1-乙基-1-甲基-2-丙炔基和不同的異構體。除非在別處具體限定,否則定義也適用於作為複合取代基的一部分的炔基,例如鹵代炔基等。術語“炔基”還可包括由多個三鍵組成的部分,例如2,5-己二炔基。
“環烷基”是指閉合形成環的烷基。非限制性實例包括但不限於環丙基、環丁基、環戊基和環己基。除非在別處明確限定,否則該定義也適用於作為複合取代基的一部分的環烷基,例如環烷基烷基等。
“環烯基”是指烯基封閉形成環,包括單環、部分不飽和的烴基。非限制性實例包括但不限於環戊烯基和環己烯基。除非在別處明確限定,否則該定義也適用於作為複合取代基的一部分的環烯基,例如環烯基烷基等。
“環炔基”是指炔基封閉形成環,包括單環、部分不飽和的基團。除非在別處具體限定,否則該定義也適用於作為複合取代基的一部分的環炔基,例如環炔基烷基等。
“環烷氧基”,“環烯氧基”等類似詞具有類似的定義。環烷氧基的非限制性實例包括環丙氧基,環戊氧基和環己氧基。除非在別處明確限定,否則該定義也適用於環烷氧基作為複合取代基的一部分,例如環烷氧基烷基等。
“鹵素”(獨立或以複合詞如“鹵代烷基”)包括氟、氯、溴或碘。此外,當用於諸如“鹵代烷基”的複合詞時,所述烷基可以部分或完全被鹵素原子取代,所述鹵素原子可以相同或不同。“鹵代烷基”的非限制性實例包括氯甲基、溴甲基、二氯甲基、三氯甲基、氟甲基、二氟甲基、三氟甲基、氯氟甲基、二氯氟甲基、氯二氟甲基、1-氯乙基、1-溴乙基、1-氟乙基、2-氟乙基、2,2-二氟乙基、2,2,2-三氟乙基、2-氯-2-氟乙基、2-氯-2,2-二氟乙基、2,2-二氯-2-氟乙基、2,2,2-三氯乙基、五氟乙基、1,1,2-二氟乙基-二氯-2,2,2-三氟乙基和1,1,1-三氟丙-2-基。除非在別處明確限定,否則這個定義也適用於鹵代烷基作為複合取代基的一部分,例如鹵代烷基氨基烷基等。
“鹵代烯基”和“鹵代炔基”的定義類似,不同的是烯基和炔基代替烷基作為取代基的一部分存在。
“鹵代烷氧基”是指直鏈或支鏈烷氧基,其中這些基團中的一些或所有氫原子可以被如上所述的鹵素原子取代。鹵代烷氧基的非限制性實例包括氯甲氧基、溴甲氧基、二氯甲氧基、三氯甲氧基、氟甲氧基、二氟甲氧基、三氟甲氧基、氯氟甲氧基、二氯氟甲氧基、氯二氟甲氧基、1-氯乙氧基、1-溴乙氧基、1-氟乙氧基、2-氟乙氧基、2,2-二氟乙氧基、2,2,2-三氟乙氧基、2-氯-2-氟乙氧基、2-氯-2,2-二氟乙氧基、2,2-二氯-2-氟乙氧基、2,2,2-三氯乙氧基、五氟乙氧基和1,1,1-三氟丙-2-氧基。除非在別處明確限定,否則該定義也適用於鹵代烷氧基作為複合取代基的一部分的基團,例如鹵代烷氧基烷基等。
術語“鹵代烷硫基”是指直鏈或支鏈烷硫基團,其中這些基團中至少一個至多所有氫原子可被如上所述的鹵素原子取代。鹵代烷硫基的非限制性實例包括氯甲硫基、碘甲硫基、溴甲硫基、二氯甲硫基、三氯甲硫基、氟甲硫基、二氟甲硫基、三氟甲硫基、氯氟甲硫基、二氯氟甲硫基、氯二氟甲硫基、1-氯乙硫基、1-溴乙硫基、1-氟乙硫基、2-氟乙硫基、2,2-二氟乙硫基、2,2,2-三氟乙硫基、2-氯-2-氟乙硫基、2-氯-2,2-二氟乙硫基、2,2-二氯-2-氟乙硫基、2,2,2-三氯乙硫基、五氟乙硫基和1,1,1-三氟-2-基硫基。除非在別處明確限定、否則該定義也適用於鹵代烷硫基作為複合取代基的一部分的基團,例如鹵代烷硫基烷基等。
“鹵代烷基亞磺醯基”的實例包括CF3
S(O)、CCl3
S(O)、CF3
CH2
S(O)。“鹵代烷基磺醯基”的非限制性實例包括CF3
S(O)2
、CCl3
S(O)2
、CF3
CH2
S(O)2
和CF3
CF2
S(O)2
。
術語“羥基”表示-OH,氨基表示-NRR,其中R可以是H或任何可能的取代基,例如烷基。羰基表示-C(O)-,羰基氧基表示-OC(O)-,亞磺醯基表示SO,磺醯基表示S(O)2
。
術語“烷氧基”(單獨使用或以複合詞的形式使用)包括C1
至C24
烷氧基,優選C1
至C15
烷氧基,更優選C1
至C10
烷氧基,最優選C1
至C6
烷氧基。烷氧基的實例包括甲氧基、乙氧基、丙氧基、1-甲基乙氧基、丁氧基、1-甲基丙氧基、2-甲基丙氧基、1,1-二甲基乙氧基、戊氧基、1-甲基丁氧基、2-甲基丁氧基、3-甲基丁氧基、2,2-二甲基丙氧基、1-乙基丙氧基、己氧基、1,1-二甲基丙氧基、1,2-二甲基丙氧基、1-甲基戊氧基、2-甲基戊氧基、3-甲基戊氧基、4-甲基戊氧基、1,1-二甲基丁氧基、1,2-二甲基丁氧基、1,3-二甲基丁氧基、2,2-二甲基丁氧基、2,3-二甲基丁氧基、3,3-二甲基丁氧基、1-乙基丁氧基、2-乙基丁氧基、1,1,2-三甲基丙氧基、1,2,2-三甲基丙氧基、1-乙基-1-甲基丙氧基和1-乙基-2-甲基丙氧基和不同的異構體。除非在別處具體限定,否則該定義也適用於烷氧基作為複合取代基的一部分,例如鹵代烷氧基、炔基烷氧基等。
術語“烷氧基烷基”表示烷基被烷氧基取代。“烷氧基烷基”的非限制性實例包括CH3
OCH、CH3
OCH2
CH2
、CH3
CH2
OCH2
、CH3
CH2
CH2
CH2
OCH2
和CH3
CH2
OCH2
CH2
。
術語“烷氧基烷氧基”表示烷氧基被烷氧基取代。
術語“烷硫基”包括支鏈或直鏈烷硫基基團,例如甲硫基、乙硫基、丙硫基、1-甲硫基硫基、丁硫基、1-甲基丙硫基、2-甲基丙硫基、1,1-二甲基乙硫基、戊硫基、1-甲基丁硫基、2-甲基丁硫基 、3-甲基丁硫基、2,2-二甲基丙硫基、1-乙基丙硫基、己硫基、1,1-二甲基丙硫基、1,2-二甲基丙硫基、1-甲基戊硫基、2-甲基戊硫基、3-甲基戊硫基、4-甲基戊硫基、1,1-二甲基丁硫基 1,2-二甲基丁硫基、1,3-二甲基丁硫基、2,2-二甲基丁硫基、2,3-二甲基丁硫基、3,3-二甲基丁硫基、1-乙基丁硫基、2-乙基丁硫基、1,1,2-三甲基丙硫基、1,2,2-二甲基丁硫基、2-三甲基丙硫基、1-乙基-1-甲基丙硫基和1-乙基-2-甲基丙硫基以及不同的異構體。
鹵代環烷基、鹵代環烯基、烷基環烷基、環烷基烷基、環烷氧基烷基、烷基亞磺醯基烷基、烷基磺醯基烷基、鹵代烷基羰基、環烷基羰基、鹵代烷氧基烷基等的定義與上述例子類似。
術語“烷基硫代烷基”表示烷基被烷硫基取代。“烷基硫代烷基”的非限制性實例包括-CH2
SCH2
、-CH2
SCH2
CH2
、CH3
CH2
SCH2
、CH3
CH2
CH2
CH2
SCH2
和CH3
CH2
SCH2
CH2
。“烷基硫代烷氧基”表示烷氧基被烷硫基取代。“環烷基代烷基氨基”表示烷基氨基被環烷基取代。
烷氧基烷氧基烷基、烷基氨基烷基、二烷基氨基烷基、環烷基氨基烷基、環烷基氨基羰基等的定義與“烷基硫代烷基”或“環烷基代烷基氨基”類似。
“烷氧基羰基”是通過羰基(-CO-)與骨架鍵合的烷氧基。除非在別處具體限定,否則該定義也適用於烷氧基羰基作為複合取代基的一部分,例如環烷基烷氧基羰基等。
術語“烷氧基羰基烷基氨基”表示烷基氨基被烷氧基羰基取代。“烷基羰基烷基氨基”表示烷基氨基被烷基羰基取代。術語烷硫基烷氧基羰基、環烷基烷基氨基烷基等的定義與此類似。
“烷基亞磺醯基”的非限制性例子包括但不限於甲基亞磺醯基、乙基亞磺醯基、丙基亞磺醯基、1-甲基乙基亞磺醯基、丁基亞磺醯基、1-甲基丙基亞磺醯基、2-甲基丁基亞磺醯基、1-甲基丁基亞磺醯基、2-甲基丁基亞磺醯基、2-甲基丁基亞磺醯基、1-乙基丙基亞磺醯基、1-乙基丙基亞磺醯基、1-2-二甲基丙基亞磺醯基、2-甲基戊基磺醯、3-甲基戊基磺醯、4-甲基戊基磺醯、1,1-二甲基丁基磺醯、1,3-二甲基丁基磺醯、2,3-二甲基丁基磺醯、3,3-二甲基丁基磺醯、1-乙基丁基磺醯、1,1,2-三甲基丙基磺醯、1-乙基1-甲基丙基磺醯和1-乙基2-甲基丙基磺醯及其異構體。“芳基亞磺醯基”一詞包括Ar-S(O),其中Ar可以是任何羧基或雜環。除非另有專門定義,否則這一定義也適用於烷基亞磺醯基作為複合取代基的一部分,例如鹵代烷基亞磺醯基等。
“烷基磺醯基”的非限制性例子包括但不限於甲基磺醯基、乙基磺醯基、丙基磺醯基、1-甲基乙基磺醯基、丁基磺醯基、1-甲基丙基磺醯基、2-甲基丁基磺醯基、1-甲基丁基磺醯基、2-甲基丁基磺醯基、3-甲基丁基磺醯基、2,2-甲基丙基磺醯基、1-乙基丙基磺醯基、1-乙基丙基磺醯基、1,2-二甲基丙基磺醯基、1-甲基磺醯基、2-甲基戊基磺基、3-甲基戊基磺基、4-甲基戊基磺基、1,1-二甲基丁基磺基、1,2-二甲基丁基磺基、2,2-二甲基丁基磺基、2,3-二甲基丁基磺基、3,3-二甲基丁基磺基、1-乙基丁基磺基、1,1,2-三甲基丙基磺基、1-乙基1-甲基丙基磺基、l-乙基2-甲基丙基磺基及其異構體。“芳基磺醯基”一詞包括Ar-S(O)2
,其中Ar可以是任何羧基或雜環。除非另有定義,這個定義也適用於烷基磺醯基作為複合取代基的一部分,例如烷基磺基烷基等。
“烷基胺基”、“二烷基胺基”等術語的定義與上述示例類似。
術語“碳環”或“碳環的”或“碳環基的”包括“芳族碳環系”和“非芳族碳環系”或多環或雙環(螺環、稠合、橋連、非稠合)環化合物,其中環可以是芳族的或非芳香族(其中芳香族表示符合休克爾規則,非芳香族表示不滿足休克爾規則)。
與環相關的術語“雜”是指至少一個環原子不是碳原子的環,其可以包含1至4個獨立地選自氮、氧和硫的雜原子,條件是每個環裏面不超過4個氮、2個氧和2個硫。
術語“芳香族”表示符合休克爾規則,“非芳香族”表示不滿足休克爾規則。
術語“雜環”或“雜環的”包括“芳香雜環”或“雜芳基環系”和“非芳香雜環系”或多環或雙環(螺環,稠合,橋連,非稠合)環化合物,環可以是芳香族的 或非芳香族,其中雜環含有至少一個選自N、O、S(O)0-2
的雜原子,和/或雜環的C環成員可以被C(=O)、C(=S)、C(=CR*R*)和C=NR*取代(*表示整數)。
術語“非芳族雜環”或“非芳族雜環”是指含有1至4個選自氧、氮和硫的雜原子的三至十五元(優選三至十二元)飽和或部分不飽和的雜環:單環,雙環或三環雜環,除碳環成員外,還含有1-3個氮原子和/或一個氧或硫原子或一個或兩個氧和/或硫原子;如果環含有多個氧原子,則它們不直接相鄰;例如(但不限於)環氧乙烷,疊氮基,氧雜環丁烷基,氮雜環丁烷基,硫雜環丁烷基,2-四氫呋喃基,3-四氫呋喃基、2-四氫噻吩基、3-四氫噻吩基、1-吡咯烷基、2-吡咯烷基、3-吡咯烷基、3-異惡唑烷基、4-異惡唑烷基、5-異惡唑烷基、3-異噻唑烷基、4-異噻唑烷基、5-異噻唑烷基、1-吡唑烷基、3-吡唑烷基、4-吡唑烷基、5-吡唑烷基、2-惡唑烷基、4-惡唑烷基、5-惡唑烷基、2-噻唑烷基、4-噻唑烷基、5-噻唑烷基、1-咪唑烷基、2-咪唑烷基、4-咪唑烷基、1,2,4-惡二唑烷-3-基、1,2,4-惡二唑烷-5-基、1,2,4-噻二唑烷-3-基、1,2,4-噻二唑烷-5-基、1,2,4-三唑烷-1-基、1,2,4-三唑烷-3-基、1,3,4-惡二唑烷-2-基、1,3,4-噻二唑烷-2-基、1,3,4-三唑烷-1-基、1,3,4-三唑烷-2-基、2,3-二氫呋喃-2-基、2,3-二氫呋喃-3-基、2,4-二氫呋喃-2-基、2,4-二氫呋喃-3-基、2,3-二氫噻吩-2-基、2,3-二氫噻吩-3-基、2,4-二氫噻吩-2-基、2,4-二氫噻吩-3-基、吡咯啉基、2-吡咯啉-2-基、2-吡咯-3-基、3-吡咯-2-基、3-吡咯-3-基、2-異惡唑啉-3-基、3-異惡唑啉-3-基、4-異惡唑啉-3-基、2-異惡唑啉-4-基、3-異惡唑啉-4-基、4-異惡唑啉-4-基、2-異惡唑啉-5-基、3-異惡唑啉-5-基、4-異惡唑啉-5-基、2-異噻唑啉-3-基、3-異噻唑啉-3-、4-異噻唑啉-3-基、2-異噻唑啉-4-基、3-異噻唑啉-4-基、4-異噻唑啉-4-基、2-異噻唑啉-5-基、3-異噻唑啉-5-基、4-異噻唑啉-5-基、2,3-二氫吡唑-1-基、2,3-二氫吡唑-2-基、2,3-二氫吡唑-3-基、2,3-二氫吡唑-4-基、2 、3-二氫吡唑-5-基、3,4-二氫吡唑-1-基、3,4-二氫吡唑-3-基、3,4-二氫吡唑-4-基、3,4-二氫吡唑-5-基、4,5-二氫吡唑-1-基、4,5-二氫吡唑-3-基、4,5-二氫吡唑-4-基、4,5-二氫吡唑-5-基、2,3-二氫惡唑-2-基、2,3-二氫惡唑-3-基、2,3-二氫惡唑-4-基、2,3-二氫惡唑-5-基、3,4-二氫惡唑-2-基、3,4-二氫惡唑-3-基、3,4-二氫惡唑-4-基、3,4-二氫惡唑-5-基、3,4-二氫惡唑-2-基、3,4-二氫惡唑-3-基、3,4-二氫惡唑-4-基、呱啶基、2點二乙烯基、3-呱啶基、4-呱啶基、吡嗪基、嗎啉基、硫代嗎啉基、1,3-二惡烷-5-基、2-四氫吡喃基、4-四氫吡喃基、2-四氫噻吩基、3-六氫噠嗪基、4-六氫噠嗪基、2-六氫嘧啶基、4-六氫嘧啶基、5-六氫嘧啶基、2-呱嗪基、1,3,5-六氫三嗪-2-基、1,2,4-六氫三嗪-3-基、環絲氨酸、2,3,4,5-四氫[1H]氮雜卓-1-或-2-或-3-或-4-或-5-或-6-或-7-基、3,4,5,6-四氫[2H]氮雜卓-2-或-3-或-4-或-5-或-6-或-7-基、2,3,4,7-四氫[1H]氮雜卓-1-或-2-或-3-或-4-或-5-或-6-或-7-基、2,3,6,7-四氫[1H]氮雜卓-1-或-2-或-3-或-4-或-5-或-6-或-7-基、六氫氮雜-1-或-2-或-3-或-4-基、四-和六氫氧雜環庚烯基、如2,3,4,5-四氫[1H]氧雜環庚烷-2-或-3-或-4-或-5-或-6-或-7-基、2,3,4,7-四氫[1H]氧雜-2-酮或-3-或-4-或-5-或-6-或-7-基、2,3,6,7-四氫[1H]氧雜-2-酮或-3-或-4-或-5-或-6-或-7-基、六氫氮雜-1-或-2--或-3-或-4-基、四-和六氫-1,3-二氮雜基、四-和六氫-1,4-二氮雜基、四-和六氫-1,3-氧氮雜基、四-和六氫-1,4-氧氮雜基、四-和六氫-1,3-二氧雜環庚烯基、四氫和六氫-1,4-二氧雜環庚烯基。除非在別處具體限定,否則該定義也適用於雜環烷基作為複合取代基的一部分,例如雜環基烷基等。
術語“雜芳基”是指包含氧、氮和硫族中的一至四個雜原子的5或6元全不飽和單環系;如果該環含有一個以上的氧原子,它們並不直接相鄰;5元雜芳基包含一至四個氮原子或一至三個氮原子及一個硫或氧原子:除了碳原子外,五元雜芳基還可含有一至四個氮原子或一至三個氮原子及一個硫或氧原子作為環成員,例如(但不限於)呋喃基、噻吩基、吡咯基、異惡唑基、異噻唑基、吡唑基、惡唑基、噻唑基、咪唑基、1,2,4-惡二唑基、1,2,4-噻二唑基1,2,4,4-三唑基、1,3,4-惡二唑基、1,3,4-噻二唑基、1,3,4-三唑基、四唑基;含有一至四個氮原子的氮鍵合的5-元雜芳基,或含有一至三個氮原子的苯並稠合的氮鍵合的5-元雜芳基:除碳原子外,可含有一至四個氮原子的五元雜芳基或者一至三個氮原子作為環成員並且其中兩個相鄰的碳環成員或一個氮和一個相鄰的碳環成員可以通過丁-1,3-二烯-1,4-二基橋接,其中一個或兩個碳原子可被氮原子取代,其中這些環通過一個氮環成員與骨架連接,例如(但不限於)1-吡咯基、1-吡唑基、1,2,4-三唑-1-基、1-咪唑基、1,2,3-三唑-1-基和1,3,4-三唑-1-基。
含有1-4個氮原子的6-元雜芳基:6-元雜芳基,其除碳原子外,還可分別含有1-3個和1-4個氮原子作為環成員,例如(但不限於)2-吡啶基、3-吡啶基、4-吡啶基、3-噠嗪基、4-噠嗪基、2-嘧啶基、4-嘧啶基、5-嘧啶基、2-吡嗪基、1,3,5-三嗪-2-基、1,2,4-三嗪-3-基和1,2,4,5-四嗪-3-基;含有一至三個氮原子或一個氮原子和一個氧或硫原子的苯並稠合的5-元雜芳基:例如(但不限於)吲哚-1-基、吲哚-2-基、吲哚-3-基、吲哚-4-基、吲哚-5-基、吲哚-6-基、吲哚-7-基、苯並咪唑-1-基、苯並咪唑-2-基、苯並咪唑-4-基、苯並咪唑-5-基、吲唑-l-基、吲唑-3-基、吲唑-4-基、吲唑-5-基、吲唑-6-基、吲唑-7-基、吲唑-2-基、1-苯並呋喃-2-基、1-苯並呋喃-3-基、1-苯並呋喃-4-基、1-苯並呋喃-5-基、1-苯並呋喃-6-基、1-苯並呋喃-7-基、1-苯並噻吩-2-基、1-苯並噻吩-3-基基團、1-苯並噻吩-4-基、1-苯並噻吩-5-基、1-苯並噻吩-6-基、1-苯並噻吩-7-基、1,3-苯並噻唑-2-基、1,3-苯並噻唑-4-基、1,3-苯並噻唑-5-基、1,3-苯並噻唑-6-基、1,3-苯並噻唑-7-基、1,3-苯並惡唑-2-基、1,3-苯並惡唑-4-基、1,3-苯並惡唑-5-基、1,3-苯並惡唑-6-基和1,3-苯並惡唑-7-基;含有一至三個氮原子的苯並稠合的6-元雜芳基:例如(但不限於)喹啉-2-基、喹啉-3-基、喹啉-4-基、喹啉-5-基、喹啉-6-基、喹啉-7-基、喹啉-8-基、異喹啉-1-基、異喹啉-3-基、異喹啉-4-基、異喹啉-5-基、異喹啉-6-基、異喹啉-7-基和異喹啉啉-8-基。
除非在其他地方特別定義,該定義也適用於雜芳基作為複合取代基的一部分,例如雜芳基烷基等。
術語“三烷基甲矽烷基”包括3個支鏈和/或直鏈烷基自由基,它們附屬於並連接在矽原子上,例如三甲基甲矽烷基,三乙基甲矽烷基和叔丁基二甲基甲矽烷基。“鹵代烷基甲矽烷基”表示三個烷基中的至少一個被鹵素原子部分或完全取代,所述鹵素原子可以相同或不同。“烷氧基三烷基甲矽烷基”表示三個烷基中的至少一個被一個或多個可以相同或不同的烷氧基取代。“三烷基甲矽烷氧基”表示通過氧連接的三烷基甲矽烷基部分。
“烷基羰基”的非限制性實例包括C(O)CH3
、C(O)CH2
CH2
CH3
和C(O)CH(CH3
)2
。“烷氧基羰基”的實例包括CH3
OC(=O)、CH3
CH2
OC(=O)、CH3
CH2
CH2
OC(=O)、(CH3
)2
CHOC(=O)和不同的丁氧基或戊氧基羰基異構體。“烷基氨基羰基”的實例包括CH3
NHC(=O)、CH3
CH2
NHC(=O)、CH3
CH2
CH2
NHC(=O)、(CH3
)2
CHNHC(=O)和不同的丁氨基-或戊基氨基羰基異構體。“二烷基氨基羰基”的實例包括(CH3
)2
NC(=O)、(CH3
CH2
)2
NC(=O)、CH3
CH2
(CH3
)NC(=O)、CH3
CH2
CH2
(CH3
)NC(=O)和(CH3
)2
CHN(CH3
)C(=O)“烷氧基烷基羰基”的實例包括CH3
OCH2
C(=O)、CH3
OCH2
CH2
C(=O)、CH3
CH2
OCH2
C(=O)、CH3
CH2
CH2
CH2
OCH2
C(=O)和CH3
CH2
OCH2
CH2
C(=O)。“烷基硫代烷基羰基”的實例包括CH3
SCH2
C(=O)、CH3
SCH2
CH2
C(=O)、CH3
CH2
SCH2
C(=O)、CH3
CH2
CH2
CH2
SCH2
C(=O)和CH3
CH2
SCH2
CH2
C(=O)。鹵代烷基磺醯基羰基、烷基磺醯基氨基羰基、烷基硫代烷氧基羰基、烷氧基羰基烷基氨基等的定義與此類似。“烷基氨基烷基羰基”的非限制性實例包括CH3
NHCH2
C(=O)、CH3
NHCH2
CH2
C(=O)、CH3
CH2
NHCH2
C(=O)、CH3
CH2
CH2
CH2
NHCH2
C(=O)和CH3
CH2
NHCH2
CH2
C(=O)。
“醯胺”指的是A-R'C = ONR''-B,其中R'和R''表示取代基,A和B表示任何基團。
“硫代醯胺”是指A-R'C=SNR''-B,其中R'和R''表示取代基,A和B表示任何基團。
取代基中的碳原子總數由“Ci
-Cj
”首碼表示,其中i和j是數字1至21。例如,C1
-C3
烷基磺醯基表示甲基磺醯基至丙基磺醯基;C2
烷氧基烷基表示CH3
OCH2
;C3
烷氧基烷基表示例如CH3
CH(OCH3
)、CH3
OCH2
CH2
或CH3
CH2
OCH2
;C4
烷氧基烷基表示被含有總共四個碳原子的烷氧基取代的烷基的各種異構體,實例包括CH3
CH2
CH2
OCH2
和CH3
CH2
OCH2
CH2
。在上述敘述中,當式(I)化合物由一個或多個雜環組成時,所有取代基通過任何可用的碳或氮通過取代所述碳或氮上的氫而連接到這些環上。
當化合物被帶有下標的取代基取代時,所述取代基表示所述取代基的數目可以超過1,所述取代基(當它們超過1時)獨立地選自所定義的取代基。此外,當(R)m
中的下標m表示範圍從例如0到4的整數時,則取代基的數目可以從0和4之間的整數中選擇。
當基團含有可以是氫的取代基時,則當該取代基被認為是氫時,可以認為所述基團未被取代。
本文中的實施方案及其各種特徵和有利的細節將參照描述中的非限制性實施方案進行說明。為避免不必要地模糊本文實施方案,省略了對已知成分和處理技術的描述。
這裏使用的示例僅旨在便於理解可以實踐本文的實施方案的方式,並且進一步使本領域技術人員能夠實踐本文的實施方案。因此,這些實施方案不應被解釋為限制本發明實施方案的範圍。
具體實施方案的描述將充分地揭示本文實施方案的大致性質,使其他人可以通過應用當前知識,能夠修改和/或適應應用這些具體實施方式而不脫離一般概念,因此, 這種適應和修改, 應被理解為具有本發明同樣地意義和範圍。需要理解的是,這裏使用的片語或術語是為了描述目的,不對本發明施加限制。因此,雖然這裏的實施方案是以首選實施方案的形式描述的,但那些精通該技術的人將認識到,在這裏描述的實施方案的精神和範圍內,通過修改可以實踐這裏的實施方案。
在本詳述中包含的對文檔、步驟、材料、裝置、物品等的任何討論僅僅是為了提供本發明的背景,不應視為承認這些事項構成現有技術基礎的一部分,或是本申請的最先日期之前存在的本領域的一般常識。
儘管在描述和描述/請求項中提到的數值可能構成本發明的本發明的關鍵部分,但是如果該偏差遵循相同的科學,則與這些數值的任何偏差仍然是本發明的範圍內。如果合適,本發明的發明化合物可以作為不同可能的異構形式的混合物存在,尤其是立體異構體的混合物,例如E和Z、蘇式和赤型、光學異構體,還有互變異構體(如果合適)。E和Z異構體以及蘇型和赤型異構體和光學異構體的任何所需混合物和可能的互變異構形式都被是本公開和請求項的範圍。
用於本發明目的的術語“害蟲”包括但不限於真菌、原生藻菌(卵菌綱)、細菌、線蟲、蟎蟲、蜱蟲、昆蟲和齧齒動物。
術語“植物”在此應理解為意指所有植物和植物種群,例如需要的和不需要的野生植物或作物植物(包括天然存在的作物植物)。作物植物可以是通過常規育種和優化方法或通過生物技術和基因工程方法或這些方法的組合獲得的植物,包括轉基因植物和植物育種者權利受保護和不受保護的植物栽培種。
用於本發明的目的的術語“植物”包括以樹木、灌木、草本植物、草、蕨類植物和苔蘚這些通常在田間生長,通過其根部吸收水和所需物質,以及通過光合作用合成葉片中的營養成分的活生物體。
用於本發明目的的“植物”的實例包括但不限於農作物,例如小麥、黑麥、大麥、黑小麥、燕麥或大米;甜菜;水果和果樹,例如梨果、核果或軟果,例如蘋果、梨、李子、桃子、杏仁、櫻桃、草莓、覆盆子、黑莓或醋栗;豆科植物,如扁豆、豌豆、苜蓿或大豆;油菜、芥菜、橄欖、向日葵、椰子、可可豆、蓖麻油植物、油棕櫚、花生或大豆等油料植物;葫蘆,如南瓜、黃瓜或甜瓜;纖維植物,如棉花、亞麻、大麻或黃麻;柑橘類水果和柑橘樹,如柳丁、檸檬、葡萄柚或柑橘;任何園藝植物、蔬菜,如菠菜、生菜、蘆筍、捲心菜、胡蘿蔔、洋蔥、番茄、土豆、葫蘆或辣椒粉;月桂科屬植物,如鱷梨、肉桂或樟腦;葫蘆科植物;含油植物;能源和原料植物,如穀物、玉米、大豆、其他豆科植物、油菜、甘蔗或油棕;煙草;堅果;咖啡;茶;可可;香蕉;胡椒;葡萄藤(鮮食葡萄和葡萄汁、葡萄藤);跳;草皮;甜葉(也稱甜葉菊);天然橡膠植物或觀賞植物和林業植物,例如花、灌木、闊葉樹或常綠植物,例如針葉樹;以及植物繁殖材料,例如種子,以及這些植物的作物材料。
優選地,用於本發明目的的植物包括但不限於穀類、玉米、大米、大豆和其他豆科植物、水果和果樹、葡萄、堅果和堅果樹、柑橘和柑橘樹、任何園藝植物、葫蘆科、含油植物、煙草、咖啡、茶、可可、甜菜、甘蔗、棉花、馬鈴薯、番茄、洋蔥、辣椒和蔬菜、觀賞植物、任何供人類和動物使用的花卉植物和其他植物。
術語“植物部分”應理解為是指植物地上和地下的所有部分和器官。為了本發明的目的,術語植物部分包括但不限於插條、葉、枝、塊莖、花、種子、分枝、根,包括主根、側根、根毛、根尖、根冠、根狀莖、幼枝、芽、果實、子實體、樹皮、莖、芽、輔助芽、分生組織、節和節間。
術語“其位點”包括土壤、植物或植物部分的周圍環境以及在播種/種植植物或植物部分之前、期間或之後使用的設備或工具。
本發明化合物或組合物(由本發明化合物和任意其他相容化合物組成的)中的本發明化合物在植物或植物材料或其所在位點上的應用包括通過本領域技術人員已知的技術施用,包括但不限於噴灑、塗料、浸漬、薰蒸、浸漬、注射和撒粉。
術語“施用”是指物理或化學性黏附於植物或植物部分,包括浸漬。
在一個實施方案中,本發明提供式(I)化合物,
式(I)
其中,
R1
選自C1-
C6
-烷基、C1-
C6
-鹵代烷基、C3
-C6
-環烷基和C3
-C6
-鹵代環烷基;
R2a
、R2b
和R2c
獨立地選自氫、X、氰基、C1
-C6
-烷基、C2
-C6
-烯基、C2
-C6
-炔基、C1
-C6
-鹵代烷基、C2
-C6
-鹵代烯基和C3
-C8
-環烷基;
A選自苯基和C5
-C6
-雜環基,其可以任選地被一個或多個R3
基團取代;
R3
選自氫、X、氰基、SCN、硝基、C1
-C6
-烷基、C2
-C6
-烯基、C2
-C6
-炔基、C1
-C6
-鹵代烷基、C2
-C6
-鹵代烯基、C2
-C6
-鹵代炔基、C3
-C8
-環烷基、C4
-C8
-環烯基、C4
-C8
-環炔基、SF5
、N(R′′)2
、OR4
、S(O)n
R″、C(=O)-R″、C1
-C8
-烷基-S(O)n
R″、C1
-C8
-烷基-C(=O)-R″和CR′=NR″;
T代表-N=S(O)0-1
R7
-、-(CR5
R6
)p
N=S(O)0-1
R7
-、-C(O)N=S(O)0-1
R7
-、-C(O)(CR5
R6
)p
N=S(O)0-1
R7
-和-C(O)NR9
S(O)-;
其中,片段T的LHS附著在A上,片段T的RHS附著在Z上;
R4
選自氫、C1
-C6
-烷基、C2
-C6
-烯基、C2
-C6
-炔基、C1
-C6
-鹵代烷基、C2
-C6
-鹵代烯基、C3
-C8
-環烷基、C6
-C10
-芳基和C3
-C8
-雜環基;
R5
和R6
獨立地選自氫、X、氰基、C1
-C6
-烷基、C2
-C6
-烯基、C1
-C6
-鹵代烷基、OR4
、C3
-C8
-環烷基;其中環狀環系統中的一個或多個碳原子可以被選自N、O、S基團,並且可以任選包括1-3個選自C(=O)、C(=S)、S(O)m
和Si(R′)2
的環成員的雜原子取代;或者
R5
和R6
與它們所連接的原子一起或與選自C、N、O、S基團,並且可以任選包括1-3個選自C(=O)、C(=S)、S(O)m
和Si(R′)2
的環成員的原子一起可以形成三至七元環,其本身可以被X、CN、R′、OR′、SR′、N(R′)2
、Si(R′)3
、COOR′和CON(R′)2
基團取代;
R7
和Z獨立地選自C1
-C6
-烷基、C1
-C6
-氰基烷基、C2
-C6
-烯基、C2
-C6
-炔基、C1
-C6
-鹵代烷基、C2
-C6
-鹵代烯基、C2
-C6
-鹵代炔基、C(=O)-R″、C1
-C8
-烷基-C(=O)-R″、C(=O)-N(R′R″)、C1
-C8
-烷基-C(=O)-N(R′R″)、C2
-C8
-烯基-C(=O)-N(R′R″)、C3
-C8
-環烷基、C4
-C8
-環烯基、C4
-C8
-環炔基、C6
-C10
-芳基、C7
-C15
-芳烷基、雙環C5
-C12
-烷基、雙環C7
-C12
-烯基、稠合或非稠合或雙環C3
-C18
-碳環;其中環狀環系統中的一個或多個碳原子可以被選自N、O、S基團,並且可以任選包括1-3個選自C(=O)、C(=S)、S(O)m
和Si(R′)2
的環成員的雜原子取代;
R8
選自氫、X、氰基、SCN、硝基、C1
-C6
-烷基、C2-
C6
-烯基、C2
-C6
-炔基、C1
-C6
-鹵代烷基、C2
-C6
-鹵代烯基、C2
-C6
-鹵代炔基、SF5
、OR4
、N(R′′)2
、Si(R′)3
、(C=O)-R″、S(O)n
R″、C1-
C8
-烷基-S(O)n
R″、C1
-C8
-烷基-(C=O)-R″、CR′=NR″、C3
-C8
-環烷基、C4
-C8
-環烯基;其中環狀環系統中的一個或多個碳原子可以被選自N、O、S基團,並且可以任選包括1-3個選自C(=O)、C(=S)、S(O)m
和Si(R′)2
的環成員的雜原子取代;
R9
選自氫、C1
-C12
-烷基、C2
-C12
-烯基、C2
-C12
-炔基、C1
-C12
-鹵代烷基、C2
-C12
-鹵代烯基、C2
-C12
-鹵代炔基、C3
-C8
-環烷基、Si(R′)3
、OR4
、(C=O)-R″;
R5
或R6
和R7
、R7
和R3
、R8
和Z或R7
和Z與它們所連接的原子一起或與選自C、N、O、S基團,並且可以任選包括1-3個選自C(=O)、C(=S)、S(O)m
和Si(R′)2
的環成員的原子一起可以形成三至七元環,其本身可以被X、CN、R′、OR′、SR′、N(R′)2
、Si(R′)3
、COOR′和CON(R′)2
基團取代;
每個R1
、R2a
、R2b
、R2c
、R3
、R4
、R5
、R6
、R7
、R8
和R9
可以任選地被一個或多個選自X、CN、R″、OR″、SR″、N(R′R″)、Si(R′)3
、COOR′和CON(R′R″)的基團取代;
X代表鹵素;
R′代表氫、C1-
C6
-烷基或C3
-C8
-環烷基;其中烷基和環烷基可任選被一個或多個X取代;
R″代表氫、C1-
C6
-烷基、C1-
C6
-鹵代烷基、C3
-C8
-環烷基、N(R′)2
、OR′和C6-
C10
-芳基;其中環狀環系統中的一個或多個碳原子可以被選自N、O、S基團,並且可以任選包括1-3個選自C(=O)、C(=S)、S(O)m
和Si(R′)2
的環成員的雜原子取代,並且每個R″可以任選地被一個或多個選自X、R″、CN、OR″、SR″、N(R′)2
,、Si(R′)3
、COOR′和CON(R′)2
的基團取代;
R′″選自氫、R″、CN、C1
-C6
-烷基、C1
-C6
-鹵代烷基、C2
-C6
-烯基、C2
-C6
-炔基、C3
-C8
-環烷基、C4
-C8
-環烯基、C4
-C8
-環炔基、OR4
、(C=O)-R′、COOR′、CON(R′)2
、C6
-C10
-芳基、C7
-C15
-芳烷基和C5
-C10
-雜環基基團;其中環狀環系統中的一個或多個碳原子可以被選自N、O、S基團,並且可以任選包括1-3個選自C(=O)、C(=S)、S(O)m
和Si(R′)2
的環成員的雜原子取代,並且每個R′″可以任選地被一個或多個選自X、R′、CN、OR′、SR′、N(R′)2
、Si(R′)3
、COOR′或CON(R′)2
的基團取代;
p代表整數1或2;
q代表整數0或1;
m和n代表整數0、1或2;
或其農業上可接受的鹽、異構體/結構異構體、立體異構體、非對映異構體、對映異構體、互變異構體、金屬絡合物、多晶型物或N-氧化物。
本發明的一個實施方案提供了式(I)化合物,其中,A是苯基,並且取代基T和Z在苯環的1、3或1、4位被取代。優選地,取代基T和Z在苯環的1、4位被取代。
在一個實施方案中,本發明提供了式(Ia)的化合物或其鹽,
式(Ia)
其中,取代基R1
選自C1-
C6
-烷基和C1-
C6
-鹵代烷基;並且取代基R2a
、R2b
、R2c
、R3
、R7
和Z如上文所定義。
在一個優選的實施方案中,本發明提供式(Iaa)化合物或其鹽,
式(Iaa)
其中,取代基R1
代表C1-
C6
-鹵代烷基,取代基R2a
、R2b
、R2c
代表鹵素,R3
選自鹵素、氰基、C1-
C6
-烷基和C1-
C6
-烯基;R7
和Z如上文所定義。
在另一個實施方案中,本發明提供式(Ib)化合物或其鹽,
式(Ib)
其中,取代基R1
選自C1-
C6
-烷基和C1-
C6
-鹵代烷基;取代基R2a
、R2b
、R2c
、R3
、R4
、R5
、R7
、p和Z如上文所定義。
在一個優選的實施方案中,本發明提供了式(Iba)化合物或其鹽,
式(Iba)
其中,取代基R1
代表C1-
C6
-鹵代烷基,取代基R2a
、R2b
、R2c
代表鹵素;R3
選自鹵素、氰基、C1-
C6
-烷基和C1-
C6
-烯基;R4
、R5
、R7
和
Z如上文所定義。
在另一個實施方案中,本發明提供了式(Ic)化合物或其鹽,
式(Ic)
其中,取代基R1
選自C1-
C6
-烷基和C1-
C6
-鹵代烷基;取代基R2a
、R2b
、R2c
、R3
、R7
、p、Y和Z如上文所定義。
在一個優選的實施方案中,本發明提供了式(Ica)化合物或其鹽,
式(Ica)
其中,取代基R1
代表C1-
C6
-鹵代烷基,取代基R2a
、R2b
、R2c
代表鹵素;R3
選自鹵素、氰基、C1-
C6
-烷基和C1-
C6
-烯基;R7
、Y和Z如上文所定義。
在另一個實施方案中,本發明提供了式(Id)化合物或其鹽,
式(Id)
其中,取代基R1
選自C1-
C6
-烷基和C1-
C6
-鹵代烷基;取代基R2a
、R2b
、R2c
、R3
、R7
、p和Z如上文所定義。
在一個優選的實施方案中,本發明提供式(Ida)化合物或其鹽,
式(Ida)
其中,取代基R1
代表C1-
C6
-鹵代烷基,取代基R2a
、R2b
、R2c
代表鹵素;R3
選自鹵素、氰基、C1-
C6
-烷基和C1-
C6
-烯基;R4
、R5
、R7
、Y和Z如上文所定義。
在另一個實施方案中,本發明提供了式(Ie)化合物或其鹽,
式(Ie)
其中,取代基R1
選自C1-
C6
-烷基和C1-
C6
-鹵代烷基;取代基R2a
、R2b
、R2c
、R3
、R4
、R5
、R7
和Z如上文所定義。
在一個優選的實施方案中,本發明提供了式(Iea)化合物或其鹽,
式(Iea)
其中,取代基R1
代表C1-
C6
-鹵代烷基,取代基R2a
、R2b
、R2c
代表鹵素;R3
選自鹵素、氰基、C1-
C6
-烷基和C1-
C6
-烯基;R9
代表氫;R7
和Z如上文所定義。
在本發明的一個優選實施方案中,提供了式(I)的化合物,其中,R1
選自C1-
C6
-烷基、C1-
C6
-鹵代烷基;
R2a
、R2b
和R2
獨立地選自氫、X、氰基、C1
-C6
-烷基、C1
-C6
-鹵代烷基和C3
-C8
-環烷基;
A選自苯基、噻吩基和吡啶基,其可以任選地被一個或多個R3
基團取代;
R3
選自氫、X、氰基、C1
-C6
-烷基、C1
-C6
-鹵代烷基、C2
-C6
-鹵代烯基、C3
-C8
-環烷基;
T選自、、、和其中,#表示與A鍵合,箭頭表示與Z鍵合;
R4
選自氫、C1
-C6
-烷基、C1
-C6
-鹵代烷基、C2
-C6
-C3
-C8
-環烷基、苯基和C3
-C6
-雜環基;
R5
選自氫、X、C1
-C6
-烷基、C1
-C6
-鹵代烷基、C3
-C8
-環烷基;
R6
選自氫、X、C1
-C6
-烷基;
R7
和Z獨立地選自C1
-C6
-烷基、C1
-C6
-氰基烷基、C2
-C6
-烯基、C2
-C6
-炔基、C1
-C6
-鹵代烷基、C2
-C6
-鹵代烯基、C2
-C6
-鹵代炔基、C(=O)-R″、C1
-C8
-烷基-C(=O)-R″、C(=O)-N(R′R″)、C1
-C8
-烷基-C(=O)-N(R′R″)、C2
-C8
-烯基-C(=O)-N(R′R″)、C3
-C8
-環烷基、C4
-C8
-環烯基、C4
-C8
-環炔基、苯基、萘基、噻吩基和吡啶基;其中每個R7
或Z基團可任選地被一個或多個R8
基團取代;
R8
選自氫、X、氰基、C1
-C6
-烷基、C2-
C6
-烯基、C2
-C6
-炔基、C1
-C6
-鹵代烷基、C2
-C6
-鹵代烯基、C2
-C6
-鹵代炔基、SF5
、OR4
、N(R′′)2
、Si(R′)3
、(C=O)-R″、S(O)n
R″、C1-
C8
-烷基-S(O)n
R″、C1
-C8
-烷基-(C=O)-R″、CR′=NR″、C3
-C8
-環烷基、C4
-C8
-環烯基;其中環狀環系統中的一個或多個碳原子可以被選自N、O、S基團,並且可以任選包括1-3個選自C(=O)、C(=S)、S(O)m
和Si(R′)2
的環成員的雜原子取代;
R9
選自氫、C1
-C12
-烷基、C3
-C8
-環烷基、OR4
、(C=O)-R″;或農業上可接受的鹽、異構體/結構異構體、立體異構體、非對映異構體、對映異構體、互變異構體、金屬絡合物、多晶型物或其N-氧化物。
特別地,在一個實施方案中,式(I)的化合物選自((2-氯代-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-6-甲基苯基)氨基)二甲基-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)二甲基-l6-磺胺酮;1-((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)四氫-1H-1l6-噻吩1-氧化物;1-((2-氯代-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-6-甲基苯基)氨基)四氫-1H-1l6-噻吩1-氧化物;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)二甲基-l6-磺胺酮;1-((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)四氫-1H-1l6-噻吩1-氧化物;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(3-氟苯基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(3-氟苯基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(3,5-二甲基苯基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)二乙基-l6-磺胺酮;環己基((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(甲基)(苯基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(4-甲氧基苯基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(2,6-二甲基苯基)(甲基)-l6-磺胺酮;1-((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)六氫-1l6-噻喃 1-氧化物;(2-氯代-6-甲基苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(2-甲氧基苯基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)二苯基-l6-磺胺酮;N-(環戊基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-(叔丁基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-甲氧基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((2-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-(烯丙基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;甲基3-(N-(4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯)-S-甲基磺醯亞胺基)丙酸酯;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(氧二苯基-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧化四氫-1l6-噻吩-1-基亞基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(二乙基(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((2-氰丙烷-2-基)(異丙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((2-氰丙烷-2-基)(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((2-氰丙烷-2-基)(異丙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異丙基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(氧代)(丙基)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(丙基)-l6-亞磺醯基)苯甲醯胺;N-((2-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-溴苯基)(環丙基甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((2-氯代-6-甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧化四氫-1l6-噻吩-1-基亞基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧化四氫-2H-1l6-噻喃-1-基亞基)苯甲醯胺;N-(環戊基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-溴苯基)(環丙基甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-(環己基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異丙基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((2-氰丙烷-2-基)(氧代)(丙基)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異丁基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異戊基(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(二甲基(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧化四氫-2H-1l6-噻喃-1-基亞基)苯甲醯胺;N-((3-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((3-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧負離子基-1l6-硫雜環丁烷基-1-基亞基)苯甲醯胺;N-((2-氰丙烷-2-基)(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異戊基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-(仲丁基(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-(環己基(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-(仲丁基(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異丁基(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(二甲基(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((2-氰丙烷-2-基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(苯基)-l6-亞磺醯基)苯甲醯胺;N-(叔丁基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-(三氟甲基)苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(4-(三氟甲氧基)苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異丁基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;2-(4-(N-(4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯)-S-甲基磺醯亞胺基)苯基)乙酸甲酯;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(4-(三氟甲氧基)苯基)-l6-亞磺醯基)苯甲醯胺;N-((2-氰丙烷-2-基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(二乙基(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(丙基)-l6-亞磺醯基)苯甲醯胺;N-(烯丙基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異戊基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-(環己基(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異戊基(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-(三氟甲基)苯基)-l6-亞磺醯基)苯甲醯胺;2-(4-(N-(4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯)-S-甲基磺醯亞胺基)苯基)乙酸甲酯;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異丁基(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(氧二苯基-l6-亞磺醯基)苯甲醯胺;N-((3-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(2-甲氧基乙基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧負離子基-1l6-硫雜環丁烷基-1-基亞基)苯甲醯胺;N-((2-氰丙烷-2-基)(氧代)(丙基)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺; 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(氧代)(丙基)-l6-亞磺醯基)-2-甲基苯甲醯胺;甲基3-(N-(4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯)-S-甲基磺醯亞胺基)丙酸酯; N-((2-氰基乙基)(4-乙基苯基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((2-氰基乙基)(4-甲氧基苯基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((2-氰基乙基)(氧代)(間甲苯基)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((2-氰基乙基)(4-乙基苯基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(對甲苯基)-l6-亞磺醯基)苯甲醯胺;N-((4-氰基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(4-氧負離子基-1,4l6-惡噻烷-4-基亞基)苯甲醯胺;N-((4-氰基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(4-((4-(三氟甲基)吡啶-2-基)氧基)苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4,5-二甲基噻唑-2-基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(3-氟苯基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(3-氟苯基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(氧代)(間甲苯基)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(氧代)(間甲苯基)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(4-((4-(三氟甲基)吡啶-2-基)氧基)苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((4-氰基苯基)(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-氰基苯基)(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二甲基苯基)(乙基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4,5-二甲基噻唑-2-基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;N-((4-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;N-((4-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(甲基(氧代)(苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(甲基(氧代)(間甲苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(甲基(氧代)(對甲苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺; N-((4-氰基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-甲氧基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(氧二苯基-l6-亞磺醯基)苯甲醯胺;N-((2-氰丙烷-2-基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;N-((2-氰丙烷-2-基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;N-((3-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;N-((2-氯代-6-甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(甲基(氧代)(苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;N-((2-氯代-6-甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;N-(叔丁基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;N-((2-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;N-((2-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(1-氧化四氫-2H-1l6-噻喃-1-基亞基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(氧二苯基-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-甲氧基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;N-((3-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(1-氧化四氫-2H-1l6-噻喃-1-基亞基)苯甲醯胺;N-((2,6-二氯苯基)(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;N-((2,6-二氯苯基)(異丙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(甲基(氧代)(4-(三氟甲基)苯基)-l6-亞磺醯基)苯甲醯胺;N-((3-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;(4-溴苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮;(2-氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(3,5-二甲基苯基)(甲基)-l6-磺胺酮;(3-溴苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(2,6-二甲基苯基)(甲基)-l6-磺胺酮;(4-溴苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(2,6-二甲基苯基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(2,6-二氟苯基)(甲基)-l6-磺胺酮;(3-氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮;(3-氯苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮;(3-溴苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)(苯基)-l6-磺胺酮;(2-氯代-6-甲基苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮;(3-溴苯基)(環丙基甲基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)-l6-磺胺酮;2-(N-(4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)-S-甲基磺醯亞胺基)-2-甲基丙腈;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(吡啶-2-基)-l6-磺胺酮;(2-氯苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(4-(三氟甲基)苯基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)二苯基-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(對甲苯基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二氯苯基)(乙基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二甲基苯基)(甲基)-l6-磺胺酮;4-(N-(4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)-S-甲基磺醯亞胺基)苄腈;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(3,5-二甲基苯基)(甲基)-l6-磺胺酮;(2-氯代-6-甲基苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(3-氟苯基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(苯基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二氯苯基)(異丙基)-l6-磺胺酮;(4-溴苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮;(3-溴苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮;(3-氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮;(2-氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)二苯基-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二氟苯基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二甲基苯基)(甲基)-l6-磺胺酮;(4-溴苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮; ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(苯基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(4-(三氟甲基)苯基)-l6-磺胺酮; ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(3-氟苯基)(甲基)-l6-磺胺酮;(2,6-二氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(乙基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(吡啶-2-基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(3,5-二甲基苯基)(甲基)-l6-磺胺酮;(2,6-二氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(異丙基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二氟苯基)(乙基)-l6-磺胺酮; (3-溴苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮;4-(N-(4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)-S-甲基磺醯亞胺基)苄腈;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)(對甲苯基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(2,6-二氯苯基)(乙基)-l6-磺胺酮;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(丙基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(間甲苯基亞磺醯基)苯甲醯胺; 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(間甲苯基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異丁基亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(苯基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異丙基亞磺醯基)-2-甲基苯甲醯胺;N-(丁基亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-((3-(三氟甲基)苯基)亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-((4-(三氟甲氧基)苯基)亞磺醯基)苯甲醯胺; 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-乙基苯基)亞磺醯基)-2-甲基苯甲醯胺;N-((4-(叔丁基)苯基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-乙基苯基)亞磺醯基)-2-甲基苯甲醯胺; 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苯基)亞磺醯基)-2-甲基苯甲醯胺;N-((4-(叔丁基)苯基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺; 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二甲基苯基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-乙基苯基)亞磺醯基)-2-甲基苯甲醯胺; N-((3-溴苯基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苯基)亞磺醯基)-2-甲基苯甲醯胺;N-(丁基亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(丙基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(3-(甲基氨基)-3-氧丙基)(氧代)-l6-亞磺醯基)苯甲醯胺; 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-(異丙基氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-甲氧基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((3-(環丙基氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-(環丁基氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-((2,2-二氟乙基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((3-(環丙基氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-(環丁基氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-((2,2-二氟乙基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-氧代-3-((2,2,2-三氟乙基)氨基)丙基)-l6-亞磺醯基)苯甲醯胺;N-((3-((1-氰基環丙基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-氧代-3-(丙基氨基)丙基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-(乙基(甲基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-(苄基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-氧代-3-((2,2,2-三氟乙基)氨基)丙基)-l6-亞磺醯基)苯甲醯胺;N-(苄基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-((1-氰基環丙基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-氧代-3-(丙基氨基)丙基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-(乙基(甲基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(5-(三氟甲基)吡啶-2-基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-甲氧基吡啶-2-基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-甲氧基乙基)(2-甲氧基苯基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((4-氰基苄基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((6-氟吡啶-2-基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((3-溴苯基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二甲基苯基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(苯基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-乙基苯基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-((4-(三氟甲氧基)苯基)亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-甲氧基苯基)亞磺醯基)-2-甲基苯甲醯胺; 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(萘-2-基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-氟苯基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二氟苯基)亞磺醯基)-2-甲基苯甲醯胺;N-((4-氰基苯基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-氰基苯基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-(苄基亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-甲氧基苄基)亞磺醯基)-2-甲基苯甲醯胺;N-(苄基亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二氯苯基)亞磺醯基)-2-甲基苯甲醯胺;N-((3-氰基苯基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二氯苯基)亞磺醯基)-2-甲基苯甲醯胺;N-((4-氯苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-溴苯基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-(叔丁基)苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-氯代-3-氟苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((5-氟-2-甲基苄基)亞磺醯基)-2-甲基苯甲醯胺;N-((3-氯代-5-氟苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-氯代-5-氟苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-氯代-4-氟苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺; N-((4-氯苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-(叔丁基)苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二氟苯基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二氯苯基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-甲氧基苄基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二氯苯基)亞磺醯基)-2-甲基苯甲醯胺;N-((4-溴苯基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-氰基苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-氰基苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-氰基苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(萘-2-基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-氟苯基)亞磺醯基)-2-甲基苯甲醯胺;N-((4-氰基苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苄基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-((4-(三氟甲氧基)苄基)亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-((4-(三氟甲氧基)苄基)亞磺醯基)苯甲醯胺和4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苄基)亞磺醯基)-2-甲基苯甲醯胺。
本發明的化合物可以作為一種或多種立體異構體存在。各種立體異構體包括對映異構體、非對映異構體、阻轉異構體和幾何異構體。本領域技術人員將理解,當相對於其他一種或多種立體異構體富集時或與其他一種或多種立體異構體分離時,一種立體異構體可以更具活性和/或可以顯示有益的作用。另外,技術人員知道如何分離,富集和/或選擇性地製備所述立體異構體。本發明的化合物可以以立體異構體的混合物、單獨的立體異構體的形式存在或以光學活性形式存在。
在式I化合物是陽離子或能夠形成陽離子的情況下,鹽的陰離子部分可以是無機或有機的。或者,在式I化合物是陰離子或能夠形成陰離子的情況下,鹽的陽離子部分可以是無機或有機的。鹽的無機陰離子部分的實例包括(但不限於)氯化物、溴化物、碘化物、氟化物、硫酸鹽、磷酸鹽、硝酸鹽、亞硝酸鹽、碳酸氫鹽、硫酸氫鹽。鹽的有機陰離子部分的實例包括(但不限於)甲酸鹽、鏈烷酸鹽、碳酸鹽、乙酸鹽、三氟乙酸鹽、三氯乙酸鹽、丙酸鹽、乙醇酸鹽、硫氰酸鹽、乳酸鹽、琥珀酸鹽、蘋果酸鹽、檸檬酸鹽、苯甲酸鹽、肉桂酸鹽、草酸鹽、烷基硫酸鹽、烷基磺酸鹽、芳基磺酸鹽、芳基二磺酸鹽、烷基膦酸鹽、芳基膦酸鹽、芳基二膦酸鹽、對甲苯磺酸鹽和水楊酸鹽。鹽的無機陽離子部分的實例包括(但不限於)鹼金屬和鹼土金屬。鹽的有機陽離子部分的實例包括(但不限於)吡啶、甲胺、咪唑、苯並咪唑、呱啶、磷腈、四甲基銨、四丁基銨、膽鹼和三甲胺。
式I化合物的金屬配合物中的金屬離子最常見的有:第二主族元素的離子,尤其是鈣和鎂;第三和第四主族的,尤其是鋁、錫和鉛;還有第一至第八過渡族的,特別是鉻、錳、鐵、鈷、鎳、銅、鋅等。優選為第四週期的元素和第一至第八過渡族的金屬離子。 這裡,金屬可以以它們可以呈現的各種價態存在。
在一個實施方案中,本發明提供了式(I)化合物、其農業上可接受的鹽、金屬配合物、結構異構體、立體異構體、非對映異構體、對映異構體、手性異構體、阻轉異構體、構象異構體、旋轉異構體、互變異構體、旋光異構體、多晶型物、幾何異構體或其N-氧化物及其與賦形劑、惰性載體或任何其他基本成分(例如表面活性劑、添加劑、固體稀釋劑和液體稀釋劑)的組合物。式(I)化合物的鹽優選為獸醫和/或農業上可接受的鹽,尤其是農業上可接受的鹽。它們可以按常規方式形成,例如,如果式(I)化合物具有鹼性官能團,則可以通過使化合物與所討論的陰離子的酸反應來進行。
術語“N-氧化物”包括任何具有至少一個被氧化成N-氧化物部分的叔氮原子的式(I)化合物。
式I的化合物(包括其所有立體異構體、N-氧化物和鹽)通常可以以多於一種形式存在。因此,式I包括式I表示的化合物的所有結晶和非結晶形式。非結晶形式包括固體(如蠟和膠)的實施方案以及液體(如溶液和熔體)的實施方案。結晶形式包括實質上表示單晶型的實施方案和表示多晶型混合物(即不同的晶型)的實施方案。術語“多晶型物”是一種特定結晶形式——化學化合物可以以不同結晶形式結晶,這些形式在晶格中具有不同的分子排列和/或構造。 儘管多晶型物可以具有相同的化學組成,但由於存在或不存在共結晶水或其他分子(這些共結晶水或其他分子可以在晶格中弱或強地結合),它們在組成上也可以不同。晶型在晶體形狀、密度、硬度、顏色、化學穩定性、熔點、吸濕性、懸浮性、溶解速度和生物利用度等化學、物理和生物特性上存在差異。本領域技術人員將理解,式I表示的化合物的多晶型物相對於另一種多晶型物或式I表示的相同化合物的多晶型物的混合物可顯示出有益效果(例如,適合製備有用的製劑、改善的生物學性能)。由式I表示的化合物的特定多晶型物的製備和分離可以通過本領域技術人員已知的方法實現,包括例如選擇溶劑在合適的溫度下結晶。
在一個實施方案中,本發明提供了一種製備式(I)化合物或農業上可接受的鹽的方法,
式(I)
由式(I)和/或表(I)定義的本發明化合物可以以已知的方式,如方案中所述的各種方式來製備。可以按照以下方案的步驟來製備本發明化合物,其中除非另有說明,否則每個變數的定義與上文對於式(I)化合物的定義一致。
式(IV)的化合物可以通過在合適的鹼(例如三乙胺、N,N-二異丙基乙基胺或吡啶)存在下,在合適的溶劑(如甲苯或二甲苯等)中使式(II)化合物與式(III)的三氟苯乙酮化合物反應來製備。式(V)化合物可以在乙酸酐和4-二甲基氨基吡啶等鹼的存在下通過使式(IV)化合物脫水來製備。式(VI)的化合物可以通過在合適的相轉移催化劑(例如溴化四丁基銨或氟化四丁基銨)的存在下在合適的溶劑例如(甲苯、水或其混合物)中,用羥胺(50%水溶液)處理式(V)化合物來製備。
式(Ic)的化合物可以通過在合適的偶聯劑(例如N-(3-二甲基氨基丙基)-N'-乙基碳二亞胺鹽酸鹽(EDC.HCl)、1-[雙(二甲基氨基)亞甲基]-1H-1,2,3-三唑並[4,5-b]吡啶鎓3-氧化六氟磷酸鹽(HATU)或丙烷膦酸酐(T3P))和合適的鹼(例如4-(二甲基氨基)吡啶(DMAP)、三乙胺、N,N-二異丙基乙基胺或吡啶)存在下在合適的溶劑(例如二氯甲烷、四氫呋喃、N,N-二甲基甲醯胺或其混合物)中使式(VI)的酸化合物與式(VII)的亞磺醯亞胺化合物反應來製備。
或者,式(Ic)化合物可通過在適當的溶劑(例如1,2-二氯甲烷或四氫呋喃)中使用適當的氯化試劑(例如草醯氯或氯氧化磷)將式(VI)的酸性化合物轉化為式(VIa)的醯氯化合物,然後在合適的鹼(例如4-(二甲氨基)吡啶(DMAP)、三乙胺、N,N-二異丙基乙胺)存在下,在合適的溶劑(如二氯甲烷、四氫呋喃或其混合物)中,使式(VIa)化合物與式(VII)的亞碸亞胺化合物反應來製備。
式(VIII)化合物可以通過在0℃下在四氫呋喃等合適的溶劑中使式(VI)化合物與合適的還原劑(例如硼烷四氫呋喃絡合物溶液)反應來製備。
式(IX)化合物可以在四溴甲烷和三苯膦的存在下,在二氯甲烷等合適的溶劑如中用式(VIII)化合物製備。
式(Ib)化合物可以通過在合適的鹼(例如氫化鈉)存在下,在合適的溶劑(例如N,N-二甲基甲醯胺)中使式(IX)的溴化物與式(VII)的亞磺醯亞胺化合物反應來製備。
式(Id-1)化合物可以按方案3所述的步驟,通過在0℃下在合適的溶劑(例如四氫呋喃、水或它們的混合物)中使式(Ic-1)化合物與合適的鹼(例如氫氧化鋰)反應來製備 。
式(I)的化合物可根據WO2009001942中所述的類似方法,通過在適當的相轉移催化劑(如溴化四丁基銨)存在下,用羥胺(50%水溶液)處理式(XII)化合物來製備。
式(XII)化合物可以根據WO2012026403中所述的類似步驟,通過在合適的鹼(例如1,8-二氮雜二環[5.4.0]十一碳-7-烯(DBU))的存在下,使式(XI)化合物與式(III)的三氟苯乙酮化合物反應來製備。
式(XI-a)化合物可以通過在約90°C和約100°C的溫度下,在合適的鈀催化劑例如三(二苄基亞乙基丙酮)二鈀(0)和配體(例如Xphos)的存在下,在合適的惰性溶劑(例如甲苯、二甲苯或它們的混合物)中使式(X-a)的溴化物與式(VII)的亞磺醯亞胺化合物進行Buchwald-Hartwig偶聯反應來製備。
式(XII-a)化合物可以根據WO2012026403中所述的類似方法,通過在合適的鹼(例如1,8-二氮雜二環[5.4.0]十一碳-7-烯(DBU))的存在下,使式(XI-a)化合物與式(III)的三氟苯乙酮化合物反應來製備。
式(Ia)化合物可以根據WO2009001942中所述的類似方法,通過在合適的相轉移催化劑(例如溴化四丁基銨)的存在下,用羥胺(50%水溶液)處理式(XII-a)化合物來製備。
式(XI-a)至(XI-d)化合物可通過使用以下方案6a、6b和6c所示的方法,用相應的式(X-a)至(X-d)化合物製備。
式(VII)化合物可以根據《德國應用化學》(2016, 55(25), 7203 – 7207
)或《合成快報》(2017, 28(19), 2525-38
)中所述的類似方法製備。
在一個實施方案中,本發明提供了一種製備對映體富集的式(I)化合物的有效方法。
在優選的實施方案中,本發明提供了一種製備式(I)化合物或其鹽的方法,該方法包括以下步驟:
a) 根據如下所示的反應方案,使式(XI)化合物與式(III)化合物反應,得到式(XII)化合物,;
b) 根據如下所示的反應方案,用羥胺化合物處理式(XII)化合物,得到式(I)化合物,。
根據取代基的性質,式(I)化合物及其中間體可以純形式或作為不同可能的異構體形式的混合物(例如立體異構體或結構異構體)存在。各種立體異構體包括對映異構體、非對映異構體、手性異構體、阻轉異構體、構象異構體、旋轉異構體、互變異構體、光學異構體、多晶型物和幾何異構體。
如通式1-6中所述,根據取代基的性質和相對位置(順/反式或同/反側),式(I)化合物和中間體(例如通式(V)、(XII)、(XIIa)化合物)也可以一種或多種幾何異構體形式存在。 因此,本發明同樣涉及所有比例的所有順/反式(或同/反側)異構體和所有可能的順/反式(或同/反側)混合物。順/反式(或同/反側)異構體可以根據本領域技術人員本身已知的常用方法分離。
在另一個實施方案中,本發明提供了製備式(XII)化合物或其鹽的方法。
可以通過上述方法製備式(I)化合物、其立體異構體、鹽和N-氧化物以及在合成過程中的前體。如果不能通過上述途徑製備單獨的化合物,則可以通過其他化合物(I)或相應的前體的衍生化或通過對所述合成路線進行常規改變來製備它們。例如,在個別情況下,某些式(I)化合物可以方便地由其他式(I)化合物通過衍生反應(例如通過酯水解、醯胺化、酯化、醚裂解、烯化、還原、氧化等反應)或通過對所述合成路線進行常規改變製得。
反應混合物按慣例進行處理,例如與水混合、分離相、對粗產品進行色譜純化(如果合適的話)。一些中間體和終產物以無色或略帶褐色的黏性油的形式獲得,這些油需要在減壓和適當的高溫下被純化或除去揮發性成分。如果中間體和最終產物以固體形式獲得,也可以通過重結晶或消化進行提純。
如果某個化合物(I)不能通過上述途徑獲得,則可以通過將其他化合物(I)衍生化來製備它們。但是,如果合成產生的是異構體的混合物,則通常不需要分離,因為在某些情況下,單個異構體可以在後處理使用期間或施用期間(例如在光,酸或鹼的作用下)相互轉化。此類轉化也可以在使用後(例如在處理過的植物中或在要控制的有害真菌中)進行。
在一個實施方案中,本發明提供了用於控制或預防無脊椎害蟲的組合物。該組合物包含生物有效量的式(I)化合物或其農業上可接受的鹽、異構體/結構異構體、立體異構體、非對映異構體、對映異構體、互變異構體、金屬絡合物、多晶型物或N-氧化物,以及至少一種選自表面活性劑和助劑的其他組分。
在另一個實施方案中,該組合物另外包含至少一種選自殺真菌劑、殺蟲劑、殺線蟲劑、殺蟎劑、生物農藥、除草劑、植物生長調節劑、抗生素、肥料或營養素的生物活性和相容性化合物。
在另一個實施方案中,本發明提供的式(I)化合物或其N-氧化物和鹽為常規類型的農業化學組合物,例如溶液、乳液、懸浮液、粉劑、粉末、糊劑、顆粒、壓制劑、膠囊及其混合物。組合物類型的實例是懸浮液(例如SC、OD、FS)、可乳化濃縮物(例如EC)、乳液(例如EW、EO、ES、ME)、膠囊(例如CS、ZC)、糊劑、錠劑、可濕性粉劑或粉劑(例如WP,SP,WS,DP,DS)、壓制劑(例如BR、TB、DT)、顆粒(例如WG、SG、GR、FG、GG、MG)、殺蟲製品(例如LN),以及用於處理植物繁殖材料如種子(例如GF)的凝膠製劑。這些和其他組合物類型在《農藥製劑類型和國際編碼系統》(技術專論第2號.61h版. 2008年5月.國際作物生命協會)有定義。
該組合物以已知的方式製備,製備方法在例如莫列特和格魯伯 貝恩(Mollet and Grube mann),《製劑技術》,Wiley VCH出版社,魏因海姆,2001; 或諾爾斯(Knowles),《作物保護產品製劑的新發展》(Agrow Reports DS243,T&F lnforma,倫敦,2005)中有描述。
合適的助劑有溶劑、液體載體、固體載體或填料、表面活性劑、分散劑、乳化劑、濕潤劑、佐劑、增溶劑、滲透促進劑、保護膠體、黏合劑、增稠劑、保濕劑、驅蟲劑、引誘劑、餵食興奮劑、增容劑、殺菌劑、抗-凍結劑、消泡劑、著色劑、增黏劑和黏合劑。
合適的溶劑和液體載體有水和有機溶劑,例如中沸點至高沸點的礦物油餾分,例如煤油、柴油;植物油或動物油;脂族、環狀和芳族烴,例如甲苯、石蠟、四氫化萘、烷基化萘;醇類,例如乙醇、丙醇、丁醇、苯甲醇、環己醇;乙二醇;DMSO;酮類,例如環己酮;酯類,例如乳酸、碳酸酯、脂肪酸酯、γ-丁內酯;脂肪酸;膦酸酯;胺;醯胺類,例如N-甲基吡咯烷酮、脂肪酸二甲基醯胺;及其混合物。
合適的固體載體或填料有礦物土,例如,矽酸鹽、矽膠、滑石、高嶺土、石灰石、石灰、白堊、黏土、白雲石、矽藻土、膨潤土、硫酸鈣、硫酸鎂、氧化鎂;多糖,例如纖維素、澱粉;肥料,例如硫酸銨、磷酸銨、硝酸銨、脲;植物來源的產品,例如穀物粉、樹皮粉、木粉,堅果殼粉及其混合物。
合適的表面活性劑有表面活性化合物,例如陰離子,陽離子,非離子和兩性表面活性劑,嵌段聚合物,聚電解質及其混合物。這些表面活性劑可用作乳化劑,分散劑,增溶劑,潤濕劑,滲透增強劑,保護膠體或佐劑。 表面活性劑的實例列於麥克卡森(McCutcheon),卷1:乳化劑和洗滌劑,《麥克卡森目錄》(McCutcheon's Directories),格蘭岩市,美國,2008(國際版或北美版)中。
合適的陰離子表面活性劑有磺酸鹽、硫酸鹽、磷酸鹽、羧酸鹽及其混合物的鹼金屬、鹼土金屬或銨鹽。磺酸鹽的實例有烷基芳基磺酸鹽、二苯基磺酸鹽、α-烯烴磺酸鹽、木質素磺酸鹽、脂肪酸和油的磺酸鹽、乙氧基化烷基酚的磺酸鹽、烷氧基化芳基酚的磺酸鹽、縮合萘的磺酸鹽、十二烷基和十三烷基苯磺酸鹽、萘磺酸鹽和烷基萘、磺基琥珀酸鹽或磺基琥珀醯胺酸鹽。硫酸鹽的實例有脂肪酸和油的硫酸鹽、乙氧基化烷基酚、醇、乙氧基化醇或脂肪酸酯的硫酸鹽。磷酸酯的實例有磷酸酯。羧酸鹽的實例有烷基羧酸鹽和羧化醇或烷基酚乙氧基化物。
合適的非離子表面活性劑有烷氧基化物,N-取代的脂肪酸醯胺、氧化胺、酯、糖基表面活性劑、聚合物表面活性劑,以及它們的混合物。烷氧基化物的實例有1至50當量烷氧基化醇類、烷基酚類、胺類、醯胺類、芳基酚類、脂肪酸或脂肪酸酯化合物。環氧乙烷和/或環氧丙烷可用於烷氧基化,優選環氧乙烷。N-取代的脂肪酸醯胺的實例有脂肪酸葡糖醯胺或脂肪酸鏈烷醇醯胺。酯的實例有脂肪酸酯,甘油酯或甘油單酯。糖基表面活性劑的實例有脫水山梨糖醇,乙氧基化脫水山梨糖醇、蔗糖和葡萄糖酯或烷基聚葡糖苷。聚合物表面活性劑的實例有乙烯基吡咯烷酮、乙烯醇或乙酸乙烯酯的均聚物或共聚物。
合適的陽離子表面活性劑有季銨表面活性劑,例如具有一個或兩個疏水基團的季銨化合物,或長鏈伯胺的鹽。合適的兩性表面活性劑有烷基甜菜鹼和咪唑啉。合適的嵌段聚合物有包含聚環氧乙烷和聚環氧丙烷嵌段的A-B或A-B-A型嵌段聚合物,或包含鏈烷醇、聚環氧乙烷和聚環氧丙烷的A-B-C型嵌段聚合物。合適的聚電解質有多元酸或多元醇。多元酸的實例有聚丙烯酸或聚酸梳狀聚合物的鹼鹽。多鹼的實例有聚乙烯胺或聚乙烯胺。
合適的佐劑為本身幾乎沒有殺蟲活性能夠提高式(I)化合物對目標的生物性能的化合物。實例有表面活性劑、礦物質或植物油以及其他助劑。其他例子列於諾爾斯的《佐劑和添加劑》(Agrow報告DS256, T&F lnforma英國,2006年,第5章)。
合適的增稠劑有多糖(例如黃原膠、羧甲基纖維素)、無機黏土(有機改性或未改性的)、多羧酸鹽和矽酸鹽。合適的殺菌劑有溴硝醇和異噻唑啉酮衍生物,例如烷基異噻唑啉酮和苯並異噻唑啉酮。合適的防凍劑有乙二醇、丙二醇、尿素和甘油。合適的消泡劑有矽氧烷、長鏈醇和脂肪酸鹽。合適的著色劑(如紅色、藍色或綠色)有低水溶性顏料和水溶性染料。實例是無機著色劑(如氧化鐵、氧化鈦、六氰基鐵酸鐵)和有機著色劑(如茜素-、偶氮-和酞菁著色劑)。合適的增黏劑或黏合劑有聚乙烯吡咯烷酮、聚乙酸乙烯酯、聚乙烯醇、聚丙烯酸酯、生物或合成蠟和纖維素醚。
組合物類型及其製備的實例有:
i) 水溶性濃縮物 (SL, LS)
將重量比為10-60%的式(I)化合物和重量比為5-15%的潤濕劑(例如醇烷氧基化物)溶解在重量比為100%的水和/或水溶性溶劑(例如醇)中。活性物質在用水稀釋即溶解。
ii) 分散性濃縮物 (DC)
將重量比為5-25%的式(I)化合物和重量比為1-10%的分散劑(例如聚乙烯吡咯烷酮)溶解在重量比為100%的有機溶劑(例如環己酮)中。用水稀釋得到分散性濃縮物。
iii) 可乳化濃縮物 (EC)
將重量比為15-70%的式(I)化合物和重量比為5-10%的乳化劑(例如十二烷基苯磺酸鈣和蓖麻油乙氧基化物)溶解在重量比為100%的水不溶性有機溶劑(例如芳族烴碳)中。用水稀釋得到乳液。
iv) 乳液 (EW, EO, ES)
將重量比為5-40%的式(I)化合物和重量比為1-10%的乳化劑(例如十二烷基苯磺酸鈣和蓖麻油乙氧基化物)溶解在重量比為20-40%的水不溶性有機溶劑(例如芳烴)中。通過乳化機將該混合物溶在重量比為100%的水中並製成均相乳液。用水稀釋得到乳液。
v) 懸浮液 (SC, OD, FS)
在攪拌球磨機中,將重量比為20-60%的式(I)化合物粉碎,加入重量比為2-10%的分散劑和潤濕劑(例如木質素磺酸鈉和醇乙氧基化物),重量比為0.1-2%的增稠劑(例如,黃原膠)和重量比為100%的水,得到細活性物質懸浮液。用水稀釋得到活性物質的穩定懸浮液。對於FS型組合物,加入重量比高達40%的黏合劑(例如聚乙烯醇)。
vi) 水分散性顆粒和水溶性顆粒 (WG, SG)
將重量比為50-80%的式(I)化合物粉碎,加入重量比為100%的分散劑和潤濕劑(例如木質素磺酸鈉和醇乙氧基化物),並通過技術器具(例如擠壓、噴霧塔、流化床)作為水分散性或水溶性顆粒製備。用水稀釋可得穩定的具有活性物質的分散體或溶液。
vii) 水分散性粉末和水溶性粉末 (WP, SP, WS)
將重量比為50-80%的式(I)化合物在轉子-定子磨機中研磨並添加重量比為1-5%的分散劑(例如木質素磺酸鈉)、重量比為1-3%的潤濕劑(例如醇乙氧基化物)和重量比為100%固體載體(例如矽膠)。用水稀釋得到穩定的具有活性物質的分散體或溶液。
viii) 凝膠 (GW, GF)
在攪拌球磨機中,將重量比為5-25%的式(I)化合物粉碎,加入重量比為3-10%分散劑(例如木質素磺酸鈉),重量比為1-5%增稠劑(例如羧甲基纖維素)和重量比為100%的水,得到有活性物質的細懸浮液。用水稀釋得到有活性物質的穩定懸浮液。
ix) 微乳劑 (ME)
將重量比為5-20%的式(I)化合物加入到重量比為5-30%的有機溶劑混合物(例如脂肪酸二甲基醯胺和環己酮),重量比為10-25%的表面活性劑混合物(例如醇乙氧基化物和芳基酚乙氧基化物),和重量比為100%的水。將該混合物攪拌1小時,自發產生熱力學穩定的微乳液。
x) 微膠囊 (CS)
將其含有重量比為5-50%的式(I)化合物、重量比為0-40%的水不溶性有機溶劑(例如芳烴)、重量比為2-15%的丙烯酸單體(例如甲基丙烯酸甲酯,甲基丙烯酸和二-或 將三丙烯酸酯)油相分散在保護膠體(例如聚乙烯醇)的水溶液中。自由基聚合形成聚(甲基)丙烯酸酯微膠囊。或者,將含有重量比為5-50%的根據本發明的式(I)的化合物,重量比為0-40%的水不溶性有機溶劑(例如芳烴)和異氰酸酯單體(例如二苯基甲烷-4,4'-二異氰酸酯)的油相分散到保護膠體(例如聚乙烯醇)的水溶液中。加入多胺(例如六甲基苯二胺)形成聚脲微膠囊。單體量占重量的1-10%。wt%為占微膠囊組合物總重量百分比。
xi) 可撒粉的粉末 (DP, DS)
將重量比為1-10%的式(I)化合物細碎研磨並與重量比為100%的固體載體(例如細碎的高嶺土)充分混合。
xii) 顆粒 (GR, FG)
將重量比為0.5-30%的式(I)化合物細碎研磨並與重量比為100%的固體載體(例如矽酸鹽)混合。通過擠制加工、噴霧乾燥或流化床實現造粒。
xiii) 超低量液 (UL)
將重量比為1-50%的式(I)化合物溶於重量比為100%的有機溶劑(例如芳烴)中。
i)至xiii)的組合物可任選地包含其他助劑,例如重量比為0.1-1%的殺菌劑,重量比為5-15%的防凍劑,重量比為0.1-1%的消泡劑和重量比為0.1-1%的著色劑。
在本發明的另一個實施方案中,提供了一種式(I)的農化學組合物,其包含重量比為0.01至95%,優選0.1至90%,更優選1至70%,特別是10%至60%的活性物質。和60重量%的活性物質。活性物質的使用純度為90%至100%,優選為95%至100%(根據NMR譜)。
處理植物繁殖材料(特別是種子)時,常使用種子處理溶液(LS)、懸浮乳液(SE)、可流動濃縮物(FS)、乾燥處理粉末(DS)、漿液處理用水分散性粉末(WS)通常使用水溶性粉末(SS)、乳液(ES)、可乳化濃縮物(EC)和凝膠(GF)。在二至十倍稀釋後,所述組合物在即用製劑中產生重量比為0.01至60%,優選0.1至40%的活性物質濃度。施用可在播種前或播種期間進行。
將式(I)化合物及其組合物分別施用到植物繁殖材料(特別是種子)上的方法包括敷料、包覆、造粒、撒粉和浸泡以及犁溝施用方法。優選地,分別通過拌種、造粒、包覆和撒粉這些不誘導發芽的方法將式(I)化合物或其組合物施用於植物繁殖材料上。
當用於植物保護時,根據所需效果,施用的活性物質的量為每公頃0.001至2千克,優選每公頃0.005至2千克,更優選每公頃0.05至0.9千克(特別是每公頃0.1至0.75千克)。
在處理植物繁殖材料如種子時,例如,通過撒粉、塗覆或浸透種子,活性物質的量為每100千克植物繁殖材料(通常需要優選種子)0.1至1000克,優選1至500克,更優選1至100克,最優選5至100克。
當用於材料或儲存物的保護時,所施加的活性物質的量取決於施用的類型和所需的效果。通常用於保護材料的量為每立方米經處理的材料施用0.001g至2kg,優選0.005g至1kg活性物質。
可以將各種類型的油、濕潤劑、佐劑、肥料或微量營養素以及其他農藥(例如除草劑、殺蟲劑、殺真菌劑、生長調節劑、安全劑、生物殺蟲劑)添加到活性物質或包含它們的組合物中作為預混物,或者如果合適的話使用前再加(罐裝混合)。這些試劑可以按照本發明的組合物以1:100至100:1,優選1:10至10:1的重量比混合。
使用者通常從預劑量裝置、背負式噴霧器、噴霧罐、噴霧飛機或灌溉系統施用根據本發明的組合物。通常,農業化學組合物由水、緩衝劑和/或其他助劑配製成所需的施用濃度,從而獲得即用型噴霧液或根據本發明的農業化學組合物。通常,每公頃農業有用區域施用20至6000升,優選35至1000升,更優選50至500升即用型噴霧液。
在一個實施方案中,根據本發明的組合物的各個成分,例如部分試劑或部分二元或三元混合物可以由用戶自己在噴霧罐或用於施用的任何其他種類的容器(如種子處理器鼓、種子造粒機械、背負式噴霧器)中混合,而且可以選擇添加其他輔助劑。
因此,本發明的化合物和組合物在農業上可用於保護大田作物免受食植性無脊椎動物害蟲的侵害,並且在非農業上可用於保護其他園藝作物和植物免受食植性無脊椎動物害蟲的侵害。 該效用包括保護包含通過基因工程(即轉基因)引入或通過誘變修飾的遺傳物質以提供有利性狀的農作物和其他植物(即農學和非農學的)。
本發明的化合物具有有利的代謝和/或土壤殘留模式,並表現出控制一系列農學和非農學無脊椎動物害蟲的活性。本發明的化合物在害蟲控制領域中是有價值的預防性和/或治療性活性成分(即使施用率較低),可用於針對昆蟲和蟎蟲等殺蟲劑抗性害蟲。此外,溫血動物、魚類和植物都能很好地耐受它們。
在本發明的上下文中,“無脊椎動物害蟲防治”是指抑制無脊椎動物害蟲的生長(包括死亡),顯著減少其進食或由其引起的其他傷害或破壞。在本發明中,術語“無脊椎動物害蟲”包括作為害蟲具有經濟重要性的節肢動物、腹足動物和線蟲。術語“節肢動物”包括昆蟲,蟎蟲,蜘蛛,蠍子,蜈蚣,千足蟲,球潮蟲和綜合綱。
術語“腹足動物”包括蝸牛、鼻涕蟲和其他有柱腹足目。術語“線蟲”包括所有蠕蟲,例如:蛔蟲、犬惡絲蟲和食植性線蟲,吸蟲,棘頭蟲以及絛蟲。本領域技術人員將認識到,並非所有化合物都同樣有效地對抗所有害蟲。
本發明的化合物顯示出對經濟上重要的農藝、森林、溫室、苗圃、觀賞植物、食物和纖維、公共和動物健康、家庭和商業結構、家庭和儲存的產品的害蟲的活性。這些包括鱗翅目的幼蟲,例如夜蛾科中的黏蟲、地老虎、彎曲蟲(例如秋黏蟲)、甜菜夜蛾、黑夜蛾、捲心菜、煙夜蛾;來自螟科的蛀蟲、鞘蛾、結網毛蟲、圓錐線蟲、卷葉蛾、雕葉蟲(例如歐洲玉米螟、臍橙螟、玉米根蚯蚓、草皮蚯蚓;卷葉蛾科的葉蟬、煙青蟲、種子蠕蟲和果子蠕蟲(例如蘋果蠹蛾)、葡萄漿果蛾、東方水果蛾;和許多其他經濟上重要的鱗翅目昆蟲(例如小菜蛾、粉紅鈴蟲、吉普賽蛾);蟑螂目若蟲和成蟲包括蟑螂科(例如東方蟑螂、亞洲蟑螂、德國蟑螂、褐蟑螂、美洲蟑螂、棕色蟑螂、馬德拉蟑螂);葉鞘幼蟲和鞘翅目的成蟲包括來自長角象蟲科、豆象科和象甲科的象鼻蟲(例如棉鈴象蟲、水稻象鼻蟲、糧倉象甲、水稻象鼻蟲); 甲殼類動物中的跳蚤甲蟲、黃瓜甲蟲、根蟲、葉甲蟲、馬鈴薯甲蟲和斑潛蠅(例如科羅拉多馬鈴薯甲蟲、西部玉米根蟲);來自金龜科中的金龜子和其他甲蟲(例如日本甲蟲和歐洲金龜子);來自皮蠹科的地毯甲蟲;來自叩頭蟲科的金針蟲;來自小蠹蟲科的樹皮甲蟲和來自擬步行蟲科的麵粉甲蟲。此外,它還包括:革翅目的成蟲和幼蟲,包括來自球螋科的地蜈蚣(例如歐洲球螋、黑色蠼螋);半翅目和同翅目的成蟲和若蟲,如盲蝽科的植物蟲、蟬科的蟬、來自葉蟬科的葉蟬、來自蟬科和飛虱科的稻飛虱、來自角蟬科的蚱蜢、來自木虱科科的木虱、來自粉虱科的粉虱、來自蚜蟲科的蚜蟲、來自根瘤蚜科的根瘤蚜、來自粉蚧科的粉蚧、來自蚧科、盾蚧科和球蛛科的鱗片、來自網蝽科家族的花邊蟲、來自蝽科的臭蟲、和來自長蝽科家族的扁蟲和其他種子蟲、來自沫蟬科的沫蟬、來自緣蝽科的南瓜蟲、來自紅蝽科的紅色臭蟲和汙棉蟲。還包括蜱蟎(蟎類)的成蟲和幼蟲,例如葉蟎科的蜘蛛蟎和紅蟎。(例如歐洲紅蟎、兩個斑點的蜘蛛蟎、麥克丹尼爾蟎、細須蟎科的扁蟎(例如柑橘扁蟎))、癭蟎科家族中的銹病和芽蟎以及其他對人類和動物健康有重要作用的葉蟎蟎和蟎蟲,即表皮蟎科的塵蟎、蛻皮科的卵蟎、穀蟎科的穀蟎、按硬蜱科的順序排列的蜱,例如鹿蜱(肩胛硬蜱)、澳大利亞麻痹蜱(全血球硬蜱)、美國狗蜱(變異革蜱)、孤星蜱(美洲軟蜱)和疥蟎科、疥蟎科和疥蟎科的疥蟎和蟎蟲;直翅目的成蟲和不成熟物種,包括蝗蟲、蝗蟲和蟋蟀,例如洄遊蚱蜢(例如血吸蟲黑鱸)、美國蚱蜢(例如美洲血吸蟲)、沙漠蝗蟲、 遷徙蝗蟲、家蟋蟀、鼴鼠;雙翅目的成蟲和幼蟲,包括葉蠅、蠓、果蠅、玻璃蠅、土壤蛆、家蠅(例如家蠅、小家蠅(例如廁蠅屬)、穩定蠅(例如廄螫蠅)、臉蠅、角蠅、吹蠅和其他肌肉樣蒼蠅害蟲、馬蠅(例如虻蟲))、牛蠐、鹿蠅、蝽螈(如綿羊蝽螈屬)和其他短尾蚴、蚊子(如伊蚊屬、按蚊屬、庫蚊屬)、黑蠅(如蝽螈屬、螈螈屬)、咬蚊、沙蠅、剪刀蟲和其他線蟲;纓尾目的成蟲和幼蟲,包括洋蔥薊馬和其他葉面薊馬;膜翅目昆蟲害蟲包括螞蟻(例如紅木匠螞蟻、黑木匠螞蟻、法老螞蟻、小火蟻、火蟻、紅色進口火蟻、阿根廷螞蟻、瘋狂螞蟻、路面螞蟻、玉米田螞蟻、氣味螞蟻)、蜜蜂(包括木匠蜜蜂)、黃蜂、黃茄克和黃蜂;等翅目昆蟲害蟲,包括東部地下白蟻、西部地下白蟻、臺灣地下白蟻、西印度幹木白蟻和其他具有經濟重要性的白蟻;纓尾目的害蟲如銀魚和家衣魚;食毛目的害蟲,包括頭蝨、體虱、雞體虱、狗咬虱、絨毛虱、綿羊體虱、短鼻牛虱、長鼻牛虱和其他吮吸和咀嚼攻擊人和動物寄生蝨子;蚤目的昆蟲害蟲包括東方鼠蚤、貓蚤、狗蚤、母雞跳蚤、黏性跳蚤、人類跳蚤和其他折磨哺乳動物和鳥類的跳蚤。其他被覆蓋的節肢動物害蟲包括:蜘蛛目蜘蛛、如棕色隱居蜘蛛和黑色寡婦蜘蛛、和蚰蜒目的蜈蚣、如家蜈蚣。活性還包括線蟲綱、頭足綱、吸蟲綱和棘頭綱的成員,包括經濟上重要的圓線蟲目、蛔蟲科、尖尾目、小杆目、旋尾目和嘴刺目的成員,例如但不限於經濟上重要的農業害蟲(如根結線蟲屬中的根結線蟲、短體線蟲屬中的病斑線蟲、毛刺線蟲屬的短根線蟲等。)以及動物和人類健康害蟲(即所有經濟上重要的吸蟲、絛蟲和蛔蟲,如馬中的強直線蟲、犬中的犬弓首線蟲、羊中的撚轉血茅線蟲、狗中的惡絲蟲、馬中的裸頭絛蟲屬、反芻動物中的肝片吸蟲等。
本發明化合物對鱗翅目的害蟲表現出特別高的活性,這些害蟲包括棉葉波紋夜蛾(棉葉蟲)、果樹黃卷蛾(果樹葉輥)、歐洲卷葉蛾和其他黃卷蛾屬、二化螟(水稻螟蟲)、稻縱卷葉螟(水稻螟蟲)、玉米根草螟、藍草蚯蚓、蘋果蠹蛾、多刺棉鈴蟲、斑點棉鈴蟲、美國棉鈴蟲、玉米穗蟲、煙草夜蛾、草皮蚯蚓、葡萄漿果蛾、粉紅鈴蟲、柑橘、大白蝴蝶、小白蝴蝶、小菜蛾、甜菜夜蛾、斜紋夜蛾(煙草夜蛾、叢生毛蟲)、秋季黏蟲、甘藍銀紋夜蛾和番茄潛葉蠅。
本發明的化合物對同翅目的成員也具有商業上顯著的活性,這些包括豌豆蚜蟲、豇豆蚜蟲、黑豆蚜蟲、棉蚜、甜瓜蚜蟲、蘋果蚜蟲、繡線菊蚜蟲、毛地黃蚜蟲、草莓蚜蟲、俄羅斯小麥蚜蟲、玫瑰蘋果蚜蟲、羊毛蘋果蚜蟲、桃大尾蚜蟲、穀物蚜蟲、馬鈴薯蚜蟲、桃蚜蚜蟲、綠桃蚜蟲、萵苣蚜蟲、根蚜和癭蚜、玉米葉蚜蟲、鳥櫻桃燕麥蚜蟲、綠蚜、麥長管蚜、苜蓿斑蚜、茶蚜、黑柑橘蚜蟲)和褐色柑橘蚜蟲;球蚜屬;根瘤蚜;美核桃根瘤蚜;粉虱(煙草粉虱、甘薯粉虱)、類作物的銀葉粉虱(銀葉粉虱)、柑橘粉虱和溫室粉虱;馬鈴薯葉蟬、較小的褐飛虱、紫菀葉蟬、綠葉蟬、稻葉蟬、褐飛虱、玉米飛虱、白背飛虱、稻飛虱、白蘋果葉蟬、葡萄葉蟬;叢生蟬;冰草屬(棉墊鱗)、毒死蜱屬(聖約瑟鱗);柑桔疫黴屬(柑桔粉虱);假球菌屬(其他粉虱複合體);赤黴屬(梨木虱)、柿子木虱。
這些化合物還對半翅目的成員具有活性,這些成員包括綠色臭蟲、南瓜蟲、長蝽若蟲、棉花邊蟲、番茄蟲、汙棉蟲、桉褐色臭蟲(棕色臭蟲)、桉褐色斑潛蠅(單點臭蟲)、葡萄球菌(種蟲複合體)、葉足松種子蟲、桉褐斑潛蠅、變色植物蟲、內紮拉病毒性林奈(南方綠臭蟲)、美洲大蠹(稻臭蟲)、大乳草蟲、棉蚤。
本發明化合物可以控制的其他昆蟲目包括纓翅目(例如、西花薊馬、柑橘薊馬、大豆薊、和洋蔥薊馬;和鞘翅目(例如,科羅拉多馬鈴薯甲蟲、墨西哥豆甲蟲和屬於金針蟲、或吸蟲屬的線蟲)。
特別地,式(I)化合物,它們的N-氧化物、它們的異構體、它們的多晶型物和它們的鹽特別適用於有效地對抗下列害蟲:來自鱗翅類(鱗翅目)的昆蟲,例如小地老虎、黃地老虎、棉葉波紋夜蛾、黎豆夜蛾、銀蛾科的蘋果銀蛾、紋夜蛾、松尺蠖、樅卷葉蛾、煙捲蛾、冬尺蛾、二點螟、雲杉卷葉蛾、樅色卷蛾、一點黏蟲、蘋果蠹蛾、歐洲松毛蟲、黃瓜絹野螟、西南玉米螟、棉斑實蛾、翠紋鑽夜蛾、南美玉米苗斑螟、葡萄與蘋果卷葉蛾、斑點夜蛾、大蠟螟、小卷葉蛾、梨小食心蟲、棉鈴蟲、棉鈴夜蛾、玉米穗蟲、菜心螟、美國白蛾、蘋果巢蛾、番茄莖麥蛾、鐵杉尺蠖、甜菜夜蛾、咖啡潛葉蛾、旋紋潛葉蛾、金紋細蛾、葡萄蛾、草地螟、黃斑螟、舞毒蛾、舞白頭鶴、桃潛葉蛾、走狗蛾、甘藍夜蛾、黃杉毒蛾、歐洲玉米螟、小眼夜蛾、棉紅鈴蟲、疆夜蛾、圓掌舟蛾、馬鈴薯塊莖蛾、柑桔潛葉蛾、菜粉蝶、苜蓿綠夜蛾、小菜蛾、大豆夜蛾、美松梢小卷蛾、三化螟、陰囊蚤、麥蛾、葡萄長須卷蛾、草地貪夜蛾、棉貪夜蛾、斜紋夜蛾、甜菜夜蛾、松行列蛾、櫟綠卷蛾、粉紋夜蛾和加拿大一枝黃花小卷蛾;和甲蟲(鞘翅目),例如梨窄吉丁、直條叩頭蟲、暗色叩頭蟲、六月金龜子、茴香屬、棉鈴象甲、蘋花象、蚜蠅科、舌甘菜隱食甲、縱坑切梢小蠹、蠶豆象、豌豆象、歐洲兵豆象、梨卷葉象、甜菜大龜甲、菜豆瑩葉甲、金花金龜、白菜籽龜象、白菜籽龜象、甜菜脛跳甲、煙草金針蟲、刁柏負泥蟲、長角葉甲,葉甲屬、黃瓜甲蟲、南美葉甲、玉米根蟲、墨西哥豆瓢蟲、煙草跳甲、象變種、松象甲、葉象甲屬、葉象甲、雲杉樹皮甲蟲、勒馬天蛾、黑角負泥蟲、馬鈴薯甲蟲、甜菜叩甲、稻水象甲、油菜露尾甲、鰓金龜、大栗鰓角金龜、水稻負泥蟲、黑葡萄耳象、、樹葉象、油菜金頭跳甲、食葉鰓金龜屬種、庭園發麗金龜、菁淡足跳甲、黃曲條菜跳甲、日本麗金龜、和穀象;蒼蠅、蚊子(雙翅目),例如埃及伊蚊、白紋伊蚊、白紋伊蚊、按實蠅、五斑按蚊、災難按蚊、白魔按蚊、岡比亞按蚊、泛生按蚊、白斑按蚊、小按蚊、四孔按蚊、紅頭麗蠅、地中海實蠅、蛆症金蠅、古人類按蚊、黃斑按蚊、盤金龜子、矽金龜子、大西洋按蚊、嗜人錐蠅、 高梁癭蚊、人皮蠅、毛庫蠓、尖音庫蚊、黑須庫蚊、致倦庫蚊、跗葉庫蚊、紫色庫蚊、黑尾賽蚊、瓜實蠅、油橄欖實蠅、油菜葉癭蚊、蔥蠅、麥地種蠅、灰地種蠅、甘藍地種蠅、人膚皮蠅、夏廁蠅、尺禾蠅屬、腸胃蠅、 刺舌蠅、須舌蠅、須舌蠅、舌蠅屬、擬寄舌蠅、西方角蠅、潛蠅屬、種蠅、紋皮蠅、托氏細蠓、美洲斑潛蠅、三葉斑潛蠅、巴西綠蠅、銅綠蠅、絲光綠蠅、曼蚊屬、黑森癭蚊、秋家蠅、家蠅、廄腐蠅、發情羊屬、禾蠅屬、瑞典麥稈蠅、天仙子泉妮、廄腐蠅、蘿蔔蠅、草種蠅屬、銀足白蛉、哥倫比亞鱗蚊、胡蘿蔔莖蠅、鱗蚊屬、原蚋屬、櫻桃繞實繩、蘋果實蠅、赤尾麻蠅、麻蠅屬、帶蚋、廄螫蠅、牛虻、北美黑虻、馬蠅、和虻屬、大蚊屬、和沼澤大蚊;白蟻目(等翅目),例如異白蟻、北美散白蟻、南方散白蟻、南歐網紋白蟻、桑特散白蟻、臺灣乳白蟻;蟑螂(蜚蠊目),例如德國蜚蠊、亞洲蜚蠊、美洲大蠊、日本大蠊、棕色蟑螂、黑胸大蠊、澳洲大蠊、和東方蜚蠊;螞蟻、蜜蜂、黃蜂、葉蜂(膜翅目)例如菜葉蜂、熱帶切葉蟻屬、大頭美切葉蟻、切葉蟻、德克薩斯切葉蟻、舉腹蟻屬、黑蟻、黃家蟻、火蟻、紅火蟻、黑火蟻、紅收穫蟻、收割機螞蟻、大頭蟻、袋蚊蜂屬、熊蜂屬、黃斑胡蜂、賓夕凡尼亞木蠊、黃邊胡蜂、長腳蜂、佛羅裏達弓背蟻、和阿根廷蟻;蟋蟀、蚱蜢、蝗蟲(直翅目),例如家蟋蟀、歐洲螻蛄、東亞飛蝗、雙帶蚱蜢、紅足黑蝗、墨西哥黑蟲皇、血黑蝗、落磯山蝗、紅翅蝗、美洲沙漠蟲皇、沙漠蝗蟲、摩洛哥戟紋蝗、加爾小車蟲皇、印度黃檀蝗、義大利蝗、澳洲疫蝗、和褐飛蝗;蜘蛛目,例如黑寡婦蜘蛛和人類被棕色遁蛛;跳蚤(蚤目),例如貓櫛首蚤、狗跳蚤、印鼠客蚤、致癢蚤、穿皮潛蚤、和具帶病蚤、蠹蟲、家衣魚(纓尾目),例如小灶衣魚、蜈蚣(蜈蚣類),例如取食螞蟻、多足類(倍足綱),例如蠼螋(革翅目),例如地蜈蚣、蝨子(虱毛目),例如人頭虱、人體虱、人體陰虱、牛血風、豬血虱、牛顎虱、牛羽虱和水牛盲虱;彈尾目(跳蟲),例如棘跳蟲屬。
他們也適用於控制線蟲:植物寄生線蟲,如根結線蟲、北方根結線蟲、南方根結線蟲、爪哇根結線蟲和其他根結線蟲;囊腫形成線蟲、馬鈴薯金線蟲和其他線蟲物種;燕麥胞囊線蟲、大豆胞囊線蟲、甜菜胞囊線蟲、三葉草胞囊線蟲和其他異皮蟲物種;種子線蟲、蛇墊刃種;莖和葉線蟲、滑刃線蟲物種;刺線蟲、芹刺線蟲和其他刺線蟲物種;松材線蟲、傘滑刃松材線蟲和其他松材線蟲;環線蟲、環屬物種、小環線蟲物種、輪線蟲物種、中環線蟲物種;莖和鱗莖線蟲、甘薯莖線蟲、鱗球莖莖線蟲和其他莖線蟲屬物種;錐線蟲、錐線蟲物種;螺旋線蟲、香蕉螺旋線蟲和其他螺旋線蟲物種;鞘和鞘線蟲、鞘線蟲物種和半輪線蟲物種;潛根線蟲屬物種;矛線蟲,矛線蟲屬;假根線蟲、珍珠線蟲物種;針線蟲、延伸長針線蟲和其他長針線蟲物種;病斑線蟲、落選短體線蟲、穿刺短體線蟲、彎曲針線蟲、短體線蟲和其他短體線蟲物種;穴居線蟲、香蕉穿孔線蟲和其他穿孔線蟲物種;腎形腎狀線蟲,盤旋線蟲和盤旋線蟲物種;盾線蟲物種;短粗根線蟲、軟骨毛刺線蟲和其他毛刺線蟲物種、擬毛刺物種;矮化線蟲,克萊頓矮化線蟲,順逆矮化線蟲和其他矮化線蟲物種;柑橘線蟲、穿刺線蟲物種;匕首線蟲、劍線蟲物種;和其他植物寄生線蟲種類。
式(I)化合物及其鹽也可用於控制蛛形綱動物(蛛形綱),例如蟎蟲(蜱蟎目),例如隱喙蜱、硬蜱科和疥蟎物種,如美洲花蜱、飾鈍眼蜱、波斯銳緣蜱、具環牛蜱、微小牛蜱、森林革蜱、長喙璃眼蜱、篦子硬蜱、淺紅硬蜱、非洲鈍緣蜱、與壁蟲、雞皮刺蟎、羊癢蟎、附加扇頭蜱、外翻扇頭蜱、疥蟎,和癭蟎科物種,如蘋果刺鏽蟎,柑橘鏽蟎和柑橘癭蟎;跗線蟎科,如側多食跗線蟎;細須蟎科,如紫紅短須蟎;葉蟎科,如朱砂葉蟎、神澤氏葉蟎、太平洋葉蟎、棉葉蟎和二斑葉蟎、蘋果全爪蟎、全爪蟎和草地小爪蟎。
在本發明的另一個實施方案中、式(I)化合物可用於防治選自吮吸或刺穿昆蟲的昆蟲、例如來自纓翅目、雙翅目和半翅目的昆蟲,特別是以下物種:
纓翅目:富氏小蠊、枕骨小蠊、黑線小蠊、檸檬黃薊馬、稻瘟病薊馬、棕櫚薊馬和薊馬;
雙翅目:例如埃及伊蚊、白紋伊蚊、白紋伊蚊、按實蠅、五斑按蚊、災難按蚊、白魔按蚊、岡比亞按蚊、泛生按蚊、白斑按蚊、小按蚊、四孔按蚊、紅頭麗蠅、地中海實蠅、蛆症金蠅、古人類按蚊、黃斑按蚊、盤金龜子、矽金龜子、大西洋按蚊、嗜人錐蠅、 高梁癭蚊、人皮蠅、毛庫蠓、尖音庫蚊、黑須庫蚊、致倦庫蚊、跗葉庫蚊、紫色庫蚊、黑尾賽蚊、瓜實蠅、油橄欖實蠅、油菜葉癭蚊、蔥蠅、麥地種蠅、灰地種蠅、甘藍地種蠅、人膚皮蠅、夏廁蠅、尺禾蠅屬、腸胃蠅、刺舌蠅、須舌蠅、舌蠅屬、擬寄舌蠅、西方角蠅、潛蠅屬、種蠅、紋皮蠅、托氏細蠓、美洲斑潛蠅、三葉斑潛蠅、巴西綠蠅、銅綠蠅、絲光綠蠅、曼蚊屬、黑森癭蚊、秋家蠅、家蠅、廄腐蠅、發情羊屬、禾蠅屬、瑞典麥稈蠅、天仙子泉妮、廄腐蠅、蘿蔔蠅、草種蠅屬、銀足白蛉、哥倫比亞鱗蚊、胡蘿蔔莖蠅、鱗蚊屬、原蚋屬、櫻桃繞實繩、蘋果實蠅、赤尾麻蠅、麻蠅屬、帶蚋、廄螫蠅、牛虻、北美黑虻、馬蠅、和虻屬、大蚊屬和沼澤大蚊;
半翅目,尤其是蚜蟲類:無網管蚜、落葉松球蚜、納豆蚜、蠶豆蚜、福建蚜、蘋果蚜、棉蚜、北美荼簏子姆、苔草蚜、卷葉蟲牙、豌豆長管蚜、茄溝無網蚜、短尾蚜屬、李短尾蚜、桃仁短尾蚜、短尾蝗、菜蚜、釘毛蚜、中瘤釘毛蚜、荼薦隱瘤姆、椎球蟲牙、雲杉椎球蟲牙、圓尾蚜、車前圓尾蚜、馬鈴薯小綠葉蟬、大尾蟲牙、超瘤蚜屬、麥長管蚜、馬鈴薯長管蚜、管蟲牙、巢菜修尾蚜、色蚜、麥無網長管蚜、冬蔥瘤額蚜、瘤蚜、衲長管蚜屬、褐飛虱、囊柄瘦綿蟲牙、甘蔗扁角飛虱、忽布疣額蚜、及蘋果木虱、梨木虱、玉米縊管蚜、稻麥蚜、圓尾蚜、麥二叉蚜、裂鞘葉蚜、麥長管蚜、溫室粉虱、桔二叉蚜和葡萄根瘤蚜。
在一個實施方案中,本發明提供包含生物有效量的式(I)化合物和至少一種另外的選自殺真菌劑、殺蟲劑、殺線蟲劑、殺蟎劑、生物殺蟲劑、除草劑、植物生長調節劑、抗生素、肥料和營養素的生物活性相容化合物的組合物。該組合物中使用的化合物和與式(I)化合物組合的化合物也稱為活性相容化合物。
已知的和報導的殺真菌劑、殺蟲劑、殺線蟲劑、殺蟎劑、生物殺蟲劑、除草劑、植物生長調節劑、抗生素和營養素可以與至少一種本公開的式(I)化合物組合。例如,WO2016156129和WO2017153200中公開和報導的殺真菌劑、殺蟲劑、殺線蟲劑、殺蟎劑、生物殺蟲劑、除草劑、植物生長調節劑、抗生素、肥料和營養素可以與至少一種本公開的式(I)化合物組合。
WO2016156129和WO2017153200中報導的殺真菌劑、殺蟲劑、殺線蟲劑、殺蟎劑、生物殺蟲劑、除草劑、植物生長調節劑、抗生素、肥料和營養素與至少一種本發明的式(I)化合物的結合應納入本文作為非限制性實施例。
特別地,本發明的化合物可以與至少一種另外的生物活性相容化合物混合形成多組分農藥,提供更廣泛的農業用途。所述化合物包括但不限於殺蟲劑、殺真菌劑、殺線蟲劑、殺菌劑、殺蟎劑、生長調節劑如生根刺激劑、化學絕育劑、化學資訊素、驅避劑、引誘劑、資訊素、餵食興奮劑、其他生物活性化合物或昆蟲病原細菌、病毒或真菌。
WO2019072906A1(第27至37頁)公開了可以與本發明的式(I)化合物組合/配製的此類生物活性化合物或試劑/配製物的實例。
在一個實施方案中,用於與本發明化合物混合的生物製劑包括蘇雲金芽孢桿菌、蘇雲金芽孢桿菌δ內毒素以及天然存在的和基因改造的病毒殺蟲劑,包括杆狀病毒科的成員以及昆蟲真菌。
在某些情況下,與其他無脊椎害蟲防治化合物或具有相似控制譜但具有不同作用模式的試劑的組合特別有利於抗性管理。因此,本發明的組合物可以進一步包含至少一種另外的生物有效量的無脊椎害蟲防治化合物或具有相似控制譜但具有不同作用模式的試劑。接觸經生物學有效量的本發明化合物基因改造的植物或植物的的位點以表達植物保護化合物(例如,蛋白質)也可以提供更廣譜的植物保護並且有利於抗性管理。
在本發明的一個實施方案中,組合物中式(I)化合物的生物有效量為組合物總重量的0.1%至99%,優選5%至50%。
本發明還涉及一種對抗昆蟲和蟎害蟲的方法,所述方法包括用生物有效量的本發明化合物或組合物接觸無脊椎動物害蟲、其棲息地、繁殖地、食物、植物、種子、土壤、無脊椎動物害蟲生長或可能生長的區域、材料或環境,或希望免受蟲害或侵擾的材料、植物、種子、土壤。
通過將一種或多種本發明化合物以有效量施用於害蟲的環境,包括農藝和/或農藝上侵染的位點、要保護的區域或直接在要控制的害蟲上來實現對無脊椎動物害蟲的控制和對農藝、園藝和特種作物的保護、實現動物和人類健康。因此,本發明進一步包括控制葉和土壤棲息的無脊椎動物和保護農藝和/或非農作物的方法,包括使無脊椎動物或其環境與生物有效量的一種或多種本發明化合物接觸,或包含至少一種這樣的化合物的組合物或包含至少一種這樣的化合物和有效量的至少一種另外的生物活性化合物或藥劑的組合物。優選的接觸方法是噴霧。或者,包含本發明化合物的顆粒組合物可以施用於植物葉子或土壤。本發明的化合物通過使植物與包含本發明化合物的組合物接觸而通過植物攝取有效遞送,所述組合物作為液體製劑的土壤浸漬劑、顆粒製劑施用於土壤,育苗箱處理或浸漬。其他接觸方法包括通過直接和殘留噴霧、空氣噴霧、種皮、微囊化、全身攝取、誘餌、耳標、大丸劑、噴霧劑、薰蒸劑、氣溶膠、粉塵和許多其他方法施用本發明的化合物或組合物。
本發明的化合物可以摻入由無脊椎動物喜愛的誘餌中或在諸如誘捕器等裝置內。包含0.01-5%活性成分、0.05-10%保濕劑和40-99%植物粉的顆粒或誘餌,特別是通過攝入而不是通過直接接觸活性成分劑量下致死能在非常低的施用率下有效控制土壤昆蟲。本發明的化合物可以其純態施用,但最常應用的施用是配合包含一種或多種具有合適載體、稀釋劑和表面活性劑的化合物的製劑,也有可能與食物組合,這取決於預期的最終用途。優選的施用方法包括噴灑化合物的水分散體或精製油溶液。與噴霧油、噴霧油濃度、塗布劑貼劑、佐劑、其他溶劑和增效劑(如胡椒基丁醚)的組合通常可提高化合物功效。
有效控制所需的施用率(即“生物有效量”)將取決於諸如待控制的無脊椎動物的種類、有害生物的生命週期、生命階段、其大小、位置、季節、宿主作物或動物、攝食行為、交配行為、環境濕度、溫度等。在正常情況下,每公頃約0.01至2千克活性成分的施用量足以控制農業生態系統中的害蟲,但也有公頃可能只需要0.0001千克,或需要多達8千克。對於非農藝用途,有效使用率範圍約為1.0至50毫克/平方米,但也可能只需0.1毫克/平方米,最多可能需要150毫克/平方米。本領域技術人員可以容易地確定防治無脊椎害蟲水準所需的生物有效量。
可以通過本領域已知的施用方法使植物生長的動物害蟲(即昆蟲、蜘蛛和線蟲)、植物、土壤或水與式(I)化合物和它們的N-氧化物和鹽或含有它們的組合物接觸。因此,“接觸”包括直接接觸(將化合物/組合物直接施用於動物害蟲或植物上通常施用於植物的葉子,莖或根)和間接接觸(將化合物/組合物施用於動物害蟲或植物的所在地)。
本發明的化合物或包含它們的殺蟲組合物可用於通過使植物/作物與殺蟲有效量的至少一種本發明的化合物接觸來保護生長的植物和作物免受動物害蟲(特別是昆蟲、蟎科或蜘蛛)的侵擾或侵染。“作物”一詞指正在生長的和收穫的作物。
在一個實施方案中,本發明提供了一種保護作物免受無脊椎動物有害生物攻擊或侵擾的方法,該方法包括使作物與生物有效量的本發明化合物或組合物、異構體、多晶型、N-氧化物或其鹽接觸。
本發明的化合物可以原樣使用或以組合物的形式使用殺蟲有效量的活性化合物處理昆蟲或植物、植物繁殖材料,如種子、土壤、表面、材料或空間使其免受殺蟲性攻擊。施用可以在植物、植物繁殖材料、例如昆蟲的種子,土壤,表面,材料或感染之前和之後間進行感染之前和之後。
在一個實施方案中,本發明提供了一種保護種子免受土壤昆蟲侵害和保護幼苗免受土壤和葉蟲侵害的根和芽的方法,該方法包括在種子播種之前和/或萌芽之後與本發明化合物或其組合物、N-氧化物或其鹽接觸種子。
此外,本發明涉及治療或保護動物免受寄生蟲侵擾或感染的方法,該方法包括口服,局部或腸胃外給予或給動物施用生物有效量的本發明化合物或組合物、異構體、多晶型物、N-氧化物或獸醫學上可接受的鹽。
對於在農業或園藝作物中用於處理農作物植物,本發明化合物的施用率(施用有效劑量)可以在1g至5000/公頃的範圍內,優選25g至600g/公頃,更優選每公頃50g至500g克。
本發明的化合物和組合物特別適用於控制各種栽培植物上的多種昆蟲,例如穀類、塊根作物、油料作物、蔬菜、香料、觀賞植物,例如硬粒小麥和其他小麥的種子、大麥、燕麥、黑麥、玉米(飼料玉米和糖玉米/甜和田玉米)、大豆、油料作物、十字花科植物、棉花、向日葵、香蕉、大米、油菜、蕪菁油菜、甜菜、飼料甜菜、茄子、土豆、草、草坪、草皮、飼料草、番茄、韭菜、南瓜/南瓜、白菜、卷心萵苣、胡椒、黃瓜、甜瓜、芸苔屬植物、甜瓜、豆類、豌豆、大蒜、洋蔥、胡蘿蔔、馬鈴薯等塊莖植物、甘蔗、煙草、葡萄、矮牽牛、天竺葵/香葉天竺葵、三色紫羅蘭和鳳仙花。
特別地,本發明的化合物或組合物可用於保護農作物,例如穀物、玉米、水稻、大豆和其他豆科植物、水果和果樹、葡萄、堅果和堅果樹、柑橘和柑橘樹、任何園藝植物、葫蘆科、含油植物、煙草、咖啡、茶、可可、甜菜、甘蔗、棉花、馬鈴薯、番茄、洋蔥、辣椒和其他蔬菜和觀賞植物。
本發明的化合物通過接觸(通過土壤、草、牆壁、床網、地毯、植物部分或動物部分)和攝取(誘餌或植物部分)都有效。
本發明的化合物還可以用於非作物昆蟲和蟎害蟲,例如螞蟻、白蟻、黃蜂、蒼蠅、蚊子、蟋蟀或蟑螂。為了對抗所述非作物害蟲,本發明化合物優選用於誘餌合成物中。
誘餌可以是液體,固體或半固體製劑(例如凝膠)。固體誘餌可以形成適合於各自的施用的各種形狀和形式,例如顆粒、塊、棒、盤。液體誘餌可以填充到各種裝置中以確保適當的應用,例如開口容器、噴霧裝置、液滴源或蒸發源。凝膠可以基於水性或油性基質,並且可以在黏性、保濕性或老化特性方面配製成特定的必需品。
該組合物中使用的誘餌是一種產品,其足以吸引諸如螞蟻、白蟻、黃蜂、蒼蠅、蚊子、蟋蟀等昆蟲或蟑螂來食用它。可以通過使用餵食興奮劑或性資訊素來操縱吸引力。例如,可以但不限於是從動物和/或植物蛋白(肉、魚粉、昆蟲部分、蛋黃)、動物和/或植物來源的脂肪和油、或單-、寡糖聚有機糖類、低聚聚有機糖、尤其是蔗糖、乳糖、果糖、右旋糖、葡萄糖、澱粉、果膠或甚至糖蜜或蜂蜜選擇食物興奮劑。水果、作物、植物、動物、昆蟲或其特定部分的新鮮或腐爛部分也可用作餵食刺激劑。已知性資訊素更具昆蟲特異性。特定的資訊素在文獻中描述並且是本領域技術人員已知的。
用於誘餌組合物時,活性成分的典型含量為占重量比的0.001%至15%,理想地為占重量比的0.001%至5%。
配置本發明化合物作為噴霧劑(例如噴霧罐)、油噴霧劑或泵式噴霧劑非常適合於非專業用戶控制害蟲如蒼蠅、跳蚤、蜱、蚊子或蟑螂。噴霧劑配方優選由活性化合物,溶劑如低級醇(如甲醇、乙醇、丙醇、丁醇),酮類(如丙酮、甲基乙基酮),沸程約為50-250°C石蠟烴(如煤油)、二甲基甲醯胺、N-甲基吡咯烷酮、二甲基亞碸、芳香族烴類如甲苯、二甲苯、水、以及輔助劑如乳化劑如山梨糖醇單油酸酯、油醯基乙氧基化物、具有3-7摩爾環氧乙烷、脂肪醇乙氧基化物、香料油等作為醚油、中等脂肪酸與低級醇的酯、芳香族化合物、如果合適的話,穩定劑如苯甲酸鈉、兩性表面活性劑、低級環氧化物、原甲酸三乙酯、如果需要,推進劑如丙烷、丁烷、氮氣、壓縮空氣、二甲醚、二氧化碳、硝基氧化物或這些氣體的混合物組成。
噴油配方與噴霧配方的不同之處在於不使用推進劑。在噴霧組合物中,活性成分的占總重量的0.001至80%,優選0.01至50%,最優選0.01至15%。
本發明的化合物及其各自的組合物也可用於蚊香和薰蒸線圈,煙盒,蒸發器板或長期的噴霧器以及蛾紙、蛾墊或其他不依賴於熱的蒸發器系統。
用式(I)化合物及其各自的組合物控制由昆蟲(例如瘧疾,登革熱和黃熱病,淋巴絲蟲病和利什曼病)傳播的傳染病的方法也包括小屋和房屋的表面處理、空氣噴灑和窗簾、帳篷、衣物、蚊帳的浸漬、采蠅捕捉器等。 用於纖維、織物、針織品、非織造織物、網狀材料或箔和防水油布的殺蟲組合物優選包含含有殺蟲劑,任選的驅蟲劑和至少一種黏合劑的混合物。合適的驅蟲劑有例如N,N-二乙基-間甲苯醯胺(DEET)、N,N-二乙基苯基乙醯胺(DEPA)、1-(3-環己烷-1-基-羰基)-2-甲基呱啶、(2-羥甲基環己基)乙酸內酯、2-乙基-1,3-己醇和醇、甲基十二醯胺(MNDA)、一種不用於昆蟲控制的擬除蟲菊酯,如(+/-)-3-烯丙基-2-甲基-4-氧代環戊-2-(+)-烯基-(+)-反式-菊酸酯(殺蚊靈)、一種來自或與植物提取物相同的驅蟲劑,如檸檬烯、丁子香酚、來自像單葉蔓荊、檸檬草等粗植物提取物。合適的黏合劑選自例如脂族酸的乙烯基酯(例如乙酸乙烯酯和叔碳酸乙烯酯)的聚合物和共聚物,醇的丙烯酸和甲基丙烯酸酯,例如丙烯酸丁酯、2-乙基己基丙烯酸酯、和丙烯酸甲酯、單和二烯屬不飽和烴,如苯乙烯和脂族二烯,如丁二烯。
通常簾子和蚊帳的浸漬方法是通過將紡織材料浸入殺蟲劑的乳液或分散劑中或將它們噴灑到網上。
本發明的化合物及其組合物可用於保護木質材料,例如樹木、板圍欄、枕木等、以及建築物,例如房屋、外屋、工廠,以及建築材料、傢俱、皮革、纖維、乙烯基製品,電線和電纜等免受螞蟻和/或白蟻的侵擾,用於控制螞蟻和白蟻對作物或人類造成傷害(例如當害蟲侵入房屋和公共設施時)。本發明的化合物不僅應用於周圍的土壤表面或地板下的土壤中以保護木質材料,而且還可以應用於諸如地板下混凝土、壁龕柱、梁、膠合板、傢俱等,木質製品如刨花板、半板等和乙烯基製品如塗層電線、乙烯基片、絕緣材料如苯乙烯泡沫等等的表面上。
本發明的化合物用於防治螞蟻危害農作物或者人類的,施用於農作物或者周圍土壤,或者直接應用於螞蟻窩等。種子處理
本發明還進一步涉及包含本發明化合物的種子,特別地,其含量為處理前種子重量的約0.0001%至約1%。
本發明的化合物還可用於處理種子來保護種子免受昆蟲蟲害,特別是土壤生活昆蟲和蟎蟲的侵擾,而且所得植物的根和芽可抵抗土壤害蟲和葉子昆蟲。
本發明的化合物用於保護種子免受土壤害蟲的侵擾,以及保護植物長出的根和芽免受土壤害蟲和葉子昆蟲的侵擾尤其有用。可優選用來保護植物長出的根和芽。更優選的是保護所得植物的枝條免受刺穿和吸吮昆蟲的侵擾,最優選的是保護其免受蚜蟲、葉蟬、薊馬和粉虱的侵擾。
因此,本發明包括保護種子免受昆蟲(特別是土壤昆蟲)侵擾,保護的幼苗根和芽免受昆蟲(特別是土壤和葉子昆蟲)侵擾的方法,所述方法包括在播種前和/或在催芽後使其本發明化合物接觸種子。在這種方法中,特別優選的是保護其中植物的根和枝被,更優選地是保護其中植物枝條免受昆蟲刺穿和吸吮,最優選的方法保護其中植物枝條免受蚜蟲的侵擾。
術語“種子”包括各種種子和植物繁殖體,包括但不限於真實種子、種子片、吸盤、球莖、球莖、果實、塊莖、穀粒、插條、切枝等,並且在優選實施方案中是指真正的種子。
術語種子處理包括本領域已知的所有合適的種子處理技術,例如拌種、種子包衣、種子撒粉、種子浸泡和種子制粒。
本發明還包括塗有或含有活性化合物的種子。種子可以用含有本發明化合物的種子包衣組合物包衣。例如,在EP3165092、EP3158864、WO2016198644、WO2016039623、WO2015192923、CA2940002、US2006150489、US2004237395、WO2011028115、EP2229808、WO2007067042、EP1795071、EP1273219、WO200178507、EP1247436、NL1012918和CA2083415中報導的種子包衣組合物。
術語“塗有和/或含有”通常表示活性成分在施用時大部分在繁殖產品的表面上,儘管成分的更多或更少部分可以滲透到繁殖產品中,取決於應用方法。當(再)種植所述繁殖產品時,它可以吸收活性成分。
合適的種子是穀物、塊根作物、油料作物、蔬菜、香料、觀賞植物的種子、例如硬粒小麥種子和其他小麥、大麥、燕麥、黑麥、玉米(飼料玉米和糖玉米/甜玉米田)、大豆、 油料作物、十字花科植物、棉花、向日葵、香蕉、大米、油菜、蕪菁油菜、甜菜、飼料甜菜、茄子、土豆、草、草坪、草皮、飼料草、番茄、韭菜、南瓜/南瓜、捲心菜、卷心萵苣、胡椒、黃瓜、甜瓜、芸苔屬植物、甜瓜、豆類、豌豆、大蒜、洋蔥、胡蘿蔔、塊莖植物如土豆、甘蔗、煙草、葡萄、矮牽牛、天竺葵、三色紫羅蘭和鳳仙花。
此外,本發明的化合物可用於處理由於育種(包括基因工程方法)而耐受除草劑或殺真菌劑或殺蟲劑的作用的植物種子。
例如,本發明的化合物可用於處理植物的種子,所述植物對除磺醯脲、咪唑啉酮、草銨膦或草甘膦-異丙基銨和類似活性物質的除草劑具有抗性(參見,例如,EP242236,EP242246)(WO92 / 00377)(EP257993,US5013659)或轉基因作物植物(例如棉花)具有產生蘇雲金芽孢桿菌毒素(Bt毒素)的能力,其使植物對某些害蟲具有抗性(EP142924,EP193259)。
此外,本發明的化合物可用於處理來自植物的種子,所述植物與現有植物組成相比具有改變的特徵——其可(例如)通過傳統育種方法和/或突變體的或通過重組程式產生。例如,已經有許多案例描述了為了修飾植物中合成的澱粉而進行重組修飾的作物植物(例如WO92 / 11376,WO92 / 14827,WO91 / 19806)或具有改性脂肪酸組合物的轉基因作物植物(WO91 / 13972)。
本發明化合物處理種子的應用是通過在播種植物之前和植物出苗之前噴灑或撒粉種子來進行。
對種子處理特別有用的組合物有,例如:
A. 可溶性濃縮物 (SL, LS)
B. 乳劑 (EW, EO, ES)
C. 懸浮劑 (SC, OD, FS)
D. 水分散性顆粒和水溶性顆粒 (WG, SG)
E. 水分散性粉末和水溶性粉末 (WP, SP, WS)
F. 凝膠製劑 (GF)
G. 可撒粉的粉末 (DP, DS)
常規的種子處理製劑包括例如可流動的濃縮物FS、溶液LS、用於乾燥處理的粉末DS、用於漿料處理的水分散性粉末WS、水溶性粉末SS和乳劑ES和EC和凝膠製劑GF。這些製劑可以施用於稀釋或未稀釋的種子。對種子的施用是在播種前進行的,既可以直接施用在種子上,也可以在種子預催芽後施用。
在一個實施方案中,FS製劑用於種子處理。特別地,FS製劑可包含1-800g/l活性成分、1-200g/l表面活性劑、0-200g/l防凍劑、0-400g/l黏合劑、0-200g/l顏料和至多1升溶劑(優選水)。
特別地,用於種子處理的本發明化合物的FS製劑通常包含重量比為0.1至80%(1至800g / l)的活性成分,重量比為0.1至20%(1至200g / l)的至少一種表面活性劑,重量比為0.05至5%的濕潤劑和0.5至15%(至多20%)的分散劑,5至20%的防凍劑,重量比為從0 至15%(例如1至15%)的顏料和/或染料,重量比為0至40%(例如1至40%)的黏合劑(黏著劑/黏合劑),任選地重量比為至多 5%(例如0.1至5%)的增稠劑,任選地重量比為0.1至2%的消泡劑,和任選的防腐劑(例如殺生物劑,抗氧化劑等),例如重量比為0.01 至1%,加上填料/載體組成100%重量。
種子處理製劑可另外包含黏合劑和著色劑。
可以添加黏合劑以改善活性材料在處理後對種子的黏附。合適的黏合劑是來自亞烷基氧化物的均聚和共聚物,如環氧乙烷或環氧丙烷、聚乙酸乙烯酯、聚乙烯醇、聚乙烯吡咯烷酮及其共聚物、乙烯-乙酸乙烯酯共聚物、丙烯酸均聚和共聚物、聚乙烯胺、聚乙烯醯胺和聚乙烯嘧啶、多糖如纖維素、侵填體和澱粉、聚烯烴均聚和共聚物如烯烴/馬來酸酐共聚物、聚氨酯、聚酯、聚苯乙烯均聚物和共聚物。
任選地,著色劑也可包含在製劑中。用於種子處理製劑的合適的著色劑或染料有羅丹明B,C.I,顏料紅112,C.I,溶劑紅1,顏料藍15:4,顏料藍15:3,顏料藍15:2,顏料藍15:1,顏料藍80,顏料黃1,顏料黃13,顏料紅112,顏料紅48:2,顏料紅48:1,顏料紅57:1,顏料紅53:1,顏料橙43,顏料橙34,顏料橙5,顏料綠36,顏料綠7,顏料白6,顏料棕25,鹼性紫10,鹼性紫49,酸性紅51,酸性紅52,酸性紅14,酸性藍9,酸性黃23,鹼性紅10,鹼性紅108。
膠凝劑的例子有卡拉膠(Satiagel®)
在種子處理中,本發明化合物的施用率通常為每100kg種子0.1g至10kg,優選為每100kg種子1g至5kg,更優選為每100kg種子1g至1000g(尤其是每100kg種子1g至200g)。因此,本發明還提供了包含如本文所定義的式(I)化合物或I的農業上有用的鹽的種子。化合物I或其可農用鹽的量通常為每100kg種子0.1g至10kg,優選每100kg種子1g至5kg(尤其是每100kg種子1g至1000g)。對於特定作物如萵苣,施用率可以更高。動物健康
本發明還提供了包含至少一種本發明化合物的農業和/或獸醫用組合物。
本發明還進一步涉及化合物、N-氧化物或獸醫學上可接受的鹽或本發明組合物在用於製備治療或保護動物免受昆蟲和蟎蟲或寄生蟲侵擾或感染的藥物中的用途。
式(I)化合物、其N-氧化物和/或獸醫學上可接受的鹽特別適合用於對抗動物中的寄生蟲。
因此,本發明的一個目的是提供控制動物體內寄生蟲的新方法。本發明的另一個目的是提供更安全的動物殺蟲劑。本發明的另一個目的是提供可以比現有殺蟲劑更低劑量使用的動物殺蟲劑。本發明的另一個目的是提供用於動物的殺蟲劑,以提供對寄生蟲的長期殘留控制。
本發明還涉及含有殺寄生物有效量的至少一種式(I)化合物、N-氧化物或獸醫學上可接受的鹽和可接受的載體的組合物,用於對抗動物體內的寄生蟲。
本發明還提供了治療、控制、預防和保護動物免受寄生蟲感染和感染的方法,該方法包括口服、局部或腸胃外給予或施用殺寄生物有效量的本發明化合物或包含它的組合物。
本發明還提供了製備用於治療、控制、預防或保護動物免受寄生蟲侵擾或感染的組合物(該組合物包含殺寄生物有效量的本發明化合物或包含它的組合物)的方法。
化合物對農業害蟲的活性並不表明它們適合控制動物體內的內寄生蟲和體表上的外寄生蟲、在口服施用時需要低的非催吐劑量、與動物的代謝相容性、低毒性和安全操作。
令人驚奇的是,現已發現本發明化合物適用於對抗動物體內的內寄生蟲和體表上的外寄生蟲。
本發明化合物和含有該化合物的組合物適用於控制和預防對動物的侵擾和感染,這些動物包括溫血動物(包括人)和魚。它們適用於控制和預防對哺乳動物(如牛、羊、豬、駱駝、鹿、馬、豬、家禽、兔子、山羊、狗和貓、水牛、驢、小鹿和馴鹿)、毛皮動物(如水貂、栗鼠和浣熊、鳥類,如母雞、鵝、火雞和鴨子)以及魚類(如新鮮和鹹水魚、如鱒魚、鯉魚和鰻魚)的侵擾和感染。
本發明化合物和含有該化合物的組合物適用於控制和預防對家畜(例如狗或貓)的侵擾和感染。
對溫血動物和魚類侵擾的害蟲包括但不限於蝨子、咬虱、蜱、鼻蠅、綿羊蜱、叮咬蒼蠅、蠅蠅、蒼蠅、蠅蛆幼蟲、恙蟎、蚊蠅、蚊子和跳蚤。
本發明化合物和含有該化合物的組合物適用於系統性和/或非系統性控制外寄生蟲和/或體內寄生蟲。 他們可以有效抵抗所有或某些發展階段。
本發明化合物尤其可用於對抗外寄生蟲。
本發明化合物特別適用於對抗下列目和物種的寄生蟲:跳蚤(劍翅目),例如貓頭蚤、圓頭蝽螂、爪蟾、蝽螂、蟑螂,如德國小蠊、細紋小蠊、美洲大蠊、日本大蠊、褐大蠊等,美洲大蠊、澳洲大蠊、東方蠊、蒼蠅、蚊子(雙翅目),例如埃及伊蚊、白紋伊蚊、伊蚊、墨西哥按實蠅、五斑按蚊、鯽魚按蚊、甘比亞按蚊、泛生按蚊、白踝瘧蚊、微小按蚊、四斑、紅頭麗蠅、大頭金蠅、腐敗錐蠅、中室斑虻、靜斑虻、大西洋斑虻、嗜人錐蠅、人皮蠅、毛庫蠓、黑須庫蚊、致倦庫蚊、環跗庫蚊、卡奇穀病毒之傳播媒介、黑尾賽蚊、人膚皮蠅、夏廁蠅、腸胃蠅、刺舌蠅、須舌蠅、擬寄舌蠅、西方角蠅、潛蠅屬、紋皮蠅、銅綠蠅、絲光綠蠅、曼蚊屬、家蠅、廄腐蠅、羊狂蠅、足白蛉、哥倫比亞鱗蚊、鱗蚊屬、原蚋屬、赤尾麻蠅、麻蠅屬、帶蚋、廄螫蠅、牛虻、北美黑虻、馬蠅、和虻屬、蝨子(虱毛目),例如人頭虱、人體虱、人體陰虱、牛血風、豬血虱、牛顎虱、牛羽虱、雞羽虱、和水牛盲虱。扁虱和寄生蟎蟲(寄蟎目):扁虱(真蜱目),例如肩突硬蜱、全環硬蜱、太平洋硬蜱、安氏革蜱、變異革蜱、美洲花蜱、斑點鈍口螈、鈍緣蜱、和寄生蟎蟲(中氣門亞目),例如柏氏禽刺蟎和雞皮刺蟎、輻蟎、粉蟎亞目、例如蜂盾蟎屬、姬螯蟎屬、肉蟎屬、瘡蟎屬、蠕形蟎屬、恙蟎屬、持鏟屬、粉蟎屬、食酪蟎屬、嗜木蟎屬、皮蟎科翼蟎屬、癢蟎屬、足蟎屬、耳蟎屬、疥蟎屬、癡蟎屬、膝蟎屬、和臭蟲 (異翅目):溫帶臭蟲、熱帶臭蟲、獵蝽屬、錐獵蝽屬、長紅獵蝽、攀錐蝽屬和輪背獵蝽、虱目,例如獸虱科、毛虱屬、人體虱屬、和管虱屬、食毛目(細角亞目),例如毛鳥虱科、短羽虱屬、鴨虱屬、牛羽虱屬、韋尼克菌屬、齧毛虱屬和貓羽虱屬。線形線蟲:
鐵線蟲和毛線蟲病(毛管目)、例如毛線蟲科(毛形屬)、鞭蟲屬、毛細線蟲屬、小杆亞綱、例如小杆線蟲屬、類圓線蟲屬、厚蟹屬、圓線蟲目、例如圓線蟲屬、鉤蟲屬、美洲鉤蟲、仰口線蟲屬(十二指腸蟲)、撚轉血矛線蟲、奧斯特屬、古柏屬、細頸線蟲屬、網尾線蟲屬、杯口屬、結節線蟲屬、有齒冠尾線蟲、盤頭線蟲屬、夏柏特線蟲屬、有齒冠尾線蟲、氣管比翼線蟲、鉤蟲屬、彎口屬、球首屬、板口線蟲屬、後圓線蟲屬、貓圓線蟲、和腎膨結線蟲、腸蛔蟲(蛔蟲科),例如人蛔蟲、豬蛔蟲、雞蛔蟲、馬副蛔蟲、蠕形住腸蟯蟲(蟯蟲)、犬弓首蛔蟲、獅弓蛔蟲、斯氏蟲屬、和馬蟯蟲、駝形目、例如麥地那龍線蟲、旋尾目、例如吸吮線蟲屬、吳策線蟲屬、布魯格絲蟲屬、盤尾屬、惡絲蟲屬、棘唇線蟲屬、腹腔絲蟲屬、絲絨蟲屬、狼尾旋線蟲、和麗線蟲屬、多刺有頭蠕蟲(棘頭綱),例如棘頭蟲屬、豬巨吻棘頭蟲和鉤棘頭蟲屬、渦蟲(扁形動物門);吸蟲(吸蟲綱),例如條華蝸牛、大擬片形吸蟲、並殖吸蟲屬、雙腔吸蟲屬、布氏薑片蟲、華支睾吸蟲、血吸蟲屬、毛畢屬吸蟲、有翼翼形吸蟲、並殖吸蟲屬、和角蟾目,尤其是多節絛蟲亞綱(絛蟲類),例如裂頭屬、條蟲屬、棘球屬、犬複孔絛蟲、多頭絛蟲屬、膜殼絛蟲屬、中帶絛蟲屬、吸漿蟲屬、莫尼茨屬、裸頭絛蟲屬。
式(I)化合物和含有它們的組合物特別適用於控制雙翅目、蚤目和真蜱目的害蟲。
在一個實施方案中,本發明提供用式(I)化合物及其組合物對抗蚊子的用途。
在一個實施方案中,本發明提供用式(I)化合物及其組合物對抗蠅的用途。
在一個實施方案中,本發明提供用式(I)化合物及其組合物對抗跳蚤的用途。
本發明化合物及其組合物用於對抗扁虱的用途是本發明的另一個實施方案。
本發明的化合物還特別適用於對抗體內寄生蟲(線形線蟲、多刺有頭蠕蟲和渦蟲)。
在一個實施方案中,本發明化合物的給藥可以預防性和治療性進行。
在一個實施方案中,本發明化合物的給藥可以直接或以合適製劑的形式口服、局部/皮膚或腸胃外給藥進行。
對於溫血動物的口服給藥,本發明化合物可配製成動物飼料、動物飼料預混物、動物飼料濃縮物、丸劑、溶液、糊劑、懸浮液、浸液、凝膠、片劑、大丸劑和膠囊。此外,本發明化合物可以在其飲用水中給予動物。對於口服給藥,所選擇的劑量應為動物提供每天0.01mg / kg至100mg / kg ×動物體重的本發明化合物,優選每天0.5mg / kg至100mg / kg ×動物體重。
或者,本發明化合物可以胃腸外給予動物,例如通過腔內、肌肉內、靜脈內或皮下注射。本發明化合物可以分散或溶解在生理學上可接受的載體中用於皮下注射。或者,可以將本發明化合物配製成用於皮下給藥的植入物。此外,本發明化合物可以透皮給藥於動物。對於腸胃外給藥,所選擇的劑量應為動物提供每天0.01mg / kg至100mg / kg ×動物體重的本發明化合物。
本發明的化合物還可以以浸漬劑、粉劑、粉劑、衣領、獎章劑、噴霧劑、洗發劑、點滴劑和澆潑劑和軟膏劑或水包油劑的形式局部施用於動物。對於局部施用,浸漬和噴霧通常含有0.5ppm至5,000ppm,優選1ppm至3,000ppm的本發明化合物。此外,本發明的化合物可以配製成動物(特別地四足動物如牛和綿羊)的耳標。
合適的製劑有:溶液,例如口服溶液、稀釋後用於口服給藥的濃縮物、用於皮膚或體腔的溶液,澆注製劑、凝膠、用於口服或皮膚給藥的乳液和懸浮液、半固體製劑、活性化合物在軟膏基質或油包水或油包水乳劑基質中加工的製劑、固體製劑(如粉末、預混料或濃縮物、顆粒、小丸、片劑、大丸劑、膠囊、 氣溶膠和吸入劑、含活性化合物的成型製品)。
適於注射的組合物通過將活性成分溶解在合適的溶劑中並任選地加入其他成分如酸、鹼、緩衝鹽、防腐劑和增溶劑來製備。
溶劑過濾和殺菌。
合適的溶劑有生理上可耐受的溶劑(例如水)、鏈烷醇(例如乙醇、丁醇、苯甲醇、甘油、丙二醇、聚乙二醇、N-甲基吡咯烷酮、2-吡咯烷酮及其混合物)。
活性化合物可任選地溶於適於注射的生理學上可耐受的植物油或合成油中。
合適的增溶劑是促進活性化合物在主要溶劑中溶解或防止其沉澱的溶劑。例如聚乙烯吡咯烷酮、聚乙烯醇、聚氧乙烯化蓖麻油和聚氧乙烯化脫水山梨糖醇酯。
合適的防腐劑有苯甲醇、三氯丁醇、對羥基苯甲酸酯和正丁醇。
口服溶液直接給藥。在預先稀釋至使用濃度後,將濃縮物口服給藥。口服溶液和濃縮物根據現有技術和如上製備注射溶液的方法製備,不需要無菌操作。
用於皮膚方法是將溶液滴上、塗抹、揉搓、灑上或噴上。
用於皮膚的溶液根據現有技術和根據如上製備注射溶液的方法製備,不需要無菌操作。
其他合適的溶劑有聚丙二醇,苯乙醇,苯氧基乙醇,酯如乙酸乙酯或乙酸丁酯,苯甲酸苯甲酯,醚類如烷基乙二醇基醚,如二丙二醇單甲醚,酮類如丙酮,甲乙酮等,芳烴,植物和合成油,二甲基甲醯胺,二甲基乙醯胺,還氧二元醇,丙酮縮甘油,碳酸丙烯酯,及其混合物。
在製備過程中加入增稠劑可能有好處。合適的增稠劑有無機增稠劑(例如膨潤土,膠體矽酸,單硬脂酸鋁)、有機增稠劑(如纖維素衍生物、聚乙烯醇及其共聚物、丙烯酸酯和甲基丙烯酸酯)。
凝膠應用於皮膚或塗抹在皮膚上或引入體腔。凝膠是通過在根據製備注射溶液的方法製備的溶液中增加足夠的增稠劑從而產生具有軟膏狀稠度的透明材料來製備。使用的增稠劑是上面列出的增稠劑。
將澆潑製劑傾倒或噴灑到皮膚的有限區域上,活性化合物滲透皮膚並作用到全身。通過在合適的皮膚相容性溶劑或溶劑混合物中將活性化合物溶解、懸浮或乳化來製備澆潑製劑。如果合適,可以加入其他助劑如著色劑、生物吸收促進物質、抗氧化劑、光穩定劑、黏合劑。
合適的溶劑有:水、鏈烷醇、二醇、聚乙二醇、聚丙二醇、甘油、芳基醇如苯甲醇、苯基乙醇、苯氧基乙醇、酯類如乙酸乙酯、乙酸丁酯、苯甲酸苯甲酯、諸如亞烷基二醇醚、二乙二醇單丁醚、丙酮、甲基乙基酮等酮類、碳酸亞丙酯等環狀碳酸酯、芳香族和/或脂肪族烴等亞烷基乙二醇醚等醚類、植物油或合成油、DMF、二甲基乙醯胺、n-烷基吡咯烷酮、如甲基吡咯烷酮、正丁基吡咯烷酮或N-辛基吡咯烷酮、N-甲基吡咯烷酮、2-吡咯烷酮、2,2-二甲基-4-氧-亞甲基-1,3-二氧戊環 和甘油縮甲醛。
合適的著色劑是允許在動物上使用並且可以溶解或懸浮的所有著色劑。
合適的吸收促進物質有:二甲基亞碸、塗布油、如肉豆蔻酸異丙酯、二丙二醇壬酸酯、矽油及其與聚醚的共聚物、脂肪酸酯、甘油三酯、脂肪醇等。
合適的抗氧化劑有亞硫酸鹽或偏亞硫酸氫鹽,例如偏亞硫酸氫鉀、抗壞血酸、丁基羥基甲苯、丁基羥基苯甲醚、生育酚等。
合適的光穩定劑有正-鄰二酸等。合適的黏合劑有,纖維素衍生物、澱粉衍生物、聚丙烯酸酯、天然聚合物如藻酸鹽、明膠等。乳劑可以口服、皮膚或注射給藥。乳液可以是油包水型或水包油型。
它們是通過將活性化合物溶解在疏水相或親水相中,並借助合適的乳化劑和適當的其他助劑(如著色劑、促進吸收物質、防腐劑、抗氧化劑、光穩定劑、增黏物質)將其與另一相的溶劑均化而製備的。合適的疏水相(油)有:
液體石蠟、矽油、天然植物油、如芝麻油、杏仁油、蓖麻油、合成甘油三酸酯、如辛酸/癸酸甘油三酯、甘油三酯混合物、鏈長為C1
-C12
的植物脂肪酸或其他特別選擇的天然脂肪酸、飽和或不飽和脂肪酸的偏甘油酯混合物、可能還含有羥基、Cs-do脂肪酸的單甘油酯和甘油二酯、脂肪酸酯如硬脂酸乙酯、己二酸二正丁酯、月桂酸己酯、二丙二醇壬酸酯、酯鏈長為C16
-C18
的飽和脂肪醇、肉豆蔻酸異丙酯、棕櫚酸異丙酯、鏈長為C12
-C18
的飽和脂肪醇的辛酸/癸酸酯、硬脂酸異丙酯、油酸油酯、油酸癸酯的中鏈長支鏈脂肪酸、油酸乙酯、乳酸乙酯、蠟狀脂肪酸酯、如合成鴨尾骨腺脂肪和脂肪、鄰苯二甲酸二丁酯、己二酸二異丙酯、以及與後者有關的酯混合物、脂肪醇如異十三烷醇、2-辛基十二烷醇、十六烷基硬脂醇、油醇、和脂肪酸如油酸及其混合物。合適的親水相是:水、醇如丙二醇、甘油、山梨糖醇及其混合物。
合適的乳化劑有非離子表面活性劑,例如聚乙氧基化蓖麻油、聚乙氧基化脫水山梨糖醇單油酸酯、脫水山梨糖醇單硬脂酸酯、甘油單硬脂酸酯、聚氧乙烯硬脂酸酯、或烷基酚聚乙二醇醚;兩性表面活性劑,例如N-月桂基-對-亞氨基二丙酸二鈉或卵磷脂。
合適的陰離子表面活性劑有十二烷基硫酸鈉、脂肪醇醚硫酸鹽、單/二烷基聚乙二醇醚正磷酸酯單乙醇胺鹽;合適的陽離子活性表面活性劑是十六烷基三甲基氯化銨等。
合適的其他助劑是增強黏度和穩定乳液的物質,如羧甲基纖維素、甲基纖維素和其他纖維素和澱粉衍生物、聚丙烯酸酯、藻酸鹽、明膠、阿拉伯樹膠、聚乙烯吡咯烷酮、聚乙烯醇、甲基乙烯基醚和馬來酸酐的共聚物、聚乙二醇、蠟、膠體矽酸或這些物質的混合物。
懸浮液可以口服或局部/皮膚給藥。它們通過將活性化合物懸浮在懸浮劑中來製備,如果合適的話還加入其他助劑如潤濕劑、著色劑、生物吸收促進物質、防腐劑、抗氧化劑、光穩定劑。
液體懸浮劑均為均相溶劑和溶劑混合物。
合適的潤濕劑(分散劑)是上文列舉的乳化劑。
上文還給出了可能提及的其他助劑。
半固體製劑可以口服或局部/皮膚給藥。它們與上述懸浮液和乳液的不同之處僅在於其黏度較高。
固體製劑的製備是將活性化合物與合適的賦形劑混合(如果合適的話加入助劑),然後製成所需的形式。
合適的賦形劑是所有生理上可耐受的固體惰性物質,包括無機和有機的物質。無機物質有氯化鈉、碳酸鹽如碳酸鈣、碳酸氫鹽、氧化鋁、氧化鈦、矽酸、泥質土、沉澱或膠體二氧化矽或磷酸鹽等。有機物質有糖、纖維素、食品和嬰兒食品(例如奶粉、動物粉、穀物粉和碎片、澱粉)等。
合適的助劑是上面提到的防腐劑、抗氧化劑、和/或著色劑。
其他合適的助劑是潤滑劑和助流劑,如硬脂酸鎂、硬脂酸、滑石粉、膨潤土、崩解促進物質如澱粉或交聯聚乙烯吡咯烷酮、黏合劑如澱粉、明膠或線性聚乙烯吡咯烷酮、和乾黏合劑如微晶纖維素。
一般而言,“殺寄生物有效量”是指實現對生長的可觀察效果(包括壞死、死亡、阻滯、預防、去除、破壞或以其他方式減少目標生物體的發生和活動的效果)所需的活性成分的量。殺寄生物有效量可以根據本發明中使用的各種化合物/組合物而變化。殺寄生物有效量的組合物也將根據主要條件而變化,例如所需的寄生蟲效應和持續時間、目標物種、施用方式等。可用於本發明的組合物通常含有約0.001-95%的本發明化合物。
通常,以每天0.5mg / kg至100mg / kg,優選每天1mg / kg至50mg / kg的總量施用本發明的化合物是有利的。即用製劑含有對寄生蟲(優選外寄生蟲)起作用的化合物,其濃度範圍為10ppm至總重量的80%,優選占總重量的0.1至65%,更優選占總重量的1至50%,最優選占總重量的5-40%。製劑在使用前稀釋,含有對外寄生蟲起作用的化合物,其濃度為占重量的0.5-90%,優選占重量的1-50%。此外,對抗體內寄生蟲的本發明化合物製劑的濃度範圍為從10ppm至占總重量2%,優選占總重量0.05至0.9%,非常特別優選占總重量0.005至0.25%。
在一個實施方案中,包含本發明化合物的組合物經皮/局部施用。
在另一個實施方案中,局部施用以含有化合物的成形製品的形式進行,例如固定在身體部位的頸圈、佩戴章、耳標、繃帶以及黏合的細條和薄片。
通常按一個週期(三周)10mg / kg至300mg / kg,優選20mg / kg至200mg / kg,最優選25mg / kg至160mg / kg的施用量施用本發明化合物的固體製劑是有利的。
使用熱塑性塑膠和柔性塑膠以及彈性體和熱塑性彈性體製備成型製品。 合適的塑膠和彈性體是聚乙烯樹脂、聚氨酯、聚丙烯酸酯、環氧樹脂、纖維素、纖維素衍生物、聚醯胺和聚酯,它們與本發明的化合物充分相容。如WO2003 / 086075中給出了塑膠和彈性體的詳細列表以及成型製品的製備方法。作物正反應:
本發明的化合物不僅有效地控制昆蟲和蟎害蟲,而且還顯示出積極的作物反應,例如植物生長增強效果,如增強的根生長,增強的耐旱性、高鹽、高溫、寒冷、冰霜或光輻射、改善開花、提高養分利用率(例如改善的氮同化作用)、提高植物產品品質、增加分蘖數、增加對真菌、昆蟲、害蟲等的抵抗力,從而提高產量。化學實例:
下列實施例闡述了製備本發明化合物的方式和方法,並且包括發明人設想的實施本發明的最佳方式,但不對本發明施加任何限制。
例
1
:
4-
(
5-
(
3,5-
二氯苯基)
-5-
(三氟甲基)
-4,5-
二氫異惡唑
-3-
基)
-2-
甲基
-N-
(氧二苯基
-6-6-
亞磺叉基)苯甲醯胺(化合物
87
號)的合成:
第
1
步:
4-(3-(3,5-
二氯苯基
)-4,4,4-
三氟
-3-
羥基丁醯基
)-2-
苯甲酸甲酯三乙銨鹽的合成:
向4-乙醯基-2-甲基苯甲酸(15 g,84 mmol)和1-(3,5-二氯苯基)-2,2,2-三氟乙烷-1-酮(24.55 g, 101 mmol)混合物的甲苯(110mL)溶液中加入三乙胺(17.5mL,126 mmol)。 將所得反應混合物在50℃下加熱16小時。然後將甲苯(15mL)加入到漿態反應混合物中,然後將其冷卻至25℃。反應完成後,將反應混合物減壓過濾,並將所得固體用甲苯(20mL)洗滌兩次,分離出產物4-(3-(3,5-二氯苯基)-4,4,4-三氟-3-羥基丁醯基)-2-甲基苯甲酸 (35 g, 84 mmol, 80%產率)。1
H-NMR (400 MHz, CHLOROFORM-D) δ 7.66-7.68 (m, 3H), 7.48 (s, 2H), 7.31 (t, J = 1.8 Hz, 1H), 6.07 (s, 1H), 3.84 (d, J = 17.6 Hz, 1H), 3.62 (d, J = 17.6 Hz, 1H), 3.12 (q, J = 7.3 Hz, 6H), 2.55 (s, 3H), 1.33 (t, J = 7.3 Hz, 9H); ESI MS (m/z) 418.90 (M)-
。
第
2
步:
4-(3-(3,5-
二氯苯基
)-4,4,4-
三氟丁基
-2-
烯醯
)-2-
甲基苯甲酸的合成:
向4-(3-(3,5-二氯苯基)-4,4,4-三氟-3-羥基丁醯基)-2-苯甲酸甲酯 (32 g, 61.3 mmol)和4-二甲基氨基吡啶 (7.48 g, 61.3 mmol)的三乙銨鹽混合物中加入乙酸酐(11.58 mL,123 mmol)。將所得反應混合物在60℃加熱9小時。將反應混合物冷卻至25℃,並加入甲苯(40mL)、水(40mL)和濃鹽酸(4.0mL)。分離混合的有機層,並用水(40mL)洗滌兩次。將混合的有機層在減壓下濃縮,得到殘餘物,將其通過矽膠柱色譜法(使用30%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到4-(3-(3,5-二氯苯基)-4,4,4-三氟丁基-2-烯醯)-2-甲基苯甲酸 (19 g, 47.1 mmol, 77%產率)。所需產物為幾何異構體的混合物,將其通過1
H-NMR分析。1
H-NMR (400 MHz, DMSO-d6
; major isomer) δ 13.27 (s,1H), 7.85-7.87 (m, 2H), 7.75-7.79 (m, 2H), 7.67 (t, J = 2.0 Hz, 1H), 7.36 (d, J = 1.7 Hz, 2H), 2.54 (s, 3H); ESI MS (m/z) 400.90 (M-H;35
Cl)-
, 402.90 (M-H;37
Cl)-
。
第
3
步:
4-(5-(3, 5-
二氯苯基
)-5-(
三氟甲基
)-4,5-
二氫異惡唑
-3-
基)苯甲酸的合成:
向4-(3-(3,5-二氯苯基)-4,4,4-三氟丁基-2-烯醯)-2-甲基苯甲酸 (20 g, 49.6 mmol)的甲苯(140mL)溶液中加入溴化四丁基銨(4.80g,14.88mmol),並將得到的反應混合物冷卻至0℃。通過將氫氧化鈉(4.36g,109mmol)分別攪拌到水(50mL)和50%的羥胺水溶液(5.96mL,99mmol)製備的溶液,然後將溶液滴加到上述反應混合物中。反應完成後,將8.8%的鹽酸水溶液(104mL,298mmol)和乙酸乙酯(100mL)加入到反應混合物中,然後分離有機層。將水層再次用乙酸乙酯(50mL)萃取兩次。混合的乙酸乙酯層用無水硫酸鈉乾燥,並減壓濃縮,得到粗產物4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲酸(16.44 g,39.3 mmol,79%產率),其無需純化即可用於進一步反應。1
H-NMR (400 MHz, DMSO-d6
) δ 13.02 (s, 1H), 7.88 (d, J = 8.6 Hz, 1H), 7.78 (t, J = 1.8 Hz, 1H), 7.61-7.64 (m, 4H), 4.39 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.3 Hz, 1H), 2.54 (s, 3H); ESI MS (m/z) 417.75 (MH;35
Cl)+
, 419.75 (MH;37
Cl)+
。
第
4
步:
4-(5-(3,5-
二氯苯基
)-5-(
三氟甲基
)-4,5-
二氫異惡唑
-3-
基)
-2-
甲基
-N-(
氧二苯基
- 6
-
亞磺醯基
)
苯甲醯胺的合成:
在5-10℃下在氮氣環境中向4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲酸 (200 mg, 0.48 mmol)的二氯甲烷(2 mL)溶液中加入1-(3-二甲基氨基丙基)-3-乙基碳二亞胺鹽酸鹽(183 mg,0.96 mmol)和4-二甲基氨基吡啶 (175 mg, 1.44 mmol),然後向反應混合物加入亞氨基二苯基- 6
-磺胺酮(125mg,0.57mmol),將反應混合物在25℃下攪拌8小時。 反應完成後,將反應混合物用二氯甲烷(25mL)稀釋,並用水(30mL)洗滌三次,將二氯甲烷層用硫酸鈉乾燥並減壓濃縮,得到殘餘物,將其通過矽膠柱色譜法(使用30%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(氧二苯基- 6
-亞磺醯基)苯甲醯胺 (80 mg, 0.130 mmol, 27 % 產率)。1
H-NMR (400 MHz, CHLOROFORM-D) δ 8.21 (d, J = 8.1 Hz, 1H), 8.04-8.06 (m, 4H), 7.52-7.62 (m, 9H), 7.48 (s, 1H), 7.43 (t, J = 1.8 Hz, 1H), 4.10 (d, J = 17.4 Hz, 1H), 3.72 (d, J = 17.4 Hz, 1H), 2.63 (s, 3H); ESI MS (m/z) 617.10 (MH)+
。
例
2
:
((4-(5-(3,5-
二氯苯基
)-5-(
三氟甲基
)-4,5-
二氫異惡唑
-3-
基)
-2-
甲基苄基
)
氨基
)(
甲基
)(
苯基
)- 6
-
磺胺酮
(162)
的合成:
第
1
步:
(4-(5-(3,5-
二氯苯基
)-5-(
三氟甲基
)-4,5-
二氫異惡唑
-3-
基)
-2-
甲基苯基
)
甲醇的合成:
在0°C下向4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲酸 (4 g, 9.56 mmol) 的四氫呋喃(28.6 mL)冰冷卻溶液中加入硼烷-四氫呋喃絡合物(24.87 mL,24.87 mmol)。將所得反應混合物在0°C攪拌2 小時,然後加熱到25℃並進一步攪拌16小時,反應完成後,將反應混合物在0℃下用水(20mL)稀釋,並用乙酸乙酯(25mL)萃取三次,混合的乙酸乙酯層用飽和碳酸氫鈉水溶液(30 mL)洗滌。有機層用硫酸鈉乾燥,減壓濃縮,得到殘留物,將其通過矽膠柱色譜法(使用40%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到(4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)甲醇 (2.5 g, 6.18 mmol, 65%產率)。1
H-NMR (400 MHz, CHLOROFORM-D) δ 7.49-7.52 (m, 3H), 7.47 (d, J = 1.5 Hz, 2H), 7.42 (t, J = 1.8 Hz, 1H), 4.74 (s, 2H), 4.08 (d, J = 17.2 Hz, 1H), 3.69 (dd, J = 17.2, 0.6 Hz, 1H), 2.35 (s, 3H), 1.63 (s, 1H); ESI MS (m/z) 401.95 (M-H;35
Cl)-
, 403.95 (M-H;37
Cl)-
。
第
2
步:
3-(4-(
溴甲基
)-3-
甲基苯基
)-5-(3,5-
二氯苯基
)-5-(
三氟甲基
)-4,5-
二氫異惡唑的合成:
在0°C下向(4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)甲醇(5.4 g, 13.36 mmol)和四溴甲烷(5.32 g,16.03 mmol)的二氯甲烷(80 mL)溶液中加入三苯基膦(4.91 g,18.70 mmol)。將反應混合物在25℃下攪拌12小時,反應完成後,將反應混合物用二氯甲烷(40mL)稀釋並用水(50mL)洗滌兩次,將二氯甲烷層用無水硫酸鈉乾燥並在減壓下濃縮,得到殘留物,將其通過矽膠柱色譜法(用10%乙酸乙酯的己烷溶液為洗脫劑)純化,得到3-(4-(溴甲基)-3-甲基苯基)-5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑(4.2 g, 8.99 mmol, 67%產率)。1
H-NMR (400 MHz, CHLOROFORM-D) δ 7.51 (d, J = 1.2 Hz, 3H), 7.46 (dd, J = 7.8, 1.5 Hz, 1H), 7.42 (t, J = 1.8 Hz, 1H), 7.37 (d, J = 7.8 Hz, 1H), 4.50 (s, 2H), 4.07 (d, J = 17.1 Hz, 1H), 3.68 (d, J = 17.4 Hz, 1H), 2.44 (s, 3H); ESI MS (m/z) 467.85 (MH)+
。
第
3
步:
((4-(5-(3,5-
二氯苯基
)-5-(
三氟甲基
)-4,5-
二氫異惡唑
-3-
基)
-2-
甲基苄基
)
氨基
)(
甲基
)(
苯基
)- 6
-
磺胺酮的合成:
在25o
C下在氬氣環境中向氨基(甲基)(苯基)- 6
-磺胺酮 (91 mg, 0.59 mmol)的無水N,N-二甲基甲醯胺(3 mL)溶液中加入氫化鈉(23.55 mg,0.59 mmol;60%的礦物油溶液)。向反應混合物中加入3-(4-(溴甲基)-3-甲基苯基)-5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑 (250 mg, 0.54 mmol)的二氯甲烷(2mL)溶液,並在25℃下攪拌3小時。反應完成後,將反應混合物用氯化銨水溶液(5mL)小心地淬滅,然後用二氯甲烷(20mL)萃取三次。混合的二氯甲烷層用水(20mL)洗滌,然後用無水硫酸鈉乾燥,減壓濃縮,得到殘餘物,將其通過矽膠柱色譜法(使用20%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)(苯基)- 6
-磺胺酮(140 mg, 0.26 mmol, 48%產率)。1
H-NMR (400 MHz, CHLOROFORM-D) δ 7.92 (d, J = 7.1 Hz, 2H), 7.63 (t, J = 7.3 Hz, 1H), 7.54-7.59 (m, 3H), 7.52 (d, J = 1.7 Hz, 2H), 7.41-7.44 (m, 3H), 4.18 (d, J = 15.2 Hz, 1H), 4.06 (dd, J = 17.1, 1.5 Hz, 1H), 3.96 (d, J = 15.4 Hz, 1H), 3.67 (d, J = 17.1 Hz, 1H), 3.19 (s, 3H), 2.27 (s, 3H); ESI MS (m/z) 541.05 (MH;35
Cl)+
, 543.05 (MH;37
Cl)+
。
例 3 : ((4-(5-(3,5- 二氯苯基 )-5-( 三氟甲基 )-4,5- 二氫異惡唑 -3- 基) -2- 甲基苯基 ) 氨基 ) 二甲基 -
6 - 磺胺酮 ( 化合物 2 號 ) :
第 1 步 : ((4- 乙醯基 -2- 甲基苯基 ) 氨基 ) 二甲基 -
6 - 磺胺酮的合成 :
向三(二苄叉丙酮)二鈀(0)[Pd2
(dba)3
] (0.064 g, 0.070 mmol)和X-phos(0.067 g,0.141 mmol)的甲苯(10 mL)溶液中加入1-(4-溴-3-甲基苯基)乙烷-1-酮(0.30 g,1.408 mmol)的甲苯(5 mL)溶液,然後加入氨基二甲基- 6
-磺胺酮 (0.144 g, 1.54 mmol)和碳酸銫(1.376g,4.22mmol)。將所得反應混合物在90℃下加熱3小時。反應完成後,將反應混合物用乙酸乙酯(20mL)稀釋,通過矽藻土床過濾,並將濾液蒸發至幹,得到粗產物。將得到的粗產物通過矽膠柱色譜法(使用20%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到((4-乙醯基-2-甲基苯基)氨基)二甲基- 6
-磺胺酮 (0.287 g, 1.273 mmol, 90%產率)。M/Z=[M+1]: 226.00;1
H-NMR (400 MHz, CHLOROFORM-D) δ 7.78 (d, J = 1.7 Hz, 1H), 7.67-7.70 (m, 1H), 7.22 (d, J = 8.3 Hz, 1H), 3.21 (s, 6H), 2.54 (s, 3H), 2.25 (s, 3H)。
以下表1列出的化合物可通過上文所述的步驟製備。表 1 :
| 序號 | 化學名 | 分析資料 | 產率 |
| 1-a | ((4-乙醯基-2-甲基苯基)氨基)二甲基- 6 -磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.78 (d, J = 1.7 Hz, 1H), 7.67-7.70 (m, 1H), 7.22 (d, J = 8.3 Hz, 1H), 3.21 (s, 6H), 2.54 (s, 3H), 2.25 (s, 3H); M/Z=[M+1]: 226.00 | 99% |
| 2-a | ((4-乙醯基-2-甲基苯基)氨基)(3-氟苯基)(甲基)- 6 -磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.76 (d, J = 1.7 Hz, 1H), 7.72 (dt, J = 7.8, 1.3 Hz, 1H), 7.65 (dt, J = 7.7, 2.0 Hz, 1H), 7.51-7.56 (m, 2H), 7.30-7.34 (m, 1H), 6.97 (d, J = 8.3 Hz, 1H), 3.30 (s, 3H), 2.48 (s, 3H), 2.38 (s, 3H) | 93% |
| 3-a | ((4-乙醯基-2-甲基苯基)氨基)(3,5-二甲基苯基)(甲基)- 6 -磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.76 (d, J = 1.5 Hz, 1H), 7.51-7.53 (m, 3H), 7.22 (d, J = 0.7 Hz, 1H), 6.99 (d, J = 8.3 Hz, 1H), 3.22-3.25 (m, 3H), 2.48 (s, 3H), 2.37-2.39 (m, 9H); M/Z=[M+1]: 316.15 | 85% |
| 4-a | ((4-乙醯基-2-甲基苯基)氨基)(環己基)(甲基)- 6 -磺胺酮 | M/Z=[M+1]: 294.15 | 68% |
| 5-a | ((4-乙醯基-2-甲基苯基)氨基)(甲基)(苯基)- 6 -磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.93-7.95 (m, 2H), 7.76 (d, J = 1.7 Hz, 1H), 7.60-7.64 (m, 1H), 7.55-7.57 (m, 2H), 7.49-7.53 (m, 1H), 6.98 (d, J = 8.3 Hz, 1H), 3.28 (s, 3H), 2.48 (s, 3H), 2.39 (s, 3H); M/Z= 287.1 | 90% |
| 6-a | ((4-乙醯基-2-甲基苯基)氨基)(4-甲氧基苯基)(甲基)- 6 -磺胺酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.83 (d, J = 9.0 Hz, 2H), 7.67 (s, 1H), 7.51-7.43 (1H), 7.13 (d, J = 9.0 Hz, 2H), 6.84 (d, J = 8.3 Hz, 1H), 3.81 (s, 3H), 3.41 (s, 3H), 2.40 (s, 3H), 2.30 (s, 3H); M/Z=[M+1]: 317.65 | 94% |
| 7-a | ((4-乙醯基-2-甲基苯基)氨基)(2,6-二甲基苯基)(甲基)- 6 -磺胺酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.70 (d, J = 1.8 Hz, 1H), 7.44 (dd, J = 8.3, 2.1 Hz, 1H), 7.38 (t, J = 7.6 Hz, 1H), 7.23 (d, J = 7.9 Hz, 2H), 6.65 (d, J = 8.6 Hz, 1H), 3.49 (s, 3H), 2.60 (s, 6H), 2.40 (s, 3H), 2.26 (s, 3H); M/Z=[M+1]: 316.10 | 95% |
| 8-a | 1-(3-甲基-4-((1-氧化四氫-2H-1 6 -噻喃-1-基亞基)氨基)苯基)乙烷-1-酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.69-7.72 (m, 1H), 7.63 (dd, J = 8.3, 2.2 Hz, 1H), 7.11 (d, J = 8.3 Hz, 1H), 3.41-3.55 (m, 2H), 3.36-26 (m, 2H), 2.45 (s, 3H), 2.23 (s, 3H), 1.92-1.98 (m, 2H), 1.75-1.85 (m, 2H), 1.63-1.68 (m, 1H), 1.48-1.59 (m, 1H); M/Z=[M+1]: 265.61 | 80% |
| 9-a | ((4-乙醯基-2-甲基苯基)氨基)(2-氯代-6-甲基苯基)(甲基)- 6 -磺胺酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.68 (s, 1H), 7.42-7.48 (m, 4H), 6.69 (d, J = 8.3 Hz, 1H), 3.65 (s, 3H), 2.75 (s, 3H), 2.39 (s, 3H), 2.27 (s, 3H); M/Z=[M+1]: 336.10 | 99% |
| 10-a | ((4-乙醯基-2-甲基苯基)氨基)(2-甲氧基苯基)(甲基)- 6 -磺胺酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.92 (dd, J = 7.8, 1.7 Hz, 1H), 7.60-7.64 (m, 2H), 7.44 (dd, J = 8.3, 2.0 Hz, 1H), 7.20 (d, J = 7.6 Hz, 1H), 7.12-7.16 (m, 1H), 6.85 (d, J = 8.3 Hz, 1H), 3.86 (s, 3H), 3.49 (s, 3H), 2.38 (s, 3H), 2.21 (s, 3H) | 94% |
| 11-a | ((4-乙醯基-2-甲基苯基)氨基)二苯基- 6 -磺胺酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.00-8.06 (m, 4H), 7.76 (d, J = 1.5 Hz, 1H), 7.58-7.67 (m, 6H), 7.51 (dd, J = 8.3, 2.2 Hz, 1H), 6.92-6.95 (m, 1H), 2.50 (s, 3H), 2.41 (s, 3H) | 85% |
第
2
步:
((4-(3-(3,5-
二氯苯基
)-4,4,4-
三氟丁基
-2-
烯醯
)-2-
甲基苯基
)
氨基
)
二甲基
- 6
-
磺胺酮的合成:
在25℃下向1-(3,5-二氯苯基)-2,2,2-三氟乙烷-1-酮 (0.259 g, 1.065 mmol)和((4-乙醯基-2-甲基苯基)氨基)二甲基- 6
-磺胺酮 (0.259 g, 1.065 mmol)的甲苯(5 mL)攪拌溶液中加入1,8-二氮雜二環[5.4.0]十一碳-7-烯 (0.027 mL, 0.178 mmol)。將所得反應混合物在115℃下攪拌12小時。真空蒸發甲苯至幹,並將殘餘物溶於乙酸乙酯(25mL)。將有機層用水(75mL)洗滌,用無水硫酸鈉乾燥,並在減壓下濃縮,得到粗產物。將所得粗產物通過矽膠柱色譜法(使用20%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到((4-(3-(3,5-二氯苯基)-4,4,4-三氟丁基-2-烯醯)-2-甲基苯基)氨基)二甲基- 6
-磺胺酮 (0.400 g, 0.888 mmol, 92%產率)。1
H-NMR (400 MHz, CHLOROFORM-D) δ 7.63 (d, J = 1.5 Hz, 1H), 7.55 (dd, J = 8.3, 2.2 Hz, 1H), 7.37 (t, J = 1.5 Hz, 1H), 7.30 (t, J = 2.0 Hz, 1H), 7.20 (d, J = 8.3 Hz, 1H), 7.17 (d, J = 1.7 Hz, 2H), 3.21 (s, 6H), 2.21 (s, 3H); M/Z=[M+1]: 449.95。
以下表2列出的化合物可通過上文所述的步驟製備。表 2 :
| 序號 | 化學名 | 分析資料 | 產率 |
| 1-b | 3((4-(3-(3,5-二氯苯基)-4,4,4-三氟丁基-2-烯醯)-2-甲基苯基)氨基)二甲基- 6 -磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.63 (d, J = 1.5 Hz, 1H), 7.55 (dd, J = 8.3, 2.2 Hz, 1H), 7.37 (t, J = 1.5 Hz, 1H), 7.30 (t, J = 2.0 Hz, 1H), 7.20 (d, J = 8.3 Hz, 1H), 7.17 (d, J = 1.7 Hz, 2H), 3.21 (s, 6H), 2.21 (s, 3H); M/Z=[M+1]: 449.95 | 92% |
| 2-b | 3-(3,5-二氯苯基)-4,4,4-三氟-1-(3-甲基-4-((1-氧化四氫-1 6 -噻吩-1-基亞基)氨基)苯基)丁基-2-烯-1-酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.63 (s, 1H), 7.57 (dd, J = 8.1, 2.4 Hz, 1H), 7.37 (d, J = 1.2 Hz, 1H), 7.30 (t, J = 1.8 Hz, 1H), 7.16-7.17 (m, 2H), 7.13 (d, J = 8.3 Hz, 1H), 3.43-3.48 (m, 2H), 3.23-3.30 (m, 2H), 2.23 (s, 3H), 1.24-1.28 (m, 4H); M/Z=[M+1]: 475.85 | 99% |
| 3-b | ((4-(3-(3,5-二氯-4-氟苯基)-4,4,4-三氟丁基-2-烯醯)-2-甲基苯基)氨基)二甲基- 6 -磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.66 (d, J = 1.5 Hz, 1H), 7.58 (dd, J = 8.3, 2.0 Hz, 1H), 7.41 (t, J = 1.3 Hz, 1H), 7.27 (d, J = 6.1 Hz, 2H), 7.23 (d, J = 8.3 Hz, 1H), 3.24 (s, 6H), 2.24 (s, 3H); M/Z=[M+1]: 467.95 | 45% |
| 4-b | 3-(3,5-二氯-4-氟苯基)-4,4,4-三氟-1-(3-甲基-4-((1-氧化四氫-1 6 -噻吩-1-基亞基)氨基)苯基)丁基-2-烯-1-酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.65 (d, J = 1.5 Hz, 1H), 7.54-7.60 (m, 1H), 7.41 (d, J = 1.5 Hz, 1H), 7.27 (d, J = 6.1 Hz, 2H), 7.02-7.15 (m, 1H), 3.40-3.47 (m, 2H), 3.24-3.31 (m, 2H), 2.23 (s, 3H), 1.27-1.32 (m, 4H); M/Z=[M+1]: 493.65 | 23% |
| 5-b | ((4-(3-(3,5-二氯苯基)-4,4,4-三氟丁基-2-烯醯)-2-甲基苯基)氨基)(3-氟苯基)(甲基)- 6 -磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.69-7.72 (m, 1H), 7.63 (dt, J = 7.3, 2.1 Hz, 2H), 7.55 (td, J = 8.1, 5.2 Hz, 1H), 7.36-7.40 (m, 1H), 7.31-7.35 (m, 2H), 7.27 (d, J = 2.0 Hz, 1H), 7.12 (d, J = 1.7 Hz, 2H), 6.93 (d, J = 8.3 Hz, 1H), 3.30 (s, 3H), 2.35 (s, 3H); M/Z=[M+1]. | 83% |
| 6-b | (Z)-((4-(3-(3,5-二氯苯基)-4,4,4-三氟丁基-2-烯醯)-2-甲基苯基)氨基)(甲基)(苯基)- 6 -磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.92 (d, J = 7.3 Hz, 3H), 7.63 (d, J = 8.6 Hz, 2H), 7.56 (t, J = 7.6 Hz, 2H), 7.38 (s, 1H), 7.31 (s, 1H), 7.12 (s, 2H), 6.94 (d, J = 8.6 Hz, 1H), 3.29 (s, 3H), 2.36 (s, 3H); M/Z=[M+1]: 512.00 | 52% |
| 7-b | ((4-(3-(3,5-二氯苯基)-4,4,4-三氟丁基-2-烯醯)-2-甲基苯基)氨基)(4-甲氧基苯基)(甲基)- 6 -磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.80-7.84 (m, 2H), 7.61 (s, 1H), 7.37 (dd, J = 8.2, 2.1 Hz, 1H), 7.31 (d, J = 1.5 Hz, 1H), 7.26 (d, J = 1.5 Hz, 1H), 7.12 (d, J = 1.5 Hz, 2H), 6.98-7.02 (m, 2H), 6.93 (d, J = 8.3 Hz, 1H), 3.87 (s, 3H), 3.27 (s, 3H), 2.35 (s, 3H); M/Z=[M+1]: 541.80 | 88% |
| 8-b | ((4-(3-(3,5-二氯苯基)-4,4,4-三氟丁基-2-烯醯)-2-甲基苯基)氨基)(2,6-二甲基苯基)(甲基)- 6 -磺胺酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.69 (d, J = 1.5 Hz, 1H), 7.61-7.64 (m, 2H), 7.36-7.43 (m, 2H), 7.22-7.26 (m, 4H), 6.65 (q, J = 4.2 Hz, 1H), 3.49-3.53 (m, 3H), 2.58-2.63 (m, 6H), 2.24-2.26 (m, 3H) | 78% |
| 9-b | 3-(3,5-二氯苯基)-4,4,4-三氟-1-(3-甲基-4-((1-氧化四氫-2H-1 6 -噻喃-1-基亞基)氨基)苯基)丁基-2-烯-1-酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.69-7.79 (m, 1H), 7.55-7.65 (m, 3H), 7.30 (t, J = 1.8 Hz, 2H), 7.08-7.14 (m, 1H), 3.42-3.46 (m, 2H), 3.26-3.34 (m, 2H), 2.20-2.25 (m, 3H), 1.95 (d, J = 19.3 Hz, 2H), 1.77-1.83 (m, 2H), 1.66 (d, J = 10.5 Hz, 1H), 1.49-1.58 (m, 1H); M/Z=[M+1]: 489.75 | 95% |
| 10-b | (2-氯代-6-甲基苯基)((4-(3-(3,5-二氯苯基)-4,4,4-三氟丁基-2-烯醯)-2-甲基苯基)氨基)(甲基)- 6 -磺胺酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.68-7.72 (m, 1H), 7.59-7.64 (m, 2H), 7.39-7.54 (m, 5H), 7.26 (d, J = 1.7 Hz, 2H), 6.67-6.71 (m, 1H), 3.66-3.68 (m, 3H), 2.75-2.77 (m, 3H), 2.25-2.27 (m, 3H); M/Z=[M+1]: 561.70 | 64% |
| 11-b | ((4-(3-(3,5-二氯苯基)-4,4,4-三氟丁基-2-烯醯)-2-甲基苯基)氨基)(2-甲氧基苯基)(甲基)- 6 -磺胺酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.90-7.95 (m, 1H), 7.71 (d, J = 1.5 Hz, 1H), 7.60-7.67 (m, 3H), 7.56 (d, J = 1.8 Hz, 1H), 7.38-7.43 (m, 1H), 7.26 (d, J = 1.8 Hz, 2H), 7.21 (t, J = 7.3 Hz, 1H), 7.13-7.17 (m, 1H), 6.83 (q, J = 2.9 Hz, 1H), 3.84 (s, 3H), 3.49-3.53 (m, 3H), 2.19-2.22 (m, 3H); M/Z=[M+1]: 542.00 | 88% |
| 12-b | ((4-(3-(3,5-二氯苯基)-4,4,4-三氟丁基-2-烯醯)-2-甲基苯基)氨基)二苯基- 6 -磺胺酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.03-8.08 (m, 4H), 7.74-7.77 (m, 1H), 7.59-7.72 (m, 8H), 7.43-7.53 (m, 2H), 7.28 (d, J = 1.8 Hz, 1H), 6.93 (d, J = 8.6 Hz, 1H), 2.49 (s, 3H) | 70% |
第
3
步:
((4-(5-(3,5-
二氯苯基
)-5-(
三氟甲基
)-4,5-
二氫異惡唑
-3-
基)
-2-
甲基苯基
)
氨基
)
二甲基
- 6
-
磺胺酮的合成:
在25℃下,在氮氣環境中向((4-(3-(3,5-二氯苯基)-4,4,4-三氟丁基-2-烯醯)-2-甲基苯基)氨基)二甲基- 6
-磺胺酮 (0.2 g, 0.444 mmol)、氫氧化鉀(0.249 g,4.44 mmol)和四丁基溴化銨(0.029 g,0.089 mmol)的二氯甲苯(2.5 mL)攪拌溶液中加入鹽酸羥胺(0.083 g, 1.33 mmol)。將得到的反應混合物在25℃下攪拌3小時。反應完成後,將反應混合物用水(10mL)稀釋,並將所得混合物用二氯甲烷(25mL)萃取。混合的有機層用鹽水洗滌,用無水硫酸鈉乾燥並在減壓下濃縮以獲得粗產物。所獲得的粗產物通過矽膠柱色譜法(使用甲醇/ 二氯甲烷(2/98)溶液作為洗脫劑)純化,得到((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)二甲基- 6
-磺胺酮(162 mg, 0.444 mmol, 78%產率)。M/Z=[M+1]:465.15,1
H-NMR (400 MHz, CHLOROFORM-D) δ 7.51 (dd, J = 6.4, 1.5 Hz, 3H), 7.40-7.42 (m, 1H), 7.33 (dd, J = 8.3, 2.0 Hz, 1H), 7.22 (d, J = 8.3 Hz, 1H), 4.05 (dd, J = 17.1, 5.6 Hz, 1H), 3.66 (d, J = 17.1 Hz, 1H), 3.20 (s, 6H), 2.25 (s, 3H)。
例
4
:
4-(5-(3,5-
二氯苯基
)-5-(
三氟甲基
)-4,5-
二氫異惡唑
-3-
基)
-N-((3,4-
二甲基苯基
)
亞磺醯基
)-2-
甲基苯甲醯胺
(217)
的合成
在0°C下向3-(N-(4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯)-3,4-二甲基苯基磺醯亞胺基)丙酸甲酯(500 mg, 0.763 mmol)的四氫呋喃(4 mL)溶液中加入氫氧化鋰一水合物(35.2 mg,0.839 mmol)的水(1 mL)溶液並在25°C下攪拌30分鐘。反應完成後,將反應混合物用水(15 mL)稀釋並用乙酸乙酯(40 mL)萃取。用無水硫酸鈉乾燥,減壓濃縮,得到粗產物,將所得粗產物通過快速色譜法(使用50%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二甲基苯基) 亞磺醯基)-2-甲基苯甲醯胺 (204 mg, 0.358 mmol, 47%產率)。1
H-NMR (400 MHz, DMSO-d6
) δ 11.56 (s, 1H), 7.80 (t,J
= 1.8 Hz, 1H), 7.59-7.63 (m, 4H), 7.54 (s, 1H), 7.49 (q,J
= 7.9 Hz, 2H), 7.35-7.38 (m, 1H), 4.37 (dd,J
= 18.3, 2.0 Hz, 1H), 4.28 (d,J
= 20.3 Hz, 1H), 2.40 (s, 3H), 2.31 (s, 3H), 2.29 (s, 3H); ESI MS (m/z
): 569.05 (M-H)。
表3中的以下化合物是使用合適的起始原料並按照通用方案1-6或實施例1-4中所述的類似方法獲得的。表 3 :
*使用Chemdraw Professional 18.1生成的化合物名稱生物實例:
| 化合物編號 | 化合物名稱 | 分析數據 |
| 1 | ((2-氯代-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-6-甲基苯基)氨基)二甲基-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.56-7.56 (m, 1H), 7.51 (dd, J = 7.8, 1.7 Hz, 2H), 7.42 (t, J = 2.0 Hz, 1H), 7.39 (q, J = 0.9 Hz, 1H), 4.04 (d, J = 17.1 Hz, 1H), 3.65 (d, J = 17.4 Hz, 1H), 3.18 (s, 6H), 2.42 (s, 3H); M/Z=[M+1]: 500.85 |
| 2 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)二甲基-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.51 (dd, J = 6.4, 1.5 Hz, 3H), 7.40-7.42 (m, 1H), 7.33 (dd, J = 8.3, 2.0 Hz, 1H), 7.22 (d, J = 8.3 Hz, 1H), 4.05 (dd, J = 17.1, 5.6 Hz, 1H), 3.66 (d, J = 17.1 Hz, 1H), 3.20 (s, 6H), 2.25 (s, 3H); M/Z=[M+1]:465.15 |
| 3 | 1-((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)四氫-1H-1l6-噻吩 1-氧化物 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.51 (s, 2H), 7.48 (s, 1H), 7.40 (s, 1H), 7.32 (d, J = 8.1 Hz, 1H), 7.14 (d, J = 8.3 Hz, 1H), 4.06 (d, J = 17.1 Hz, 1H), 3.66 (d, J = 17.1 Hz, 1H), 3.36-3.42 (m, 2H), 3.17-3.23 (m, 2H), 2.30-2.42 (m, 2H), 2.25 (t, J = 8.2 Hz, 5H); M/Z=[M+1]: 491.00 |
| 4 | 1-((2-氯代-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-6-甲基苯基)氨基)四氫-1H-1l6-噻吩 1-氧化物 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.55 (d, J = 1.7 Hz, 1H), 7.50 (d, J = 1.5 Hz, 2H), 7.42 (t, J = 1.8 Hz, 1H), 7.40 (d, J = 1.5 Hz, 1H), 4.03 (d, J = 17.1 Hz, 1H), 3.65 (d, J = 17.1 Hz, 1H), 3.44-3.50 (m, 2H), 3.11-3.18 (m, 2H), 2.43 (s, 3H), 2.29-2.38 (m, 4H); M/Z=[M+1]: 526.80 |
| 5 | ((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)二甲基-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.59 (d, J = 6.1 Hz, 2H), 7.49 (d, J = 1.7 Hz, 1H), 7.31-7.34 (m, 1H), 7.21 (d, J = 8.3 Hz, 1H), 4.06 (d, J = 17.1 Hz, 1H), 3.65 (d, J = 17.1 Hz, 1H), 3.19 (s, 6H), 2.23 (s, 3H); M/Z=[M+1]: 482.65 |
| 6 | 1-((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)四氫-1H-1l6-噻吩1-氧化物 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.59 (d, J = 6.1 Hz, 2H), 7.48 (s, 1H), 7.32 (dd, J = 8.2, 2.1 Hz, 1H), 7.15 (d, J = 8.1 Hz, 1H), 4.06 (d, J = 17.1 Hz, 1H), 3.64 (d, J = 17.1 Hz, 1H), 3.39-3.45 (m, 2H), 3.18-3.24 (m, 2H), 2.27-2.43 (m, 4H), 2.24 (s, 3H); M/Z=[M+1]: 508.65 |
| 7 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(3-氟苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.71 (dd, J = 7.8, 1.5 Hz, 1H), 7.62-7.65 (m, 1H), 7.46-7.56 (m, 4H), 7.39 (q, J = 1.9 Hz, 1H), 7.28-7.33 (m, 1H), 7.13-7.17 (m, 1H), 6.97 (d, J = 8.3 Hz, 1H), 4.00 (dd, J = 17.1, 5.4 Hz, 1H), 3.60 (d, J = 17.1 Hz, 1H), 3.28 (s, 3H), 2.36 (s, 3H); M/Z=[M+1]: 545.00 |
| 8 | ((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(3-氟苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.71 (d, J = 8.6 Hz, 1H), 7.62-7.64 (m, 1H), 7.52-7.57 (m, 3H), 7.46-7.47 (m, 1H), 7.32 (d, J = 7.3 Hz, 1H), 7.13-7.15 (m, 1H), 6.96-7.00 (m, 1H), 4.00 (dd, J = 17.1, 5.1 Hz, 1H), 3.58 (d, J = 16.1 Hz, 1H), 3.28 (s, 3H), 2.36 (s, 3H); M/Z=[M+1]: 563.00 |
| 9 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(3,5-二甲基苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.77 (t, J = 1.5 Hz, 1H), 7.57 (s, 2H), 7.53 (s, 2H), 7.45 (s, 1H), 7.29 (s, 1H), 7.20 (d, J = 7.9 Hz, 1H), 6.86 (q, J = 4.1 Hz, 1H), 4.21 (dd, J = 18.3, 4.9 Hz, 1H), 4.12 (dd, J = 18.0, 4.0 Hz, 1H), 3.40 (s, 3H), 2.32 (s, 6H), 2.28 (s, 3H); M/Z=[M+1]:555.10 |
| 10 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)二乙基-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.52 (d, J = 1.5 Hz, 2H), 7.47 (d, J = 2.0 Hz, 1H), 7.40 (t, J = 2.0 Hz, 1H), 7.28-7.30 (m, 1H), 7.24 (d, J = 8.3 Hz, 1H), 4.05 (d, J = 17.1 Hz, 1H), 3.65 (d, J = 17.1 Hz, 1H), 3.18-3.25 (m, 4H), 2.24 (s, 3H), 1.40 (t, J = 7.5 Hz, 6H); M/Z=[M+1]: 493.05 |
| 11 | 環己基((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.52 (d, J = 1.5 Hz, 2H), 7.47-7.49 (m, 1H), 7.40 (t, J = 1.8 Hz, 1H), 7.28-7.32 (m, 1H), 7.22-7.26 (m, 1H), 4.05 (dd, J = 17.1, 1.2 Hz, 1H), 3.65 (d, J = 17.1 Hz, 1H), 3.08-3.14 (m, 1H), 2.92 (s, 3H), 2.32-2.34 (m, 2H), 2.23 (s, 3H), 1.96-2.00 (m, 2H), 1.77 (d, J = 12.5 Hz, 1H), 1.51-1.66 (m, 3H), 1.17-1.43 (m, 2H); M/Z=[M+1]: 533.10 |
| 12 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(甲基)(苯基)-l6-磺胺酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.90-7.92 (m, 2H), 7.76 (q, J = 1.7 Hz, 1H), 7.59-7.69 (m, 3H), 7.57 (s, 2H), 7.45 (d, J = 2.0 Hz, 1H), 7.19 (dd, J = 8.3, 2.2 Hz, 1H), 6.85 (dd, J = 8.3, 2.9 Hz, 1H), 4.20 (dd, J = 18.2, 4.5 Hz, 1H), 4.11 (dd, J = 18.1, 5.1 Hz, 1H), 3.45 (s, 3H), 2.28 (s, 3H); M/Z=[M+1]: 527.00; M/Z=[M+1]: 527.00 |
| 13 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(4-甲氧基苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.80-7.84 (m, 2H), 7.77 (q, J = 1.6 Hz, 1H), 7.57 (s, 2H), 7.45 (s, 1H), 7.19 (dd, J = 8.3, 2.0 Hz, 1H), 7.10-7.14 (m, 2H), 6.84 (dd, J = 8.3, 2.9 Hz, 1H), 4.21 (dd, J = 18.1, 3.4 Hz, 1H), 4.11 (dd, J = 18.3, 4.6 Hz, 1H), 3.80-3.82 (m, 3H), 3.39-3.42 (m, 2H), 2.27-2.30 (m, 3H); M/Z=[M+1]: 557.10 |
| 14 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(2,6-二甲基苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.76 (q, J = 2.0 Hz, 1H), 7.56 (d, J = 1.2 Hz, 2H), 7.48 (d, J = 1.8 Hz, 1H), 7.37 (td, J = 7.6, 2.6 Hz, 1H), 7.21 (d, J = 7.3 Hz, 2H), 7.14-7.16 (m, 1H), 6.65 (d, J = 8.6 Hz, 1H), 4.15 (qd, J = 18.1, 8.4 Hz, 2H), 3.48 (s, 3H), 2.59 (s, 6H), 2.24 (s, 3H); M/Z=[M+1]: 555.15 |
| 15 | 1-((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)六氫-1l6-噻喃 1-氧化物 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.78 (t, J = 1.8 Hz, 1H), 7.61 (d, J = 2.0 Hz, 2H), 7.48 (d, J = 1.5 Hz, 1H), 7.37 (dd, J = 8.3, 2.0 Hz, 1H), 7.10 (d, J = 8.3 Hz, 1H), 4.26 (d, J = 18.1 Hz, 1H), 4.16 (d, J = 18.3 Hz, 1H), 3.41 (d, J = 14.2 Hz, 2H), 3.22-3.29 (m, 2H), 2.21 (s, 3H), 1.91-1.94 (m, 2H), 1.74-1.84 (m, 2H), 1.64-1.67 (m, 1H), 1.49-1.57 (m, 1H); M/Z=[M+1]: 505.10 |
| 16 | (2-氯代-6-甲基苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.74 (q, J = 2.0 Hz, 1H), 7.53 (d, J = 1.2 Hz, 2H), 7.36-7.46 (m, 4H), 7.15 (d, J = 8.6 Hz, 1H), 6.67 (d, J = 7.9 Hz, 1H), 4.13 (qd, J = 18.0, 8.1 Hz, 2H), 3.61 (s, 3H), 2.71 (s, 3H), 2.22 (s, 3H); M/Z=[M+1]: 577.00 |
| 17 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(2-甲氧基苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.88-7.91 (m, 1H), 7.76 (q, J = 1.8 Hz, 1H), 7.58-7.63 (m, 1H), 7.56 (d, J = 1.7 Hz, 2H), 7.40 (d, J = 1.7 Hz, 1H), 7.15-7.20 (m, 2H), 7.10-7.14 (m, 1H), 6.84 (d, J = 7.8 Hz, 1H), 4.19 (dd, J = 18.1, 5.9 Hz, 1H), 4.10 (dd, J = 18.3, 5.4 Hz, 1H), 3.83 (s, 3H), 3.47 (s, 3H), 2.20 (s, 3H); M/Z=[M+1]: 557.05 |
| 18 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)二苯基-l6-磺胺酮 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.03-8.06 (m, 4H), 7.79 (t, J = 1.8 Hz, 1H), 7.55-7.68 (m, 9H), 7.25 (dd, J = 8.3, 2.0 Hz, 1H), 6.95 (d, J = 8.3 Hz, 1H), 4.25 (d, J = 18.1 Hz, 1H), 4.15 (d, J = 18.3 Hz, 1H); M/Z=[M+1]: 589.1 |
| 19 | N-(環戊基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.98 (d, J = 8.6 Hz, 1H), 7.59 (d, J = 6.1 Hz, 2H), 7.48 (d, J = 7.3 Hz, 2H), 4.09 (d, J = 17.4 Hz, 1H), 3.93-4.01 (m, 1H), 3.69 (d, J = 17.4 Hz, 1H), 3.36 (s, 3H), 2.60 (s, 3H), 2.04-2.28 (m, 4H), 1.69-1.95 (m, 4H); M/Z=[M+1]: 565.00 |
| 20 | N-(叔丁基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.98 (d, J = 8.3 Hz, 1H), 7.50-7.52 (m, 3H), 7.46 (s, 1H), 7.42 (t, J = 1.8 Hz, 1H), 4.09 (d, J = 17.1 Hz, 1H), 3.70 (d, J = 17.1 Hz, 1H), 3.41 (s, 3H), 2.64 (s, 3H), 1.57 (s, 9H); M/Z=[M+1]: 535.00 |
| 21 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-甲氧基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.08 (dd, J = 8.2, 1.6 Hz, 1H), 7.95-7.98 (m, 2H), 7.53 (q, J = 3.9 Hz, 3H), 7.47 (d, J = 4.2 Hz, 1H), 7.43 (dd, J = 3.3, 1.3 Hz, 1H), 7.07-7.10 (m, 2H), 4.09 (d, J = 17.4 Hz, 1H), 3.90 (s, 3H), 3.71 (d, J = 17.4 Hz, 1H), 3.44 (s, 3H), 2.62 (s, 3H); M/Z=[M+1]: 585.00 |
| 22 | N-((2-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.32-8.35 (m, 1H), 8.07 (d, J = 8.1 Hz, 1H), 7.56-7.65 (m, 5H), 7.51 (d, J = 7.8 Hz, 1H), 7.45 (s, 1H), 4.09 (d, J = 17 Hz, 1H), 3.71 (d, J = 17 Hz, 1H), 3.55 (s, 3H), 2.57 (s, 3H); M/Z=[M+1]: 609.00 |
| 23 | N-(烯丙基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.01 (d, J = 8.3 Hz, 1H), 7.59 (d, J = 6.1 Hz, 2H), 7.48-7.52 (m, 2H), 5.93-6.04 (m, 1H), 5.56-5.62 (m, 2H), 4.36 (dd, J = 13.8, 7.7 Hz, 1H), 4.21 (dd, J = 13.8, 7.7 Hz, 1H), 4.09 (d, J = 17.1 Hz, 1H), 3.69 (d, J = 17.1 Hz, 1H), 3.26 (s, 3H), 2.63 (s, 3H); M/Z=[M+1]: 536.70 |
| 24 | 甲基3-(N-(4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯)-S-甲基磺醯亞胺基)丙酸酯 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.84 (d, J = 8.8 Hz, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.62 (d, J = 1.7 Hz, 2H), 7.59 (d, J = 7.1 Hz, 2H), 4.38 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.6 Hz, 1H), 3.79-3.90 (m, 2H), 3.63 (s, 3H), 3.49 (s, 3H), 2.92 (td, J = 7.3, 4.0 Hz, 2H), 2.51 (s, 3H); M/Z=[M+1]: 564.95 |
| 25 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.08 (d, J = 8.1 Hz, 1H), 7.62 (s, 2H), 7.52-7.54 (m, 3H), 7.48 (s, 1H), 7.42-7.44 (m, 1H), 7.30 (s, 1H), 4.10 (d, J = 17.2, 1H), 3.71 (d, J = 17.2, 1H), 3.40 (s, 3H), 2.62 (s, 3H), 2.41 (s, 6H); M/Z=[M+1]: 583.10 |
| 26 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(氧二苯基-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.21 (d, J = 8.1 Hz, 1H), 8.04-8.06 (m, 4H), 7.53-7.62 (m, 9H), 7.47 (s, 1H), 4.10 (d, J = 17.1 Hz, 1H), 3.70 (d, J = 17.4 Hz, 1H), 2.61 (s, 3H); M/Z=[M+1]: 635.05 |
| 27 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(苯基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.09 (d, J = 8.1 Hz, 1H), 8.03-8.06 (m, 2H), 7.69-7.73 (m, 1H), 7.62-7.65 (m, 2H), 7.59 (d, J = 6.1 Hz, 2H), 7.52-7.54 (m, 1H), 7.47 (s, 1H), 4.10 (d, J = 17.1 Hz, 1H), 3.69 (d, J = 17.1 Hz, 1H), 3.45 (s, 3H), 2.62 (s, 3H); M/Z=[M+1]: 573.00 |
| 28 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.08 (d, J = 8.1 Hz, 1H), 7.62 (s, 2H), 7.59 (d, J = 6.1 Hz, 2H), 7.53 (dd, J = 8.1, 1.7 Hz, 1H), 7.47 (s, 1H), 7.30 (s, 1H), 4.09 (d, J = 17 Hz, 1H), 3.69 (d, J = 17.2 Hz, 1H), 3.42 (s, 3H), 2.60 (s, 3H), 2.42 (s, 6H); M/Z=[M+1]: 600.80 |
| 29 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧化四氫-1l6-噻吩-1-基亞基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.04 (d, J = 7.8 Hz, 1H), 7.59 (d, J = 6.1 Hz, 2H), 7.49-7.52 (m, 2H), 4.07-4.13 (m, 1H), 3.67-3.74 (m, 3H), 3.34-3.41 (m, 2H), 2.63 (s, 3H), 2.29-2.44 (m, 4H); M/Z=[M+1]: 536.70 |
| 30 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.17 (td, J = 8.5, 6.0 Hz, 1H), 8.01 (d, J = 8.1 Hz, 1H), 7.51-7.52 (m, 3H), 7.46 (s, 1H), 7.42 (t, J = 1.8 Hz, 1H), 7.15-7.19 (m, 1H), 7.00-7.05 (m, 1H), 4.08 (d, J = 17.4 Hz, 1H), 3.69 (d, J = 17.4 Hz, 1H), 3.53 (s, 3H), 2.59 (s, 3H); M/Z=[M+1]: 590.95 |
| 31 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(二乙基(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.01 (dd, J = 7.8, 2.4 Hz, 1H), 7.59 (dd, J = 6.1, 2.0 Hz, 2H), 7.48-7.52 (m, 2H), 4.09 (d, J = 17.1 Hz, 1H), 3.69 (d, J = 17.1 Hz, 1H), 3.58 (m, 2H), 3.46 (m, 2H), 2.62 (s, 3H), 1.44-1.50 (m, 6H); M/Z=[M+1]: 539.10 |
| 32 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.08 (d, J = 8.1 Hz, 1H), 7.49-7.58 (m, 5H), 7.46 (s, 1H), 7.12-7.17 (m, 1H), 4.07 (d, J = 17.1 Hz, 1H), 3.67 (d, J = 17.1 Hz, 1H), 3.41 (s, 3H), 2.60 (s, 3H); M/Z=[M+1]: 608.75 |
| 33 | N-((2-氰丙烷-2-基)(異丙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.02 (d, J = 8.1 Hz, 1H), 7.50-7.53 (m, 4H), 7.43 (t, J = 1.8 Hz, 1H), 4.07-4.18 (m, 2H), 3.70 (d, J = 17.4 Hz, 1H), 2.65 (s, 3H), 1.95 (s, 3H), 1.93 (s, 3H), 1.76 (d, J = 6.8 Hz, 3H), 1.68 (d, J = 6.8 Hz, 3H); M/Z=[M+1]: 573.90 |
| 34 | N-((2-氰丙烷-2-基)(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.04 (d, J = 8.1 Hz, 1H), 7.59 (d, J = 5.9 Hz, 2H), 7.51 (m, 2H), 4.09 (d, J = 17.1 Hz, 1H), 3.85-3.99 (m, 2H), 3.69 (d, J = 17.1 Hz, 1H), 2.65 (s, 3H), 1.93 (s, 3H), 1.90 (s, 3H), 1.66 (t, J = 7.5 Hz, 3H); M/Z=[M+1]:578.05 |
| 35 | N-((2-氰丙烷-2-基)(異丙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.94 (d, J = 8.8 Hz, 1H), 7.82 (d, J = 6.1 Hz, 2H), 7.64 (d, J = 7.1 Hz, 2H), 4.30-4.46 (m, 3H), 2.57 (s, 3H), 1.89 (s, 3H), 1.87 (s, 3H), 1.61 (d, J = 6.8 Hz, 3H), 1.52-1.56 (d, J = 6.8 Hz, 3H); M/Z=[M+1]: 591.85 |
| 36 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異丙基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.81 (d, J = 8.6 Hz, 1H), 7.78 (t, J = 1.8 Hz, 1H), 7.55-7.60 (m, 4H), 4.34 (d, J = 18.4 Hz, 1H), 4.24 (d, J = 18.4 Hz, 1H), 3.79 (q, J = 6.8 Hz, 1H), 3.56-3.68 (m, 2H), 2.49 (s, 3H), 1.35 (d, J = 6.8 Hz, 6H), 1.29 (t, J = 7.3 Hz, 3H); M/Z=[M+1]: 535.05 |
| 37 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(氧代)(丙基)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.86 (d, J = 8.1 Hz, 1H), 7.81-7.83 (m, 2H), 7.58-7.61 (m, 2H), 4.35 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.50-3.66 (m, 4H), 2.54 (s, 3H), 1.76-1.87 (m, 2H), 1.33 (t, J = 7.3 Hz, 3H), 1.05 (t, J = 7.3 Hz, 3H); M/Z=[M+1]: 552.75 |
| 38 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(丙基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.86 (d, J = 7.8 Hz, 1H), 7.82 (d, J = 6.4 Hz, 2H), 7.60 (d, J = 8.6 Hz, 2H), 4.35 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.52-3.62 (m, 2H), 3.41 (s, 3H), 2.55 (s, 3H), 1.78-1.87 (m, 2H), 1.05 (t, J = 7.5 Hz, 3H); M/Z=[M+1]: 538.75 |
| 39 | N-((2-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.32-8.35 (m, 1H), 8.07 (d, J = 8.1 Hz, 1H), 7.56-7.65 (m, 3H), 7.51-7.52 (m, 3H), 7.45 (s, 1H), 7.42 (t, J = 1.8 Hz, 1H), 4.06 (d, J = 17.4 Hz, 1H), 3.69 (d, J = 17.4 Hz, 1H), 3.55 (s, 3H), 2.57 (s, 3H); M/Z=[M+1]: 590.75 |
| 40 | N-((3-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.10 (d, J = 8.1 Hz, 1H), 8.02 (t, J = 2.0 Hz, 1H), 7.92 (dq, J = 7.9, 1.0 Hz, 1H), 7.66-7.68 (m, 1H), 7.58-7.60 (m, 3H), 7.52-7.56 (m, 1H), 7.48 (s, 1H), 4.09 (d, J = 17.4 Hz, 1H), 3.70 (d, J = 17.4 Hz, 1H), 3.41 (s, 3H), 2.60 (s, 3H); M/Z=[M+1]: 606.75 |
| 41 | N-((3-溴苯基)(環丙基甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.17 (t, J = 1.8 Hz, 1H), 8.10 (d, J = 8.1 Hz, 1H), 7.96 (m, 1H), 7.81-7.83 (m, 1H), 7.59 (d, J = 6.1 Hz, 2H), 7.54 (dd, J = 8.2, 1.3 Hz, 1H), 7.47-7.52 (m, 2H), 4.10 (d, J = 17.4 Hz, 1H), 3.70 (d, J = 17.4 Hz, 1H), 3.54 (m, 2H), 2.62 (s, 3H), 0.96-1.06 (m, 1H), 0.56-0.68 (m, 2H), 0.22-0.28 (m, 1H), 0.13-0.19 (m, 1H); M/Z=[M+1]: 692.95 |
| 42 | N-((2-氯代-6-甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.04 (d, J = 8.1 Hz, 1H), 7.58 (d, J = 6.1 Hz, 2H), 7.50 (d, J = 8.1 Hz, 1H), 7.45 (s, 1H), 7.39-7.42 (m, 2H), 7.29-7.33 (m, 1H), 4.08 (d, J = 17.4 Hz, 1H), 3.68 (d, J = 17.4 Hz, 1H), 3.61 (s, 3H), 2.92 (s, 3H), 2.57 (s, 3H); M/Z=[M+1]: 623.00 |
| 43 | N-((4-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.09 (d, J = 8.3 Hz, 1H), 7.90 (dt, J = 8.9, 2.2 Hz, 2H), 7.77 (dt, J = 9.0, 2.1 Hz, 2H), 7.53 (dd, J = 11.4, 1.3 Hz, 3H), 7.47 (s, 1H), 7.43 (t, J = 1.8 Hz, 1H), 4.09 (d, J = 17.1 Hz, 1H), 3.70 (d, J = 17.1 Hz, 1H), 3.43 (s, 3H), 2.61 (s, 3H); M/Z=[M+1]: 634.60 |
| 44 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧化四氫-1l6-噻吩-1-基亞基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.03 (d, J = 8.1 Hz, 1H), 7.49-7.52 (m, 4H), 7.42 (t, J = 1.8 Hz, 1H), 4.09 (d, J = 17.4 Hz, 1H), 3.67-3.75 (m, 3H), 3.34-3.40 (m, 2H), 2.63 (s, 3H), 2.27-2.47 (m, 4H); M/Z=[M+1]: 519.15 |
| 45 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.10 (d, J = 8.1 Hz, 1H), 7.84 (dq, J = 7.8, 0.9 Hz, 1H), 7.75 (dt, J = 7.8, 2.1 Hz, 1H), 7.62-7.59 (m, 3H), 7.54 (dd, J = 8.2, 1.3 Hz, 1H), 7.48 (s, 1H), 7.40 (td, J = 8.3, 2.5 Hz, 1H), 4.10 (d, J = 17.1 Hz, 1H), 3.65 (d, J = 17.1 Hz, 1H), 3.45 (s, 3H), 2.60 (s, 3H); M/Z=[M+1]: 591.00 |
| 46 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧化四氫-2H-1l6-噻喃-1-基亞基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.01 (d, J = 8.1 Hz, 1H), 7.48-7.52 (m, 4H), 7.42 (t, J = 1.8 Hz, 1H), 4.09 (d, J = 17.4 Hz, 1H), 3.75-3.81 (m, 2H), 3.70 (d, J = 17.4 Hz, 1H), 3.26-3.33 (m, 2H), 2.63 (s, 3H), 2.06-2.26 (m, 4H), 1.65-1.80 (m, 2H); M/Z=[M+1]: 533.05 |
| 47 | N-(環戊基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.98 (d, J = 8.6 Hz, 1H), 7.47-7.52 (m, 4H), 7.42-7.43 (m, 1H), 4.09 (d, J = 17.1Hz, 1H), 3.92 (d, J = 17.1Hz, 1H), 3.68-3.73 (m, 1H), 3.38 (s, 3H), 2.62 (s, 3H), 2.17-2.28 (m, 2H), 2.07-2.16 (m, 2H), 1.82-1.95 (m, 2H), 1.68-1.80 (m, 2H); M/Z=[M+1]: 547.10 |
| 48 | N-((3-溴苯基)(環丙基甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.17 (t, J = 1.8 Hz, 1H), 8.11 (d, J = 8.1 Hz, 1H), 7.96 (dq, J = 8.0, 0.9 Hz, 1H), 7.82 (dt, J = 8.1, 0.7 Hz, 1H), 7.47-7.56 (m, 5H), 7.43 (t, J = 1.8 Hz, 1H), 4.07-4.13 (d, J = 17.4 Hz, 1H), 3.71 (d, J = 17.4 Hz, 1H), 3.49-3.58 (m, 2H), 2.62 (s, 3H), 0.97-1.06 (m, 1H), 0.56-0.68 (m, 2H), 0.13-0.28 (m, 2H); M/Z=[M+1]: 674.95 |
| 49 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.10 (d, J = 8.1 Hz, 1H), 7.57-7.61 (m, 2H), 7.56 (d, J = 1.2 Hz, 1H), 7.53 (dd, J = 7.7, 1.3 Hz, 2H), 7.49 (s, 1H), 7.43 (t, J = 1.8 Hz, 1H), 7.14 (tt, J = 8.3, 2.2 Hz, 1H), 4.10 (d, J = 17.1 Hz, 1H), 3.71 (d, J = 17.1 Hz, 1H), 3.44 (s, 3H), 2.61 (s, 3H); M/Z=[M+1]: 590.70 |
| 50 | N-(環己基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.99 (d, J = 7.8 Hz, 1H), 7.48-7.52 (m, 4H), 7.42 (t, J = 1.8 Hz, 1H), 4.09 (d, J = 17.4 Hz, 1H), 3.70 (d, J = 17.1 Hz, 1H), 3.50 (tt, J = 12.2, 3.4 Hz, 1H), 3.30 (s, 3H), 2.59-2.65 (m, 3H), 2.28 (t, J = 14.5 Hz, 2H), 1.98-2.04 (m, 2H), 1.79 (d, J = 13.0 Hz, 1H), 1.59-1.68 (m, 1H), 1.32-1.45 (m, 2H), 1.19-1.30 (m, 2H); M/Z=[M+1]: 560.80 |
| 51 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異丙基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.00 (d, J = 8.3 Hz, 1H), 7.59 (d, J = 6.1 Hz, 2H), 7.49 (d, J = 7.6 Hz, 2H), 4.09 (d, J = 17.1 Hz, 1H), 3.82-3.89 (m, 1H), 3.66-3.75 (m, 2H), 3.52-3.43 (m, 1H), 2.64 (s, 3H), 1.52 (d, J = 2.9 Hz, 3H), 1.50 (d, J = 2.9 Hz, 3H), 1.47 (t, J = 7.5 Hz, 3H); M/Z=[M+1]: 552.70 |
| 52 | N-((2-氰丙烷-2-基)(氧代)(丙基)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.02 (d, J = 7.9 Hz, 1H), 7.51 (dd, J = 6.6, 5.0 Hz, 4H), 7.43 (t, J = 1.8 Hz, 1H), 4.09 (d, J = 17.1 Hz, 1H), 3.74-3.90 (m, 2H), 3.70 (d, J = 17.4 Hz, 1H), 2.64 (s, 3H), 2.05-2.22 (m, 2H), 1.92 (s, 3H), 1.90 (s, 3H), 1.16 (t, J = 7.3 Hz, 3H); M/Z=[M+1]: 573.90 |
| 53 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異丁基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.83 (d, J = 8.1 Hz, 1H), 7.80 (d, J = 6.4 Hz, 2H), 7.57-7.59 (m, 2H), 4.35 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.57-3.68 (m, 2H), 3.52 (dd, J = 14.1, 6.5 Hz, 1H), 3.41 (dd, J = 14.2, 6.6 Hz, 1H), 2.52 (s, 3H), 2.28-2.38 (m, 1H), 1.31 (q, J = 7.4 Hz, 3H), 1.07 (d, J = 6.8 Hz, 6H); M/Z=[M+1]: 566.75 |
| 54 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異戊基(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.83 (d, J = 8.3 Hz, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.62 (d, J = 1.5 Hz, 2H), 7.59 (d, J = 7.6 Hz, 2H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.54-3.62 (m, 2H), 3.42 (s, 3H), 2.51 (s, 3H), 1.60-1.78 (m, 3H), 0.92 (s, 3H), 0.90 (s, 3H); M/Z=[M+1]: 549.10 |
| 55 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(二甲基(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.01-8.03 (m, 1H), 7.59 (d, J = 5.9 Hz, 2H), 7.50 (t, J = 6.5 Hz, 2H), 4.09 (d, J = 17.4 Hz, 1H), 3.69 (d, J = 17.1 Hz, 1H), 3.40 (s, 6H), 2.63 (s, 3H); M/Z=[M+1]: 510.95 |
| 56 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧化四氫-2H-1l6-噻喃-1-基亞基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.00-8.02 (m, 1H), 7.58-7.60 (m, 2H), 7.46-7.51 (m, 2H), 4.10 (d, J = 17.4 Hz, 1H), 3.75-3.81 (m, 2H), 3.69 (d, J = 17.4 Hz, 1H), 3.27-3.33 (m, 2H), 2.63 (s, 3H), 2.03-2.26 (m, 4H), 1.65-1.80 (m, 2H); M/Z=[M+1]: 551.05 |
| 57 | N-((3-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.17 (t, J = 1.8 Hz, 1H), 8.09 (d, J = 8.1 Hz, 1H), 7.96 (dq, J = 7.9, 0.9 Hz, 1H), 7.81-7.84 (m, 1H), 7.59 (d, J = 6.1 Hz, 2H), 7.48-7.55 (m, 3H), 4.10 (d, J = 17.1 Hz, 1H), 3.69 (d, J = 17.1 Hz, 1H), 3.44 (s, 3H), 2.61 (s, 3H); M/Z=[M+1]: 652.85 |
| 58 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.05-8.08 (m, 1H), 7.51-7.54 (m, 3H), 7.45 (s, 1H), 7.42 (t, J = 1.8 Hz, 1H), 7.36 (t, J = 7.6 Hz, 1H), 7.20 (d, J = 7.6 Hz, 2H), 4.08 (d, J = 17.1 Hz, 1H), 3.70 (d, J = 17.1 Hz, 1H), 3.40 (s, 3H), 2.74 (s, 6H), 2.59 (s, 3H); M/Z=[M+1]: 582.95 |
| 59 | N-((3-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.17 (t, J = 1.8 Hz, 1H), 8.09 (d, J = 8.1 Hz, 1H), 7.97 (dq, J = 8.0, 0.9 Hz, 1H), 7.82 (d, J = 8.1 Hz, 1H), 7.49-7.56 (m, 5H), 7.43 (t, J = 1.8 Hz, 1H), 4.09 (d, J = 17.1 Hz, 1H), 3.70 (d, J = 17.1 Hz, 1H), 3.44 (s, 3H), 2.60 (s, 3H); M/Z=[M+1]: 634.65 |
| 60 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧負離子基-1l6-硫雜環丁烷基-1-基亞基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.07 (d, J = 8.1 Hz, 1H), 7.51 (d, J = 6.8 Hz, 4H), 7.43 (s, 1H), 4.50-4.57 (m, 2H), 4.28-4.36 (m, 2H), 4.10 (d, J = 17.1 Hz, 1H), 3.71 (d, J = 17.4 Hz, 1H), 2.65 (s, 3H), 2.46-2.57 (m, 2H); M/Z=[M+1]: 504.90 |
| 61 | N-((2-氰丙烷-2-基)(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.04 (d, J = 8.1 Hz, 1H), 7.50-7.53 (m, 4H), 7.43 (t, J = 1.8 Hz, 1H), 4.09 (d, J = 17.4 Hz, 1H), 3.84-3.99 (m, 2H), 3.70 (d, J = 17.4 Hz, 1H), 2.65 (s, 3H), 1.93 (s, 3H), 1.90 (s, 3H), 1.66 (t, J = 7.5 Hz, 3H); M/Z=[M+1]: 560.05 |
| 62 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異戊基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.80-7.83 (m, 2H), 7.62 (d, J = 1.8 Hz, 2H), 7.59 (d, J = 7.3 Hz, 2H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.52-3.64 (m, 4H), 2.51 (s, 3H), 1.57-1.75 (m, 3H), 1.31 (t, J = 7.3 Hz, 3H), 0.90 (d, J= 6.4 Hz, 6H); M/Z=[M+1]: 562.80 |
| 63 | N-(仲丁基(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.83 (d, J = 7.9 Hz, 1H), 7.80 (d, J = 6.4 Hz, 2H), 7.58 (d, J = 8.6 Hz, 2H), 4.36 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.6 Hz, 1H), 3.54-3.72 (m, 3H), 2.51 (s, 3H), 2.04 (m, 1H), 1.48-1.63 (m, 1H), 1.29-1.41 (m, 6H), 1.01 (t, J = 7.3 Hz, 3H); M/Z=[M+1]: 567.15 |
| 64 | N-(環己基(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.83 (d, J = 7.6 Hz, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.62 (d, J = 1.8 Hz, 2H), 7.58 (d, J = 8.3 Hz, 2H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.57-3.69 (m, 3H), 2.51 (s, 3H), 2.12 (t, J = 15.0 Hz, 2H), 1.85 (d, J = 13.1 Hz, 2H), 1.65 (d, J = 12.8 Hz, 1H), 1.45-1.60 (m, 2H), 1.25-1.39 (m, 5H), 1.14-1.22 (m, 1H); M/Z=[M+1]: 575.05 |
| 65 | N-(仲丁基(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.83 (d, J = 8.3 Hz, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.62 (d, J = 1.5 Hz, 2H), 7.58 (d, J = 7.6 Hz, 2H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.54-3.70 (m, 3H), 2.51 (s, 3H), 2.01-2.08 (m, 1H), 1.48-1.61 (m, 1H), 1.29-1.38 (m, 6H), 1.01 (t, J = 7.5 Hz, 3H); M/Z=[M+1]: 549.00 |
| 66 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異丁基(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.84 (d, J = 7.9 Hz, 1H), 7.80 (d, J = 6.1 Hz, 2H), 7.59-7.57 (m, 2H), 4.34 (d, J =18.3 Hz, 1H), 4.29 (d, J =18.3 Hz, 1H), 3.50 (m, 5H), 2.56 (s, 3H), 2.33 (m, 1H), 1.07 (d, J = 6.7 Hz, 6H); M/Z=[M+1]: 552.75 |
| 67 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(二甲基(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.01-8.03 (m, 1H), 7.49-7.52 (m, 4H), 7.43 (t, J = 1.8 Hz, 1H), 4.09 (d, J = 17.1 Hz, 1H), 3.70 (d, J = 17.1 Hz, 1H), 3.40 (s, 6H), 2.63 (s, 3H); M/Z=[M+1]: 492.85 |
| 68 | N-((2-氰丙烷-2-基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.01 (d, J = 8.1 Hz, 1H), 7.49-7.54 (m, 4H), 7.41-7.43 (m, 1H), 4.09 (d, J = 17.1 Hz, 1H), 3.66-3.72 (m, 4H), 2.65 (s, 3H), 1.94 (s, 3H), 1.91 (s, 3H); M/Z=[M+1]: 546.05 |
| 69 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(苯基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.10 (d, J = 8.3 Hz, 1H), 8.04-8.06 (m, 2H), 7.69-7.73 (m, 1H), 7.62-7.65 (m, 2H), 7.53 (dd, J = 10.5, 1.7 Hz, 3H), 7.48 (s, 1H), 7.43 (t, J = 1.8 Hz, 1H), 4.09 (d, J = 17.1 Hz, 1H), 3.71 (d, J = 17.4 Hz, 1H), 3.45 (s, 3H), 2.62 (s, 3H); M/Z=[M+1]: 555.00 |
| 70 | N-(叔丁基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.98 (d, J = 8.1 Hz, 1H), 7.59 (d, J = 6.1 Hz, 2H), 7.50 (d, J = 8.1 Hz, 1H), 7.46 (s, 1H), 4.09 (d, J = 17.1 Hz, 1H), 3.69 (d, J = 17.1 Hz, 1H), 3.40 (s, 3H), 2.64 (s, 3H), 1.56 (s, 9H); M/Z=[M+1]: 553.05 |
| 71 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-(三氟甲基)苯基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.32-8.36 (m, 2H), 8.16 (d, J = 7.8 Hz, 1H), 7.96 (dd, J = 7.9, 5.7 Hz, 2H), 7.80 (t, J = 1.8 Hz, 1H), 7.59-7.63 (m, 4H), 4.38 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.70 (s, 3H), 2.45 (s, 3H); M/Z=[M+1]: 623.00 |
| 72 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(4-(三氟甲氧基)苯基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.15-8.18 (m, 2H), 7.95 (d, J = 8.1 Hz, 1H), 7.80 (t, J = 2.0 Hz, 1H), 7.70 (d, J = 8.1 Hz, 2H), 7.58-7.64 (m, 4H), 4.37 (d, J = 18.6 Hz, 1H), 4.28 (d, J = 18.6 Hz, 1H), 3.65 (s, 3H), 2.46 (s, 3H); M/Z=[M+1]: 638.95 |
| 73 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異丁基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.83 (d, J = 8.3 Hz, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.62 (d, J = 1.5 Hz, 2H), 7.58-7.60 (m, 2H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.62-3.67 (m, 2H), 3.52 (dd, J = 14.4, 6.4 Hz, 1H), 3.41 (dd, J = 14.2, 6.6 Hz, 1H), 2.51 (s, 3H), 2.30-2.36 (m, 1H), 1.30 (t, J = 7.3 Hz, 3H), 1.07 (d, J = 6.7 Hz, 6H); M/Z=[M+1]: 559.00 |
| 74 | 2-(4-(N-(4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯)-S-甲基磺醯亞胺基)苯基)乙酸甲酯 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.94-8.00 (m, 3H), 7.80 (d, J = 6.1 Hz, 2H), 7.57-7.61 (m, 4H), 4.37 (d, J = 18.3 Hz, 1H), 4.30 (d, J = 18.6 Hz, 1H), 3.86 (s, 2H), 3.63 (s, 3H), 3.59 (s, 3H), 2.46 (s, 3H); M/Z=[M+1]: 645.05 |
| 75 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(4-(三氟甲氧基)苯基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.15-8.19 (m, 2H), 7.96 (d, J = 8.1 Hz, 1H), 7.80 (d, J = 6.1 Hz, 2H), 7.71 (d, J = 8.3 Hz, 2H), 7.61 (d, J = 8.1 Hz, 1H), 7.57 (s, 1H), 4.37 (d, J = 18.3 Hz, 1H), 4.30 (d, J = 18.3 Hz, 1H), 3.65 (s, 3H), 2.47 (s, 3H); M/Z=[M+1]: 657.00 |
| 76 | N-((2-氰丙烷-2-基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.02 (d, J = 8.1 Hz, 1H), 7.59 (d, J = 5.9 Hz, 2H), 7.50-7.53 (m, 2H), 4.09 (d, J = 17.1 Hz, 1H), 3.67-3.71 (m, 4H), 2.65 (s, 3H), 1.94 (s, 3H), 1.92 (s, 3H); M/Z=[M+1]: 564.10 |
| 77 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(二乙基(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.01 (d, J = 8.6 Hz, 1H), 7.48-7.52 (m, 4H), 7.42 (t, J = 1.8 Hz, 1H), 4.09 (d, J = 17.1 Hz, 1H), 3.70 (d, J = 17.4 Hz, 1H), 3.58 (dt, J = 21.4, 7.5 Hz, 2H), 3.46 (dt, J = 21.4, 7.4 Hz, 2H), 2.62 (s, 3H), 1.45-1.50 (m, 6H); M/Z=[M+1]: 521.10 |
| 78 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(丙基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.86 (d, J = 8.3 Hz, 1H), 7.83 (t, J = 1.8 Hz, 1H), 7.64 (d, J = 1.7 Hz, 2H), 7.61 (d, J = 7.6 Hz, 2H), 4.36 (s, J = 18.6 Hz, 1H), 4.27 (s, J = 18.6 Hz, 1H), 3.52-3.62 (m, 2H), 3.44 (s, 3H), 2.54 (s, 3H), 1.79-1.87 (m, 2H), 1.05 (t, J = 7.5 Hz, 3H); M/Z=[M+1]: 521.05 |
| 79 | N-(烯丙基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.01 (d, J = 8.3 Hz, 1H), 7.49-7.52 (m, 4H), 7.42 (t, J = 2.0 Hz, 1H), 5.93-6.03 (m, 1H), 5.56-5.62 (m, 2H), 4.36 (dd, J = 13.9, 7.5 Hz, 1H), 4.21 (dd, J = 13.9, 7.5 Hz, 1H), 4.09 (d, J = 17.1 Hz, 1H), 3.70 (d, J = 17.4 Hz, 1H), 3.24 (s, 3H), 2.61 (s, 3H); M/Z=[M+1]: 519.00 |
| 80 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異戊基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.83 (d, J = 7.9 Hz, 1H), 7.80 (d, J = 6.4 Hz, 2H), 7.58 (m, 2H), 4.36 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.3 Hz, 1H), 3.52-3.64 (m, 4H), 2.52 (s, 3H), 1.58-1.73 (m, 3H), 1.31 (t, J = 7.3 Hz, 3H), 0.89 (d, J= 7.2 Hz, 6H); M/Z=[M+1]: 580.80 |
| 81 | N-(環己基(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.85 (d, J = 8.1 Hz, 1H), 7.82 (d, J = 6.4 Hz, 2H), 7.60 (d, J = 9.5 Hz, 2H), 4.35 (d, J = 18.5 Hz, 1H), 4.28 (d, J = 18.5 Hz, 1H), 3.58-3.73 (m, 3H), 2.50 (s, 3H), 2.15 (t, J = 14.8 Hz, 2H), 1.87 (d, J = 12.7 Hz, 2H), 1.68 (d, J = 12.7 Hz, 1H), 1.48-1.62 (m, 2H), 1.27-1.41 (m, 5H), 1.13-1.25 (m, 1H); M/Z=[M+1]: 592.80 |
| 82 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異戊基(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.83 (d, J = 7.9 Hz, 1H), 7.80 (d, J = 6.1 Hz, 2H), 7.58 (m, 2H), 4.36 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.3 Hz, 1H), 3.58 (m, 2H), 3.44 (s, 3H), 2.51 (s, 3H), 1.61-1.75 (m, 3H), 0.91 (d, J = 5.5 Hz, 6H); M/Z=[M+1]: 566.80 |
| 83 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-(三氟甲基)苯基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.32-8.36 (m, 2H), 8.17 (d, J = 7.9 Hz, 1H), 7.94-7.98 (m, 2H), 7.80 (d, J = 6.4 Hz, 2H), 7.61 (d, J = 8.3 Hz, 1H), 7.58 (s, 1H), 4.37 (d, J = 18.3 Hz, 1H), 4.30 (d, J = 18.3 Hz, 1H), 3.70 (s, 3H), 2.45 (s, 3H); M/Z=[M+1]: 641.10 |
| 84 | 2-(4-(N-(4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯)-S-甲基磺醯亞胺基)苯基)乙酸甲酯 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.98 (m, 3H), 7.82 (t, J = 1.8 Hz, 1H), 7.60-7.64 (m, 6H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.86 (s, 2H), 3.63 (s, 3H), 3.57 (s, 3H), 2.47 (s, 3H); M/Z=[M+1]: 627.10 |
| 85 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異丁基(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.86 (d, J = 8.3 Hz, 1H), 7.83 (t, J = 2.0 Hz, 1H), 7.59-7.64 (m, 4H), 4.36 (d, J = 18.6 Hz, 1H), 4.27 (d, J = 18.6 Hz, 1H), 3.52 (m, 5H), 2.54 (s, 3H), 2.31-2.41 (m, 1H), 1.07 (d, J= 7.2 Hz, 6H); M/Z=[M+1]: 534.75 |
| 86 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.10 (d, J = 8.3 Hz, 1H), 7.84 (dq, J = 7.9, 0.9 Hz, 1H), 7.76 (dt, J = 7.8, 2.2 Hz, 1H), 7.63 (td, J = 8.1, 5.1 Hz, 1H), 7.52-7.55 (m, 2H), 7.48 (s, 1H), 7.38-7.43 (m, 2H), 4.09 (d, J = 17.4 Hz, 1H), 3.71 (d, J = 16.9 Hz, 1H), 3.45 (s, 3H), 2.61 (s, 3H); ESI MS (m/z): 573.00 (M+H) ; M/Z = 573.00 (M+H) |
| 87 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(氧二苯基-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.21 (d, J = 8.1 Hz, 1H), 8.04-8.06 (m, 4H), 7.52-7.62 (m, 9H), 7.48 (s, 1H), 7.43 (t, J = 1.8 Hz, 1H), 4.10 (d, J = 17.4 Hz, 1H), 3.72 (d, J = 17.4 Hz, 1H), 2.63 (s, 3H); M/Z=[M+1]: 617.10 |
| 88 | N-((3-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.10 (d, J = 8.1 Hz, 1H), 8.02 (t, J = 2.0 Hz, 1H), 7.92 (dq, J = 7.9, 1.0 Hz, 1H), 7.66-7.68 (m, 1H), 7.53-7.60 (m, 2H), 7.52 (d, J = 1.5 Hz, 2H), 7.49 (s, 1H), 7.43 (t, J = 1.8 Hz, 1H), 4.09 (d, J = 17.4 Hz, 1H), 3.71 (d, J = 17.4 Hz, 1H), 3.43 (s, 3H), 2.61 (s, 3H); M/Z=[M+1]: 589.05 |
| 89 | N-((4-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.09 (d, J = 8.3 Hz, 1H), 7.88-7.93 (m, 2H), 7.75-7.79 (m, 2H), 7.59 (d, J = 6.1 Hz, 2H), 7.53 (dd, J = 8.1, 1.2 Hz, 1H), 7.47 (s, 1H), 4.09 (d, J = 17.4 Hz, 1H), 3.69 (d, J = 17.1 Hz, 1H), 3.43 (s, 3H), 2.60 (s, 3H); M/Z=[M+1]: 652.90 |
| 90 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.17 (td, J = 8.6, 5.7 Hz, 1H), 8.01 (d, J = 8.1 Hz, 1H), 7.59 (d, J = 6.1 Hz, 2H), 7.50-7.52 (m, 1H), 7.45 (s, 1H), 7.15-7.19 (m, 1H), 6.99-7.05 (m, 1H), 4.08 (d, J = 17.4 Hz, 1H), 3.68 (d, J = 17.1 Hz, 1H), 3.51 (s, 3H), 2.56 (s, 3H); M/Z=[M+1]: 609.00 |
| 91 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(2-甲氧基乙基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.85 (d, J = 7.8 Hz, 1H), 7.80 (d, J = 6.1 Hz, 2H), 7.58 (m, 2H), 4.36 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.73-3.97 (m, 4H), 3.49-3.59 (m, 2H), 3.28 (s, 3H), 2.53 (s, 3H), 1.32 (t, J = 7.3 Hz, 3H); M/Z=[M+1]: 569.05 |
| 92 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧負離子基-1l6-硫雜環丁烷基-1-基亞基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.91 (d, J = 8.6 Hz, 1H), 7.80 (d, J = 6.1 Hz, 2H), 7.60 (m, 2H), 4.28-4.52 (m, 6H), 2.54 (s, 3H), 2.27-2.44 (m, 2H); M/Z=[M+1]: 522.95 |
| 93 | N-((2-氰丙烷-2-基)(氧代)(丙基)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.02 (d, J = 8.1 Hz, 1H), 7.59 (d, J = 6.1 Hz, 2H), 7.50-7.52 (m, 2H), 4.12 (d, J = 17.4 Hz, 1H), 3.82-3.90 (m, 1H), 3.72-3.80 (m, 1H), 3.69 (d, J = 17.4 Hz, 1H), 2.64 (s, 3H), 2.14-2.25 (m, 1H), 2.01-2.12 (m, 1H), 1.92 (s, 3H), 1.90 (s, 3H), 1.16 (t, J = 7.5 Hz, 3H); M/Z=[M+1]: 592.10 |
| 94 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(氧代)(丙基)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.83 (d, J = 8.3 Hz, 1H), 7.81 (t, J = 1.8 Hz, 1H), 7.62 (d, J = 1.8 Hz, 2H), 7.59 (d, J = 7.3 Hz, 2H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.6 Hz, 1H), 3.48-3.64 (m, 4H), 2.51 (s, 3H), 1.73-1.84 (m, 2H), 1.30 (t, J = 7.3 Hz, 3H), 1.02 (t, J = 7.3 Hz, 3H); M/Z=[M+1]: 534.75 |
| 95 | 甲基 3-(N-(4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯)-S-甲基磺醯亞胺基)丙酸酯 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.85 (d, J = 8.6 Hz, 1H), 7.80 (d, J = 6.1 Hz, 2H), 7.57-7.59 (m, 2H), 4.37 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.6 Hz, 1H), 3.77-3.92 (m, 2H), 3.63 (s, 3H), 3.49 (s, 3H), 2.88-2.95 (m, 2H), 2.52 (s, 3H); M/Z=[M+1]: 583.00 |
| 96 | N-((2-氰基乙基)(4-乙基苯基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.07 (d, J = 8.1 Hz, 1H), 7.91 (d, J = 8.3 Hz, 2H), 7.80 (d, J = 6.1 Hz, 2H), 7.55-7.62 (m, 4H), 4.38 (d, J = 18.3 Hz, 1H), 4.30 (d, J = 18.3 Hz, 1H), 4.08-4.15 (m, 1H), 3.98-4.05 (m, 1H), 2.98 (dd, J = 13.8, 7.5 Hz, 2H), 2.73 (q, J = 7.5 Hz, 2H), 2.48 (s, 3H), 1.21 (t, J = 7.3 Hz, 3H); M/Z=[M+1]: 639.95 |
| 97 | N-((2-氰基乙基)(4-甲氧基苯基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.05 (d, J = 8.1 Hz, 1H), 7.93 (dd, J = 6.8, 2.0 Hz, 2H), 7.81 (t, J = 2.0 Hz, 1H), 7.59-7.63 (m, 4H), 7.23 (dd, J = 7.0, 2.1 Hz, 2H), 4.39 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.6 Hz, 1H), 4.14-3.98 (m, 2 H), 3.87 (s, 3H), 2.91-3.02 (m, 2H); M/Z=[M+1]: 624.20 |
| 98 | N-((2-氰基乙基)(氧代)(間甲苯基)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.14 (d, J = 8.1 Hz, 1H), 7.80-7.82 (m, 2H), 7.55 (dd, J = 7.2, 1.3 Hz, 3H), 7.50-7.52 (m, 2H), 7.50 (s, 1H), 7.43 (t, J = 1.8 Hz, 1H), 4.10 (d, J = 17.1 Hz, 1H), 3.86-3.93 (m, 1H), 3.69-3.76 (m, 2H), 3.00 (qd, J = 8.6, 6.2 Hz, 1H), 2.87 (qd, J = 8.7, 6.5 Hz, 1H), 2.62 (s, 3H), 2.47 (s, 3H); M/Z=[M+1]: 607.95 |
| 99 | N-((2-氰基乙基)(4-乙基苯基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.07 (d, J = 8.1 Hz, 1H), 7.91 (d, J = 8.6 Hz, 2H), 7.80 (t, J = 1.8 Hz, 1H), 7.59-7.62 (m, 4H), 7.56 (d, J = 8.6 Hz, 2H), 4.39 (d, J = 18.6 Hz, 1H), 4.29 (d, J = 18.8 Hz, 1H), 4.08-4.15 (m, 1H), 3.97-4.04 (m, 1H), 2.93-3.05 (m, 2H), 2.73 (q, J = 7.6 Hz, 2H), 2.48 (s, 3H), 1.21 (t, J = 7.3 Hz, 3H); M/Z=[M+1]: 622.00 |
| 100 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(對甲苯基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.08 (d, J = 8.1 Hz, 1H), 7.91 (d, J = 8.3 Hz, 2H), 7.59 (d, J = 6.1 Hz, 2H), 7.51-7.53 (m, 1H), 7.47 (s, 1H), 7.42 (d, J = 8.6 Hz, 2H), 4.07-4.13 (m, 1H), 3.69 (d, J = 17.1 Hz, 1H), 3.43 (s, 3H), 2.61 (s, 3H), 2.47 (s, 3H); 587.10 (MH; 35Cl)+, 589.10 (MH; 37Cl)+ |
| 101 | N-((4-氰基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.16 (d, J = 8.6 Hz, 2H), 8.10 (d, J = 8.1 Hz, 1H), 7.93 (d, J = 8.3 Hz, 2H), 7.59 (d, J = 5.9 Hz, 2H), 7.54 (d, J = 8.1 Hz, 1H), 7.47 (s, 1H), 4.09 (d, J = 17.1 Hz, 1H), 3.69 (d, J = 17.1 Hz, 1H), 3.44 (s, 3H), 2.59 (s, 3H); 597.90 (MH; 35Cl)+, 599.90 (MH; 37Cl)+ |
| 102 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(4-氧負離子基-1,4l6-惡噻烷-4-基亞基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.92 (d, J = 8.6 Hz, 1H), 7.80 (t, J = 2.0 Hz, 1H), 7.59-7.62 (m, 4H), 4.38 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.3 Hz, 1H), 4.13-4.18 (m, 2H), 3.91-3.96 (m, 2H), 3.81-3.86 (m, 2H), 3.59-3.65 (m, 2H), 2.54 (s, 3H); 535.05 (MH; 35Cl)+, 537.05 (MH; 37Cl)+ |
| 103 | N-((4-氰基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.20 (dd, J = 13.0, 8.8 Hz, 4H), 7.97 (d, J = 8.1 Hz, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.58-7.62 (m, 4H), 4.38 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.6 Hz, 1H), 3.66 (s, 3H), 2.45 (s, 3H); 577.80 (MH; 35Cl)+, 579.80 (MH; 37Cl)+ |
| 104 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(4-((4-(三氟甲基)吡啶-2-基)氧基)苯基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.45 (d, J = 5.4 Hz, 1H), 8.08-8.11 (m, 2H), 7.97 (d, J = 8.1 Hz, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.61-7.64 (m, 4H), 7.58 (d, J = 5.1 Hz, 2H), 7.52 (dd, J = 6.8, 2.0 Hz, 2H), 4.38 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.3 Hz, 1H), 3.64 (s, 3H), 2.50 (s, 3H).; 715.95 (MH; 35Cl)+, 717.95 (MH; 37Cl)+ |
| 105 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4,5-二甲基噻唑-2-基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.94 (d, J = 8.1 Hz, 1H), 7.81 (t, J = 2.0 Hz, 1H), 7.61-7.64 (m, 4H), 4.39 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.3 Hz, 1H), 3.72 (s, 3H), 2.51 (s, 3H), 2.48 (s, 3H), 2.36 (s, 3H); 589.70 (MH; 35Cl)+, 591.70 (MH; 37Cl)+ |
| 106 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(3-氟苯基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.98 (d, J = 8.3 Hz, 1H), 7.80-7.84 (m, 3H), 7.77 (td, J = 8.1, 5.5 Hz, 1H), 7.62-7.68 (m, 4H), 7.59 (s, 1H), 4.38 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.3 Hz, 1H), 3.70-3.82 (m, 2H), 2.47 (s, 3H), 1.17 (t, J = 7.2 Hz, 3H); 587.00 (MH; 35Cl)+, 589.00 (MH; 37Cl)+ |
| 107 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(3-氟苯基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.98 (d, J = 8.1 Hz, 1H), 7.74-7.84 (m, 5H), 7.60-7.68 (m, 2H), 7.58 (s, 1H), 4.37 (d, J = 18.3 Hz, 1H), 4.30 (d, J = 18.3 Hz, 1H), 3.71-3.82 (m, 2H), 2.47 (s, 3H), 1.17 (t, J = 7.2 Hz, 3H); 604.75 (MH; 35Cl)+, 606.75 (MH; 37Cl)+ |
| 108 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(氧代)(間甲苯基)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.95 (d, J = 8.1 Hz, 1H), 7.81 (t, J = 2.0 Hz, 1H), 7.74-7.78 (m, 2H), 7.62 (dd, J = 5.0, 1.6 Hz, 3H), 7.58 (d, J = 4.9 Hz, 3H), 4.38 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.3 Hz, 1H), 3.61-3.76 (m, 2H), 2.47 (s, 3H), 2.43 (s, 3H), 1.14 (t, J = 7.2 Hz, 3H); 582.75 (MH; 35Cl)+, 584.75 (MH; 37Cl)+ |
| 109 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(氧代)(間甲苯基)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.95 (d, J = 8.1 Hz, 1H), 7.76-7.81 (m, 4H), 7.57-7.62 (m, 4H), 4.37 (d, J = 18.3 Hz, 1H), 4.30 (d, J = 17.9 Hz, 1H), 3.65-3.74 (m, 2H), 2.47 (s, 3H), 2.43 (s, 3H), 1.14 (t, J = 7.3 Hz, 3H); 601.05 (MH; 35Cl)+, 603.05 (MH; 37Cl)+ |
| 110 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(4-((4-(三氟甲基)吡啶-2-基)氧基)苯基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.44 (d, J = 5.1 Hz, 1H), 8.09 (dd, J = 6.8, 2.0 Hz, 2H), 7.97 (d, J = 8.3 Hz, 1H), 7.80 (d, J = 6.1 Hz, 2H), 7.58-7.64 (m, 4H), 7.51-7.54 (m, 2H), 4.37 (d, J = 18.3 Hz, 1H), 4.30 (d, J = 18.6 Hz, 1H), 3.64 (s, 3H), 2.50 (d, J = 1.7 Hz, 3H); 734.05 (MH; 35Cl)+, 736.05 (MH; 37Cl)+ |
| 111 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.94 (d, J = 8.1 Hz, 1H), 7.88 (d, J = 8.3 Hz, 1H), 7.81 (d, J = 2.0 Hz, 1H), 7.58-7.62 (m, 4H), 7.31 (t, J = 8.3 Hz, 2H), 4.38 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.53 (s, 3H), 2.56 (s, 3H), 2.46 (s, 3H), 2.36 (s, 3H); 583.10 (MH; 35Cl)+, 585.10 (MH; 37Cl)+ |
| 112 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.94 (d, J = 8.1 Hz, 1H), 7.88 (d, J = 8.1 Hz, 1H), 7.80 (d, J = 6.4 Hz, 2H), 7.60 (d, J = 8.1 Hz, 1H), 7.57 (s, 1H), 7.32 (d, J = 8.3 Hz, 1H), 7.29 (s, 1H), 4.37 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.6 Hz, 1H), 3.53 (s, 3H), 2.56 (s, 3H), 2.46 (s, 3H), 2.36 (s, 3H); 601.10 (MH; 35Cl)+, 603.10 (MH; 37Cl)+ |
| 113 | N-((4-氰基苯基)(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.19 (d, J = 8.6 Hz, 2H), 8.14-8.17 (m, 2H), 7.99 (d, J = 8.1 Hz, 1H), 7.80 (d, J = 6.4 Hz, 2H), 7.61 (d, J = 8.1 Hz, 1H), 7.58 (s, 1H), 4.37 (d, J = 18.3 Hz, 1H), 4.30 (d, J = 18.6 Hz, 1H), 3.78 (qd, J = 14.3, 7.3 Hz, 2H), 2.46 (s, 3H), 1.16-1.19 (m, 3H); 611.95 (MH; 35Cl)+, 613.95 (MH; 37Cl)+ |
| 114 | N-((4-氰基苯基)(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.14-8.20 (m, 4H), 7.99 (d, J = 7.9 Hz, 1H), 7.81 (t, J = 1.8 Hz, 1H), 7.59-7.63 (m, 4H), 4.38 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.3 Hz, 1H), 3.78 (qd, J = 14.4, 7.3 Hz, 2H), 2.46 (s, 3H), 1.17 (t, J = 7.3 Hz, 3H); 594.00 (MH; 35Cl)+, 596.00 (MH; 37Cl)+ |
| 115 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二甲基苯基)(乙基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.96 (d, J = 8.1 Hz, 1H), 7.83 (d, J = 8.1 Hz, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.61-7.62 (m, 3H), 7.58 (s, 1H), 7.32 (d, J = 8.3 Hz, 1H), 7.29 (s, 1H), 4.38 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.69 (td, J = 14.5, 7.4 Hz, 1H), 3.52-3.60 (m, 1H), 2.53 (s, 3H), 2.47 (s, 3H), 2.36 (s, 3H), 1.16 (t, J = 7.3 Hz, 3H); 597.10 (MH; 35Cl)+, 599.10 (MH; 37Cl)+ |
| 116 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4,5-二甲基噻唑-2-基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.95 (d, J = 8.1 Hz, 1H), 7.79 (t, J = 6.2 Hz, 2H), 7.62 (d, J = 8.3 Hz, 1H), 7.60 (s, 1H), 4.38 (d, J = 18.6 Hz, 1H), 4.30 (d, J = 18.6 Hz, 1H), 3.72 (s, 3H), 2.51 (s, 3H), 2.48 (s, 3H), 2.36 (s, 3H); 605.95 (MH; 35Cl)+, 607.95 (MH; 37Cl)+ |
| 117 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.18 (d, J = 8.6 Hz, 2H), 7.69 (d, J = 8.6 Hz, 2H), 7.51 (s, 2H), 7.42 (t, J = 1.8 Hz, 1H), 7.35 (t, J = 7.6 Hz, 1H), 7.19 (d, J = 7.6 Hz, 2H), 4.08-4.13 (m, 1H), 3.71 (d, J = 17.4 Hz, 1H), 3.46 (s, 3H), 2.74 (s, 6H); 569.05 (MH; 35Cl)+, 571.05 (MH; 37Cl)+ |
| 118 | N-((4-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.19 (d, J = 8.6 Hz, 2H), 7.91 (d, J = 8.8 Hz, 2H), 7.77 (d, J = 8.3 Hz, 2H), 7.70 (d, J = 8.6 Hz, 2H), 7.59 (d, J = 5.9 Hz, 2H), 4.11 (d, J = 17.4 Hz, 1H), 3.71 (d, J = 17.4 Hz, 1H), 3.47 (s, 3H); 638.35 (MH; 35Cl)+, 640.35 (MH; 37Cl)+ |
| 119 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.21 (d, J = 8.6 Hz, 2H), 7.70 (d, J = 8.6 Hz, 2H), 7.63 (s, 2H), 7.59 (d, J = 5.9 Hz, 2H), 7.30 (s, 1H), 4.12 (d, J = 17.1 Hz, 1H), 3.71 (d, J = 17.4 Hz, 1H), 3.44 (s, 3H), 2.42 (s, 6H); 587.00 (MH; 35Cl)+, 589.00 (MH; 37Cl)+ |
| 120 | N-((4-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.19 (d, J = 8.6 Hz, 2H), 7.91 (d, J = 8.8 Hz, 2H), 7.77 (d, J = 8.3 Hz, 2H), 7.71 (d, J = 8.6 Hz, 2H), 7.52 (d, J = 1.7 Hz, 2H), 7.43 (t, J = 1.8 Hz, 1H), 4.11 (d, J = 17.4 Hz, 1H), 3.72 (d, J = 17.4 Hz, 1H), 3.47 (s, 3H); 620.95 (MH; 35Cl)+, 622.95 (MH; 37Cl)+ |
| 121 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(甲基(氧代)(苯基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.21 (dd, J = 6.8, 2.0 Hz, 2H), 8.05-8.07 (m, 2H), 7.70-7.73 (m, 3H), 7.64 (dd, J = 7.9, 7.5 Hz, 2H), 7.52 (d, J = 1.5 Hz, 2H), 7.43 (t, J = 1.8 Hz, 1H), 4.11 (d, J = 17.4 Hz, 1H), 3.72 (d, J = 17.4 Hz, 1H), 3.49 (s, 3H); 541.05 (MH; 35Cl)+, 543.05 (MH; 37Cl)+ |
| 122 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(甲基(氧代)(間甲苯基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.21 (d, J = 8.6 Hz, 2H), 7.84 (d, J = 3.7 Hz, 2H), 7.70 (d, J = 8.6 Hz, 2H), 7.59 (d, J = 6.1 Hz, 2H), 7.50 (d, J = 5.4 Hz, 2H), 4.11 (d, J = 17.1 Hz, 1H), 3.71 (d, J = 17.6 Hz, 1H), 3.47 (s, 3H), 2.48 (s, 3H); 573.10 (MH; 35Cl)+, 575.10 (MH; 37Cl)+ |
| 123 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(甲基(氧代)(對甲苯基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.09 (d, J = 8.6 Hz, 2H), 7.91 (d, J = 7.8 Hz, 2H), 7.72-7.82 (m, 4H), 7.46-7.50 (m, 2H),4.39 (d, J = 18.3 Hz, 1H), 4.32 (d, J = 18.3 Hz, 1H), 3.60 (s, 3H), 2.42 (s, 3H); 573.35 (MH; 35Cl)+, 575.35 (MH; 37Cl)+ |
| 124 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.16-8.23 (m, 3H), 7.70-7.72 (m, 2H), 7.54 (t, J = 1.7 Hz, 2H), 7.45 (t, J = 1.8 Hz, 1H), 7.17-7.21 (m, 1H), 7.01-7.06 (m, 1H), 4.12 (d, J = 17.1 Hz, 1H), 3.73 (d, J = 17.1 Hz, 1H), 3.58 (s, 3H); 577.20 (M-H)+ |
| 125 | N-((4-氰基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.14-8.18 (m, 4H), 7.91-7.96 (m, 2H), 7.71 (dd, J = 6.7, 1.8 Hz, 2H), 7.52-7.60 (m, 2H), 4.09-4.15 (m, 1H), 3.69-3.73 (m, 1H), 3.48 (s, 3H); 584.00 (MH; 35Cl)+, 586.00 (MH; 37Cl)+ |
| 126 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-甲氧基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.13-8.18 (m, 3H), 7.63-7.69 (m, 3H), 7.52-7.60 (m, 2H), 7.21 (t, J = 7.3 Hz, 1H), 7.07 (d, J = 8.3 Hz, 1H), 4.08-4.13 (m, 1H), 3.91 (s, 3H), 3.70 (d, J = 17.4 Hz, 1H), 3.59 (d, J = 0.5 Hz, 3H); 589.05 (MH; 35Cl)+, 591.05 (MH; 37Cl)+ |
| 127 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(氧二苯基-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.28 (d, J = 8.6 Hz, 2H), 8.05-8.07 (m, 4H), 7.73 (d, J = 8.6 Hz, 2H), 7.54-7.63 (m, 8H), 4.12 (d, J = 17.4 Hz, 1H), 3.72 (d, J = 17.1 Hz, 1H); 621.10.05 (MH; 35Cl)+, 623.10 (MH; 37Cl)+ |
| 128 | N-((2-氰丙烷-2-基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.14 (d, J = 8.8 Hz, 2H), 7.71 (d, J = 8.6 Hz, 2H), 7.59 (d, J = 6.1 Hz, 2H), 4.11 (d, J = 17.1 Hz, 1H), 3.68-3.73 (m, 4H), 1.97 (s, 3H), 1.94 (s, 3H); 547.90 (M-H; 35Cl)+, 549.90 (M-H; 37Cl)+ |
| 129 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.18 (dd, J = 6.8, 2.0 Hz, 2H), 7.68 (dd, J = 6.7, 1.8 Hz, 2H), 7.52-7.59 (m, 2H), 7.35 (t, J = 7.6 Hz, 1H), 7.19 (d, J = 7.8 Hz, 2H), 4.08-4.13 (m, 1H), 3.70 (d, J = 17.4 Hz, 1H), 3.46 (s, 3H), 2.74 (s, 6H); 587.05 (MH; 35Cl)+, 589.05 (MH; 37Cl)+ |
| 130 | N-((2-氰丙烷-2-基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.14 (dd, J = 6.8, 2.0 Hz, 2H), 7.71 (dd, J = 6.7, 1.8 Hz, 2H), 7.52 (s, 2H), 7.43 (t, J = 1.8 Hz, 1H), 4.11 (d, J = 17.4 Hz, 1H), 3.68-3.74 (m, 4H), 1.97 (s, 3H), 1.94 (s, 3H); 532.05 (MH; 35Cl)+, 534.05 (MH; 37Cl)+ |
| 131 | N-((3-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.20 (d, J = 8.6 Hz, 2H), 8.03 (t, J = 1.8 Hz, 1H), 7.93 (d, J = 7.8 Hz, 1H), 7.69 (dd, J = 14.4, 8.3 Hz, 3H), 7.56-7.60 (m, 3H), 4.12 (d, J = 17.1 Hz, 1H), 3.72 (d, J = 17.4 Hz, 1H), 3.48 (s, 3H); 592.90 (MH; 35Cl)+, 594.90 (MH; 37Cl)+ |
| 132 | N-((2-氯代-6-甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.16 (d, J = 8.6 Hz, 2H), 7.68 (d, J = 8.7 Hz, 2H), 7.51 (s, 2H), 7.42 (t, J = 1.8 Hz, 1H), 7.38 (t, J = 2.9 Hz, 2H), 7.31 (q, J = 3.0 Hz, 1H), 4.09 (d, J = 16.6 Hz, 1H), 3.71 (d, J = 17.1 Hz, 1H), 3.64 (s, 3H), 2.89 (s, 3H); 589.00 (MH; 35Cl)+, 591.00 (MH; 37Cl)+ |
| 133 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(甲基(氧代)(苯基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.21 (d, J = 8.6 Hz, 2H), 8.05-8.07 (m, 2H), 7.71 (t, J = 8.2 Hz, 3H), 7.59-7.66 (m, 4H), 4.11 (d, J = 18.1 Hz, 1H), 3.71 (d, J = 17.4 Hz, 1H), 3.49 (s, 3H); 559.05 (MH; 35Cl)+, 561.05 (MH; 37Cl)+ |
| 134 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.21-8.23 (m, 2H), 7.87 (d, J = 7.8 Hz, 1H), 7.79 (dd, J = 7.8, 2.2 Hz, 1H), 7.73 (d, J = 8.8 Hz, 2H), 7.64-7.68 (m, 1H), 7.60-7.63 (m, 2H), 7.43 (td, J = 8.2, 2.5 Hz, 1H), 4.14 (t, J = 8.6 Hz, 1H), 3.74 (d, J = 17.4 Hz, 1H), 3.51 (s, 3H); 577.00 (MH; 35Cl)+, 579.00 (MH; 37Cl)+ |
| 135 | N-((2-氯代-6-甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.16 (dd, J = 6.8, 2.0 Hz, 2H), 7.68 (dd, J = 6.7, 1.8 Hz, 2H), 7.52-7.59 (m, 2H), 7.37-7.41 (m, 2H), 7.29-7.33 (m, 1H), 4.08-4.15 (m, 1H), 3.70 (d, J = 17.1 Hz, 1H), 3.64 (s, 3H), 2.89 (s, 3H); 608.95 (MH)+ |
| 136 | N-(叔丁基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.12-8.16 (m, 2H), 7.69 (dt, J = 8.6, 1.8 Hz, 2H), 7.52 (d, J = 1.7 Hz, 2H), 7.43 (t, J = 1.8 Hz, 1H), 4.08-4.15 (m, 1H), 3.72 (d, J = 17.1 Hz, 1H), 3.41 (d, J = 0.5 Hz, 3H), 1.59 (s, 9H); 521.05 (MH; 35Cl)+, 523.05 (MH; 37Cl)+ |
| 137 | N-((2-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.33 (dd, J = 7.7, 1.8 Hz, 1H), 8.17 (d, J = 8.6 Hz, 2H), 7.68 (d, J = 8.6 Hz, 2H), 7.55-7.63 (m, 5H), 4.08-4.13 (m, 1H), 3.70 (d, J = 17.4 Hz, 1H), 3.59 (s, 3H); 595.00 (MH; 35Cl)+, 597.00 (MH; 37Cl)+ |
| 138 | N-((2-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.33 (dd, J = 7.6, 2.0 Hz, 1H), 8.17 (d, J = 8.8 Hz, 2H), 7.69 (d, J = 8.6 Hz, 2H), 7.55-7.63 (m, 3H), 7.51 (s, 2H), 7.42 (t, J = 1.8 Hz, 1H), 4.10 (d, J = 17.1 Hz, 1H), 3.71 (d, J = 17.1 Hz, 1H), 3.59 (s, 3H); 574.90 (MH; 35Cl)+, 576.90 (MH; 37Cl)+ |
| 139 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.18 (dd, J = 6.7, 1.8 Hz, 2H), 7.72 (dd, J = 6.8, 2.0 Hz, 2H), 7.58-7.60 (m, 2H), 7.52 (d, J = 1.5 Hz, 2H), 7.43 (t, J = 1.8 Hz, 1H), 7.15 (td, J = 8.3, 2.0 Hz, 1H), 4.11 (d, J = 17.1 Hz, 1H), 3.72 (d, J = 17.1 Hz, 1H), 3.47 (s, 3H); 576.95 (MH; 35Cl)+, 578.95 (MH; 37Cl)+ |
| 140 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(1-氧化四氫-2H-1l6-噻喃-1-基亞基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.18 (d, J = 8.6 Hz, 2H), 7.69 (d, J = 8.8 Hz, 2H), 7.52 (d, J = 1.0 Hz, 2H), 7.43 (t, J = 1.8 Hz, 1H), 4.09-4.13 (m, 1H), 3.82 (d, J = 12.2 Hz, 2H), 3.72 (d, J = 17.1 Hz, 1H), 3.27-3.33 (m, 2H), 2.23 (s, 2H), 2.12 (d, J = 18.6 Hz, 2H), 1.73-1.76 (m, 2H); 518.70 (MH; 35Cl)+, 520.70 (MH; 37Cl)+ |
| 141 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(氧二苯基-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.28 (d, J = 8.6 Hz, 2H), 8.05-8.07 (m, 4H), 7.73 (d, J = 8.6 Hz, 2H), 7.52-7.63 (m, 8H), 7.43 (t, J = 2.0 Hz, 1H), 4.12 (d, J = 17.4 Hz, 1H), 3.73 (d, J = 17.6 Hz, 1H); 602.75 (MH; 35Cl)+, 604.75 (MH; 37Cl)+ |
| 142 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-甲氧基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.16-8.18 (m, 2H), 8.14 (dd, J = 8.1, 1.7 Hz, 1H), 7.68 (d, J = 8.8 Hz, 2H), 7.64 (d, J = 6.8 Hz, 1H), 7.51 (d, J = 1.7 Hz, 2H), 7.42 (t, J = 1.8 Hz, 1H), 7.21 (t, J = 7.7 Hz, 1H), 7.07 (d, J = 8.3 Hz, 1H), 4.10 (d, J = 17.1 Hz, 1H), 3.91 (s, 3H), 3.71 (d, J = 17.4 Hz, 1H), 3.59 (d, J = 0.5 Hz, 3H); 570.75 (MH; 35Cl)+, 572.75 (MH; 37Cl)+ |
| 143 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.20-8.24 (m, 2H), 7.71 (dd, J = 6.7, 1.8 Hz, 2H), 7.63 (s, 2H), 7.52 (d, J = 1.7 Hz, 2H), 7.43 (t, J = 1.8 Hz, 1H), 7.30 (d, J = 0.7 Hz, 1H), 4.09-4.15 (m, 1H), 3.72 (d, J = 17.4 Hz, 1H), 3.43 (d, J = 9.5 Hz, 3H), 2.42 (s, 6H); 569.05 (MH; 35Cl)+, 571.05 (MH; 37Cl)+ |
| 144 | N-((3-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.20 (d, J = 8.8 Hz, 2H), 8.03 (t, J = 2.0 Hz, 1H), 7.93 (d, J = 7.8 Hz, 1H), 7.71 (d, J = 8.6 Hz, 2H), 7.67 (d, J = 8.1 Hz, 1H), 7.58 (t, J = 7.9 Hz, 1H), 7.52 (s, 2H), 7.43 (t, J = 1.8 Hz, 1H), 4.11 (d, J = 17.4 Hz, 1H), 3.72 (d, J = 17.4 Hz, 1H), 3.48 (s, 3H); 577.00 (MH; 35Cl)+, 579.00 (MH; 37Cl)+ |
| 145 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.18 (dd, J = 6.7, 1.8 Hz, 2H), 7.72 (dd, J = 6.7, 1.8 Hz, 2H), 7.59-7.61 (m, 4H), 7.13-7.17 (m, 1H), 4.09-4.14 (m, 1H), 3.72 (d, J = 17.1 Hz, 1H), 3.47 (s, 3H); 594.90 (MH; 35Cl)+, 596.90 (MH; 37Cl)+ |
| 146 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(1-氧化四氫-2H-1l6-噻喃-1-基亞基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.18 (d, J = 8.8 Hz, 2H), 7.52-7.70 (m, 4H), 4.11 (d, J = 17.4 Hz, 1H), 3.77-3.83 (m, 2H), 3.71 (d, J = 17.4 Hz, 1H), 3.27-3.33 (m, 2H), 2.18-2.24 (m, 2H), 2.15 (d, J = 3.4 Hz, 2H), 1.72-1.75 (m, 2H); 536.95 (MH; 35Cl)+, 538.95 (MH; 37Cl)+ |
| 147 | N-((2,6-二氯苯基)(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.17 (d, J = 8.6 Hz, 2H), 7.69 (d, J = 8.6 Hz, 2H), 7.50 (d, J = 7.1 Hz, 4H), 7.39-7.43 (m, 2H), 4.10 (d, J = 17.1 Hz, 1H), 3.77-3.84 (m, 2H), 3.71 (d, J = 17.4 Hz, 1H), 1.50 (t, J = 7.5 Hz, 3H); 624.90 (MH; 35Cl)+, 627.00 (MH; 37Cl)+ |
| 148 | N-((2,6-二氯苯基)(異丙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.17 (d, J = 8.3 Hz, 2H), 7.68-7.74 (m, 2H), 7.51 (s, 2H), 7.48-7.50 (m, 2H), 7.42 (t, J = 1.8 Hz, 1H), 7.39 (ddd, J = 8.8, 7.2, 0.9 Hz, 1H), 4.05-4.15 (m, 2H), 3.71 (d, J = 17.4 Hz, 1H),1.72 (d, J = 6.6 Hz, 3H), 1.38 (d, J = 6.8 Hz, 3H); 639.00 (MH)+ |
| 149 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(甲基(氧代)(4-(三氟甲基)苯基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.19 (d, J = 8.6 Hz, 4H), 7.90 (d, J = 8.6 Hz, 2H), 7.71 (dd, J = 6.7, 1.8 Hz, 2H), 7.52 (d, J = 1.5 Hz, 2H), 7.43 (t, J = 2.0 Hz, 1H), 4.11 (d, J = 17.1 Hz, 1H), 3.66-3.74 (m, 1H), 3.49 (s, 3H); 609.10 (MH; 35Cl)+, 611.10 (MH; 37Cl)+ |
| 150 | N-((3-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.17-8.21 (m, 3H), 7.98 (d, J = 8.1 Hz, 1H), 7.83 (d, J = 8.1 Hz, 1H), 7.72 (d, J = 8.8 Hz, 2H), 7.51-7.53 (m, 3H), 7.43 (t, J = 1.8 Hz, 1H), 4.11 (d, J = 17.4 Hz, 1H), 3.72 (d, J = 17.1 Hz, 1H), 3.48 (s, 3H); 621.05 (MH; 35Cl)+, 623.05 (MH; 37Cl)+ |
| 151 | (4-溴苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.73-7.76 (m, 2H), 7.66-7.69 (m, 2H), 7.52 (d, J = 6.1 Hz, 3H), 7.40-7.43 (m, 3H), 4.18 (d, J = 15.4 Hz, 1H), 4.07 (d, J = 17, 1H), 3.94 (d, J = 15 Hz, 1H), 3.67 (d, J = 17 Hz, 1H), 3.17 (s, 3H), 2.26-2.28 (s, 3H); M/Z=[M+1]: 621.00 |
| 152 | (2-氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.18 (dd, J = 7.6, 1.5 Hz, 1H), 7.45-7.55 (m, 6H), 7.37-7.42 (m, 3H), 4.13-4.16 (m, 1H), 4.05 (dd, J = 17.2, 2.6 Hz, 1H), 3.91 (d, J = 14.9 Hz, 1H), 3.66 (d, J = 17.1 Hz, 1H), 3.37 (s, 3H), 2.28 (s, 3H); M/Z=[M+1]: 576.75 |
| 153 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(3,5-二甲基苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.57 (d, J = 7.9 Hz, 1H), 7.52 (s, 2H), 7.49 (s, 2H), 7.43 (d, J = 7.9 Hz, 3H), 7.21 (s, 1H), 4.17 (d, J = 15.3 Hz, 1H), 4.06 (dd, J = 17.1, 2.4 Hz, 1H), 3.95 (d, J = 15.3 Hz, 1H), 3.67 (d, J = 17.7 Hz, 1H), 3.13 (s, 3H), 2.36 (s, 6H), 2.29 (s, 3H); M/Z=[M+1]: 569.15 |
| 154 | (3-溴苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.99 (q, J = 2.0 Hz, 1H), 7.84 (d, J = 7.8 Hz, 1H), 7.71-7.74 (m, 1H), 7.59 (d, J = 5.9 Hz, 2H), 7.49 (d, J = 8.3 Hz, 1H), 7.39-7.44 (m, 3H), 4.20 (d, J = 15.2 Hz, 1H), 4.07 (dd, J = 17.1, 1.2 Hz, 1H), 3.99 (d, J = 15.2 Hz, 1H), 3.66 (d, J = 17.4 Hz, 1H), 3.24 (s, 3H), 2.30 (s, 3H); M/Z=[M+1]: 639.00 |
| 155 | ((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(2,6-二甲基苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.59 (d, J = 6.1 Hz, 2H), 7.47-7.52 (m, 1H), 7.39 (m, 2H), 7.33 (t, J = 7.6 Hz, 1H), 7.17 (d, J = 7.3 Hz, 2H), 4.21 (d, J = 15.2 Hz, 1H), 4.08 (dd, J = 17.1, 1.2 Hz, 1H), 3.92 (d, J = 15.2 Hz, 1H), 3.67 (d, J = 17.1 Hz, 1H), 3.30 (s, 3H), 2.70 (s, 6H), 2.28 (s, 3H); M/Z=[M+1]: 587.15 |
| 156 | (4-溴苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.77 (dd, J = 8.7, 1.1 Hz, 2H), 7.68 (dd, J = 8.7, 1.8 Hz, 2H), 7.57-7.60 (m, 2H), 7.52 (m, 1H), 7.38-7.42 (m, 2H), 4.16 (d, J = 15.2 Hz, 1H), 4.06 (dd, J = 17.1, 1.2 Hz, 1H), 3.97 (d, J = 15.2 Hz, 1H), 3.66 (d, J = 17.1 Hz, 1H), 3.23 (s, 3H), 2.28 (s, 3H); M/Z=[M+1]: 639.00 |
| 157 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(2,6-二甲基苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.51-7.53 (m, 3H), 7.40-7.44 (m, 3H), 7.32 (t, J = 7.6 Hz, 1H), 7.17 (d, J = 7.3 Hz, 2H), 4.22 (d, J = 15.4 Hz, 1H), 4.04-4.09 (d, J = 17.1 Hz, 1H), 3.90 (d, J = 15.2 Hz, 1H), 3.67 (d, J = 17.1 Hz, 1H), 3.26 (s, 3H), 2.72 (s, 6H), 2.28 (s, 3H); M/Z=[M+1]: 569.15 |
| 158 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(2,6-二氟苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.50-7.52 (m, 3H), 7.39-7.43 (m, 5H), 7.00-7.07 (m, 1H), 4.20 (d, J = 15.2 Hz, 1H), 4.06 (dd, J = 14.9 & 1.6 Hz, 1H), 3.96 (d, J = 14.9 Hz, 1H), 3.67 (d, J = 17.4 Hz, 1H), 3.16 (s, 3H), 2.29 (s, 3H); M/Z=[M+1]: 576.75 |
| 159 | (3-氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.84 (q, J = 1.9 Hz, 1H), 7.75-7.77 (m, 1H), 7.54-7.58 (m, 1H), 7.46-7.52 (m, 4H), 7.40-7.42 (m, 3H), 4.19 (d, J = 15.2 Hz, 1H), 4.07 (dd, J = 15.2 & 1.6 Hz, 1H), 3.96 (d, J = 15.2 Hz, 1H), 3.67 (d, J = 17.1 Hz, 1H), 3.16 (s, 3H), 2.27 (s, 3H); M/Z=[M+1]: 577.05 |
| 160 | (3-氯苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.85 (q, J = 1.9 Hz, 1H), 7.79 (d, J = 7.8 Hz, 1H), 7.56-7.60 (m, 3H), 7.47-7.52 (m, 2H), 7.40-7.41 (m, 2H), 4.20 (d, J = 14.9 Hz, 1H), 4.06 (dd, J = 15.2 & 1.6 Hz, 1H), 3.98 (d, J = 15.2 Hz, 1H), 3.66 (d, J = 17.1 Hz, 1H), 3.22 (s, 3H), 2.29 (s, 3H); M/Z=[M+1]: 593.05 |
| 161 | (3-溴苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.98 (q, J = 1.9 Hz, 1H), 7.81 (d, J = 7.8 Hz, 1H), 7.69-7.72 (m, 1H), 7.48-7.52 (m, 3H), 7.39-7.43 (m, 4H), 4.19 (d, J = 15.2 Hz, 1H), 4.07 (dd, J = 17.1, 3.2 Hz, 1H), 3.97 (d, J = 15.2 Hz, 1H), 3.67 (d, J = 17.1 Hz, 1H), 3.17 (s, 3H), 2.29 (s, 3H); M/Z=[M+1]: 619.00 |
| 162 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)(苯基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.92 (d, J = 7.1 Hz, 2H), 7.61-7.65 (m, 1H), 7.54-7.59 (m, 3H), 7.52 (d, J = 1.7 Hz, 2H), 7.41-7.44 (m, 3H), 4.18 (d, J = 15.2 Hz, 1H), 4.06 (dd, J = 17.1, 1.5 Hz, 1H), 3.96 (d, J = 15.4 Hz, 1H), 3.67 (d, J = 17.1 Hz, 1H), 3.19 (s, 3H), 2.27 (s, 3H); M/Z=[M+1]: 541.05 |
| 163 | (2-氯代-6-甲基苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.47-7.51 (m, 3H), 7.40-7.41 (m, 2H), 7.36-7.38 (m, 2H), 7.33 (t, J = 7.7 Hz, 1H), 7.23-7.25 (m, 1H), 4.19 (d, J = 15.2 Hz, 1H), 4.05 (dd, J = 17.2, 1.3 Hz, 1H), 3.94 (d, J = 14.9 Hz, 1H), 3.66 (d, J = 17.1 Hz, 1H), 3.43 (s, 3H), 2.74 (s, 3H), 2.29 (s, 3H); M/Z=[M+1]: 588.75 |
| 164 | (3-溴苯基)(環丙基甲基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.98 (q, J = 1.6 Hz, 1H), 7.81 (d, J = 7.8 Hz, 1H), 7.70-7.73 (m, 1H), 7.58-7.62 (m, 2H), 7.54-7.56 (m, 1H), 7.38-7.42 (m, 3H), 4.24 (d, J = 15.4 Hz, 1H), 4.01-4.10 (m, 2H), 3.66 (d, J = 17.1 Hz, 1H), 3.18-3.25 (m, 2H), 2.29 (s, 3H), 1.01-1.11 (m, 1H), 0.49-0.64 (m, 2H), 0.23 (td, J = 9.9, 5.0 Hz, 1H), 0.05 (dt, J = 14.9, 5.1 Hz, 1H); M/Z=[M+1]: 679.00 |
| 165 | 2-(N-(4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)-S-甲基磺醯亞胺基)-2-甲基丙腈 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.52-7.70 (m, 4H), 7.40-7.45 (m, 2H), 4.50 (d, J = 15.2 Hz, 1H), 4.38 (d, J = 15.2 Hz, 1H), 4.06-4.13 (m, 1H), 3.68 (d, J = 17.1 Hz, 1H), 3.11 (s, 3H), 1.78 (s, 6H); 536.05 (MH; 35Cl)+, 538.05 (MH; 37Cl)+ |
| 166 | ((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(吡啶-2-基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.74 (d, J = 3.9 Hz, 1H), 8.10 (d, J = 7.8 Hz, 1H), 7.92 (td, J = 7.7, 1.7 Hz, 1H), 7.58 (d, J = 6.1 Hz, 2H), 7.53 (d, J = 8.3 Hz, 2H), 7.49 (ddd, J = 7.6, 4.7, 1.2 Hz, 1H), 7.39 (d, J = 8.1 Hz, 2H), 4.25 (d, J = 14.9 Hz, 1H), 4.05 (d, J = 16.4 Hz, 2H), 3.65 (d, J = 17.1 Hz, 1H), 3.32 (s, 3H); 546.15 (MH; 35Cl)+, 548.15 (MH; 37Cl)+ |
| 167 | (2-氯苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.19 (dt, J = 7.5, 1.0 Hz, 1H), 7.52-7.59 (m, 6H), 7.46-7.50 (m, 1H), 7.40 (d, J = 8.3 Hz, 2H), 4.16 (d, J = 14.9 Hz, 1H), 4.06 (dd, J = 17.1, 1.0 Hz, 1H), 3.96 (d, J = 14.9 Hz, 1H), 3.66 (d, J = 17.1 Hz, 1H), 3.37 (s, 3H); 581.00 (MH; 35Cl)+, 583.00 (MH; 37Cl)+ |
| 168 | ((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(4-(三氟甲基)苯基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.04 (d, J = 8.1 Hz, 2H), 7.83 (t, J = 8.1 Hz, 2H), 7.57-7.60 (m, 4H), 7.41 (d, J = 8.1 Hz, 2H), 4.23 (d, J = 14.7 Hz, 1H), 4.06 (d, J = 17.1 Hz, 1H), 4.00 (d, J = 14.9 Hz, 1H), 3.66 (d, J = 17.1 Hz, 1H), 3.18 (s, 3H); 613.10 (MH; 35Cl)+, 615.10 (MH; 37Cl)+ |
| 169 | ((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)二苯基-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.99-8.01 (m, 4H), 7.59-7.62 (m, 4H), 7.46-7.55 (m, 8H), 4.30 (s, 2H), 4.08 (d, J = 17.1 Hz, 1H), 3.68 (d, J = 17.1 Hz, 1H); 607.10 (MH; 35Cl)+, 609.10 (MH; 37Cl)+ |
| 170 | ((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(對甲苯基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.78-7.83 (m, 2H), 7.52-7.60 (m, 4H), 7.42-7.52 (m, 2H), 7.35-7.37 (m, 2H), 4.13-4.22 (m, 1H), 4.05-4.11 (m, 1H), 4.00 (d, J = 14.9 Hz, 1H), 3.67 (d, J = 17.1 Hz, 1H), 3.17 (s, 3H), 2.45 (s, 3H); 559.15 (MH; 35Cl)+, 561.15 (MH; 37Cl)+ |
| 171 | ((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二氯苯基)(乙基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.59 (d, J = 5.9 Hz, 2H), 7.54 (dd, J = 8.4, 7.2 Hz, 2H), 7.44-7.46 (m, 4H), 7.32 (dd, J = 8.3, 7.3 Hz, 1H), 4.36 (d, J = 14.9 Hz, 1H), 4.09-4.13 (m, 1H), 4.06 (dd, J = 17.1, 1.2 Hz, 1H), 3.61-3.70 (m, 2H), 3.58-3.49 (m, 1H), 1.40 (td, J = 7.5, 0.7 Hz, 3H); 629.05 (MH; 35Cl)+, 631.05 (MH; 37Cl)+ |
| 172 | ((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二甲基苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.56-7.59 (m, 4H), 7.42 (d, J = 8.3 Hz, 2H), 7.31 (t, J = 7.6 Hz, 1H), 7.17 (d, J = 7.6 Hz, 2H), 4.25 (d, J = 15.2 Hz, 1H), 4.06 (d, J = 17.1 Hz, 1H), 3.95 (d, J = 14.7 Hz, 1H), 3.66 (d, J = 16.9 Hz, 1H), 3.24 (s, 3H), 2.72 (s, 6H); 573.05 (MH; 35Cl)+, 575.05 (MH; 37Cl)+ |
| 173 | 4-(N-(4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)-S-甲基磺醯亞胺基)苄腈 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.06 (dd, J = 6.7, 1.6 Hz, 2H), 7.87-7.90 (m, 2H), 7.54-7.62 (m, 4H), 7.43 (d, J = 8.6 Hz, 2H), 4.25 (d, J = 14.9 Hz, 1H), 4.10 (dd, J = 17.1, 0.5 Hz, 1H), 4.00 (d, J = 15.2 Hz, 1H), 3.69 (d, J = 17.4 Hz, 1H), 3.20 (s, 3H); 570.05 (MH; 35Cl)+, 572.05 (MH; 37Cl)+ |
| 174 | ((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(3,5-二甲基苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.59-7.62 (m, 4H), 7.54 (d, J = 5.1 Hz, 2H), 7.46 (d, J = 8.3 Hz, 2H), 7.25 (d, J = 0.7 Hz, 1H), 4.23 (d, J = 14.9 Hz, 1H), 4.09 (dd, J = 17.1, 1.5 Hz, 1H), 4.04 (d, J = 15.2 Hz, 1H), 3.69 (d, J = 17.1 Hz, 1H), 3.13 (s, 3H), 2.39 (s, 6H); 573.20 (MH; 35Cl)+, 575.20 (MH; 37Cl)+ |
| 175 | (2-氯代-6-甲基苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.55 (dd, J = 6.5, 1.8 Hz, 2H), 7.51 (d, J = 1.5 Hz, 2H), 7.38-7.42 (m, 4H), 7.33 (t, J = 7.7 Hz, 1H), 7.24 (d, J = 7.6 Hz, 1H), 4.22 (d, J = 14.9 Hz, 1H), 4.02-4.07 (m, 1H), 4.00 (d, J = 14.7 Hz, 1H), 3.64 (t, J = 16.9 Hz, 1H), 3.43 (s, 3H), 2.74 (s, 3H); 575.00 (MH; 35Cl)+, 577.00 (MH; 37Cl)+ |
| 176 | ((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(3-氟苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.69-7.71 (m, 1H), 7.52-7.63 (m, 6H), 7.42 (d, J = 8.3 Hz, 2H), 7.32 (tdd, J = 8.2, 2.6, 0.9 Hz, 1H), 4.22 (d, J = 14.9 Hz, 1H), 4.07 (d, J = 17.6 Hz, 1H), 4.01 (d, J = 15.2 Hz, 1H), 3.67 (d, J = 17.1 Hz, 1H), 3.16 (s, 3H); 563.10 (MH; 35Cl)+, 565.10 (MH; 37Cl)+ |
| 177 | ((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(苯基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.91-7.93 (m, 2H), 7.55-7.65 (m, 7H), 7.43 (d, J = 8.3 Hz, 2H), 4.21 (d, J = 15.2 Hz, 1H), 4.07 (d, J = 17.1 Hz, 1H), 4.01 (d, J = 14.9 Hz, 1H), 3.67 (d, J = 17.1 Hz, 1H), 3.16 (s, 3H); 544.90 (MH; 35Cl)+, 546.90 (MH; 37Cl)+ |
| 178 | ((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二氯苯基)(異丙基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.54-7.59 (m, 4H), 7.43-7.46 (m, 4H), 7.31 (dd, J = 8.4, 7.5 Hz, 1H), 4.37 (d, J = 15.2 Hz, 1H), 4.12 (dd, J = 11.1, 4.0 Hz, 1H), 4.06 (dd, J = 17.1, 1.2 Hz, 1H), 3.89-3.95 (m, 1H), 3.66 (d, J = 17.1 Hz, 1H), 1.52 (d, J = 6.8 Hz, 3H), 1.34 (dd, J = 6.7, 1.1 Hz, 3H); 643.00 (MH) |
| 179 | (4-溴苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.76 (d, J = 8.1 Hz, 2H), 7.69 (dd, J = 8.8, 1.5 Hz, 2H), 7.57-7.60 (m, 4H), 7.41 (d, J = 8.3 Hz, 2H), 4.21 (d, J = 14.9 Hz, 1H), 4.07 (d, J = 17.1 Hz, 1H), 3.99 (d, J = 15.2 Hz, 1H), 3.67 (d, J = 17.1 Hz, 1H), 3.15 (s, 3H); 624.80 (MH; 35Cl)+, 626.80 (MH; 37Cl)+ |
| 180 | (3-溴苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.02 (s, 1H), 7.83 (d, J = 7.8 Hz, 1H), 7.73 (d, J = 7.8 Hz, 1H), 7.57-7.60 (m, 4H), 7.40-7.45 (m, 3H), 7.26 (s, 3H), 4.22 (d, J = 14.9 Hz, 1H), 4.07 (dd, J = 17.1, 1.7 Hz, 1H), 4.02 (d, J = 14.9 Hz, 1H), 3.67 (d, J = 17.4 Hz, 1H), 3.17 (s, 3H); 624.95 (MH; 35Cl)+, 626.95 (MH; 37Cl)+ |
| 181 | (3-氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.87-7.88 (m, 1H), 7.78 (dt, J = 7.7, 1.3 Hz, 1H), 7.56-7.59 (m, 3H), 7.47-7.52 (m, 3H), 7.40-7.42 (m, 3H), 4.22 (d, J = 14.9 Hz, 1H), 4.07 (dd, J = 17.1, 1.2 Hz, 1H), 3.96-4.03 (m, 1H), 3.68 (d, J = 17.4 Hz, 1H), 3.15 (s, 3H); 563.05 (MH; 35Cl)+, 565.05 (MH; 37Cl)+ |
| 182 | (2-氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.18-8.22 (m, 1H), 7.48-7.61 (m, 7H), 7.41-7.44 (m, 3H), 5.32 (s, 0H), 4.18 (d, J = 14.7 Hz, 1H), 4.08 (dd, J = 17.1, 0.7 Hz, 1H), 3.98 (d, J = 14.9 Hz, 1H), 3.69 (d, J = 17.1 Hz, 1H), 3.37 (s, 3H); 563.05 (MH; 35Cl)+, 565.05 (MH; 37Cl)+ |
| 183 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)二苯基-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.99-8.01 (m, 4H), 7.61 (d, J = 8.6 Hz, 2H), 7.46-7.55 (m, 10H), 7.42 (t, J = 1.8 Hz, 1H), 4.30 (s, 2H), 4.08 (d, J = 17.1 Hz, 1H), 3.69 (d, J = 17.1 Hz, 1H); 589.05 (MH; 35Cl)+, 591.05 (MH; 37Cl)+ |
| 184 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二氟苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.59-7.63 (m, 2H), 7.52 (d, J = 1.5 Hz, 2H), 7.36-7.46 (m, 5H), 7.00-7.08 (m, 1H), 4.23 (d, J = 14.9 Hz, 1H), 4.07 (d, J = 17.1 Hz, 1H), 4.01 (d, J = 14.9 Hz, 1H), 3.66-3.76 (m, 1H), 3.16 (s, 3H); 563.05 (MH; 35Cl)+, 565.05 (MH; 37Cl)+ |
| 185 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二甲基苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.57 (d, J = 8.3 Hz, 2H), 7.51 (d, J = 1.5 Hz, 2H), 7.41-7.43 (m, 3H), 7.31 (t, J = 7.6 Hz, 1H), 7.16-7.18 (m, 2H), 4.25 (d, J = 14.9 Hz, 1H), 4.06 (d, J = 17.1 Hz, 1H), 3.96 (d, J = 14.9 Hz, 1H), 3.67 (d, J = 17.1 Hz, 1H), 3.24 (s, 3H), 2.72 (s, 6H); 555.10 (MH; 35Cl)+, 557.10 (MH; 37Cl)+ |
| 186 | (4-溴苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.76 (dd, J = 8.8, 1.0 Hz, 2H), 7.69 (dt, J = 6.8, 1.9 Hz, 2H), 7.58 (d, J = 8.3 Hz, 2H), 7.52 (d, J = 1.7 Hz, 2H), 7.39-7.42 (m, 3H), 4.21 (d, J = 14.9 Hz, 1H), 4.07 (dd, J = 17.1, 1.2 Hz, 1H), 3.99 (d, J = 14.9 Hz, 1H), 3.68 (d, J = 17.1 Hz, 1H), 3.15 (s, 3H); 607.00 (MH)+ |
| 187 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(苯基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.91-7.93 (m, 2H), 7.55-7.65 (m, 5H), 7.52 (d, J = 1.5 Hz, 2H), 7.41-7.44 (m, 3H), 4.21 (d, J = 14.9 Hz, 1H), 4.07 (dd, J = 17.2, 0.6 Hz, 1H), 4.01 (d, J = 14.9 Hz, 1H), 3.68 (d, J = 17.4 Hz, 1H), 3.16 (s, 3H); 527.10 (MH; 35Cl)+, 529.10 (MH; 37Cl)+ |
| 188 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(4-(三氟甲基)苯基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.04 (d, J = 8.8 Hz, 2H), 7.82 (d, J = 8.1 Hz, 2H), 7.58 (d, J = 8.1 Hz, 2H), 7.51 (d, J = 1.5 Hz, 2H), 7.39-7.42 (m, 3H), 4.23 (d, J = 15.2 Hz, 1H), 4.06 (d, J = 17.1 Hz, 1H), 4.00 (d, J = 14.9 Hz, 1H), 3.67 (d, J = 17.4 Hz, 1H), 3.1s (s, 3H); 595.10 (MH; 35Cl)+, 597.10 (MH; 37Cl)+ |
| 189 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(3-氟苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.70 (d, J = 7.8 Hz, 1H), 7.54-7.63 (m, 4H), 7.52 (d, J = 1.5 Hz, 2H), 7.41-7.45 (m, 3H), 7.32 (tdd, J = 8.2, 2.6, 0.9 Hz, 1H), 4.22 (d, J = 15.2 Hz, 1H), 4.07 (d, J = 17.4 Hz, 1H), 4.01 (d, J = 15.2 Hz, 1H), 3.68 (d, J = 17.1 Hz, 1H), 3.16 (s, 3H); 545.15 (MH; 35Cl)+, 547.15 (MH; 37Cl)+ |
| 190 | (2,6-二氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(乙基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.51-7.56 (m, 4H), 7.41-7.45 (m, 5H), 7.32 (dd, J = 8.8, 7.3 Hz, 1H), 4.36 (d, J = 14.7 Hz, 1H), 4.11 (d, J = 14.7 Hz, 1H), 4.05 (d, J = 17.4 Hz, 1H), 3.61-3.69 (m, 2H), 3.50-3.58 (m, 1H), 1.40 (t, J = 7.5 Hz, 3H); 611.05 (MH; 35Cl)+, 613.05 (MH; 37Cl)+ |
| 191 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(吡啶-2-基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.74 (dq, J = 4.7, 0.9 Hz, 1H), 8.09 (d, J = 7.8 Hz, 1H), 7.91 (td, J = 7.7, 1.7 Hz, 1H), 7.44-7.54 (m, 5H), 7.37-7.42 (m, 3H), 4.25 (d, J = 15.2 Hz, 1H), 4.07 (s, 1H), 4.03 (d, J = 2.2 Hz, 1H), 3.66 (d, J = 17.4 Hz, 1H), 3.31 (s, 3H); 528.10 (MH; 35Cl)+, 530.10 (MH; 37Cl)+ |
| 192 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(3,5-二甲基苯基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.58 (d, J = 8.3 Hz, 2H), 7.50-7.52 (m, 4H), 7.41-7.44 (m, 3H), 7.22 (s, 1H), 4.20 (d, J = 14.9 Hz, 1H), 4.04-4.09 (m, 1H), 4.02 (d, J = 15.2 Hz, 1H), 3.68 (d, J = 17.4 Hz, 1H), 3.13 (s, 3H), 2.38 (s, 6H); 555.00 (MH; 35Cl)+, 557.00 (MH; 37Cl)+ |
| 193 | (2,6-二氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(異丙基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.55 (d, J = 7.6 Hz, 2H), 7.51 (d, J = 1.5 Hz, 2H), 7.41-7.45 (m, 5H), 7.30 (dd, J = 8.6, 7.3 Hz, 1H), 4.37 (d, J = 14.9 Hz, 1H), 4.13 (d, J = 15.4 Hz, 1H), 4.06 (dd, J = 17.4, 1.2 Hz, 1H), 3.93 (t, J = 6.8 Hz, 1H), 3.67 (d, J = 17.1 Hz, 1H), 1.52 (d, J = 6.8 Hz, 3H), 1.34 (dd, J = 6.8, 1.0 Hz, 3H); 624.90 (MH; 35Cl)+, 626.90 (MH; 37Cl)+ |
| 194 | ((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二氟苯基)(乙基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.55-7.58 (m, 2H), 7.50-7.54 (m, 3H), 7.43-7.45 (m, 3H), 7.02 (dd, J = 9.3, 8.6 Hz, 2H), 4.46 (d, J = 14.9 Hz, 1H), 4.17-4.20 (m, 1H), 4.08 (d, J = 17.1 Hz, 1H), 3.69 (d, J = 17.1 Hz, 1H), 3.47-3.56 (m, 2H), 1.43-1.47 (m, 3H); 577.05 (MH; 35Cl)+, 579.05 (MH; 37Cl)+ |
| 195 | (3-溴苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.96-8.02 (m, 1H), 7.81-7.85 (m, 1H), 7.71-7.74 (m, 1H), 7.57-7.59 (m, 2H), 7.52 (d, J = 1.5 Hz, 2H), 7.39-7.45 (m, 4H), 4.22 (d, J = 14.9 Hz, 1H), 4.07 (dd, J = 17.1, 1.7 Hz, 1H), 4.01 (d, J = 14.9 Hz, 1H), 3.68 (d, J = 17.1 Hz, 1H), 3.16 (s, 3H); 607.05 (MH; 35Cl)+, 609.05 (MH; 37Cl)+ |
| 196 | 4-(N-(4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)-S-甲基磺醯亞胺基)苄腈 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.04 (d, J = 8.1 Hz, 2H), 7.86-7.88 (m, 2H), 7.61 (d, J = 6.1 Hz, 2H), 7.54 (t, J = 4.0 Hz, 1H), 7.44-7.47 (m, 2H), 4.21 (d, J = 15.4 Hz, 1H), 4.09 (d, J = 17.1 Hz, 1H), 3.94 (d, J = 15.2 Hz, 1H), 3.69 (d, J = 17.4 Hz, 1H), 3.20 (s, 3H), 2.29 (s, 3H); 584.15 (MH; 35Cl)+, 586.15 (MH; 37Cl)+ |
| 197 | ((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)(對甲苯基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.78 (d, J = 8.3 Hz, 2H), 7.58-7.61 (m, 3H), 7.41-7.45 (m, 2H), 7.35 (d, J = 8.1 Hz, 2H), 4.16 (d, J = 15.4 Hz, 1H), 4.07 (dd, J = 17.1, 2.0 Hz, 1H), 3.93 (d, J = 15.4 Hz, 1H), 3.66 (d, J = 17.1 Hz, 1H), 3.14 (s, 3H), 2.44 (s, 3H), 2.26 (s, 3H); 575.20 (MH; 35Cl)+, 577.15 (MH; 37Cl)+ |
| 198 | ((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(2,6-二氯苯基)(乙基)-l6-磺胺酮 | 1 H-NMR (400 MHz, CHLOROFORM-D) δ 7.78 (d, J = 8.3 Hz, 2H), 7.58-7.61 (m, 3H), 7.41-7.45 (m, 2H), 7.35 (d, J = 8.1 Hz, 2H), 4.16 (d, J = 15.4 Hz, 1H), 4.07 (dd, J = 17.1, 2.0 Hz, 1H), 3.93 (d, J = 15.4 Hz, 1H), 3.66 (d, J = 17.1 Hz, 1H), 3.14 (s, 3H), 2.44 (s, 3H), 2.26 (s, 3H); 642.90 (MH; 35Cl)+, 644.90 (MH; 37Cl)+ |
| 199 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(丙基亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.25 (s, 1H), 7.81 (t, J = 1.8 Hz, 1H), 7.66 (d, J = 7.6 Hz, 2H), 7.62 (d, J = 1.7 Hz, 2H), 7.52 (d, J = 7.8 Hz, 1H), 4.39 (d, J = 18.3 Hz, 1H), 4.30 (d, J = 18.6 Hz, 1H), 2.96-3.05 (m, 2H), 2.39 (s, 3H), 1.57-1.69 (m, 2H), 1.00 (t, J = 7.3 Hz, 3H)) ESI MS (m/z): 504.95 (M-H); ESI MS (m/z): 504.95 (M-H) |
| 200 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.22 (s, 1H), 7.81 (t, J = 1.8 Hz, 1H), 7.66 (d, J = 7.8 Hz, 2H), 7.62 (d, J = 1.7 Hz, 2H), 7.52 (d, J = 7.8 Hz, 1H), 4.39 (d, J = 18.6 Hz, 1H), 4.30 (d, J = 18.3 Hz, 1H), 2.93-3.09 (m, 2H), 2.39 (s, 3H), 1.15-1.19 (m, 3H) ESI MS (m/z): 491.00 (M-H); ESI MS (m/z): 491.00 (M-H) |
| 201 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.36 (s, 1H), 7.80 (d, J = 6.1 Hz, 2H), 7.65 (d, J = 7.3 Hz, 2H), 7.54 (d, J = 8.1 Hz, 1H), 4.39 (d, J = 18.3 Hz, 1H), 4.31 (d, J = 18.8 Hz, 1H), 2.80 (s, 3H), 2.39 (s, 3H); ESI MS (m/z): 494.75 (M-H); ESI MS (m/z): 494.75 (M-H) |
| 202 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(間甲苯基亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.64 (s, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.48-7.64 (m, 8H), 7.41 (d, J = 7.6 Hz, 1H), 4.39 (dd, J = 18.3, 1.7 Hz, 1H), 4.32 (d, J = 18.3 Hz, 1H), 2.40 (s, 6H); ESI MS (m/z): 553.00 (M-H); ESI MS (m/z): 553.00 (M-H) |
| 203 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(間甲苯基亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.64 (s, 1H), 7.79 (d, J = 6.4 Hz, 2H), 7.48-7.62 (m, 6H), 7.41 (d, J = 7.3 Hz, 1H), 4.37 (dd, J = 18.3, 1.7 Hz, 1H), 4.29 (d, J = 18.3 Hz, 1H), 2.40 (s, 6H); ESI MS (m/z): 570.95 (M-H); ESI MS (m/z): 570.95 (M-H) |
| 204 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異丁基亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.30 (s, 1H), 7.83 (t, J = 1.8 Hz, 1H), 7.68 (d, J = 7.6 Hz, 2H), 7.64 (d, J = 1.7 Hz, 2H), 7.54 (d, J = 8.1 Hz, 1H), 4.42 (dd, J = 18.5, 1.3 Hz, 1H), 4.32 (d, J = 18.6 Hz, 1H), 2.90-3.00 (m, 2H), 2.41 (s, 3H), 1.96-2.03 (m, 1H), 1.04 (d, J = 6.4 Hz, 6H) ); ESI MS (m/z): 519.15 |
| 205 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.36 (s, 1H), 7.80-7.82 (m, 1H), 7.66 (dd, J = 9.3, 3.2 Hz, 2H), 7.62 (t, J = 1.8 Hz, 2H), 7.54 (d, J = 7.8 Hz, 1H), 4.40 (d, J = 18.3 Hz, 1H), 4.30 (d, J = 18.3 Hz, 1H), 2.79 (s, 3H), 2.39 (s, 3H); ESI MS (m/z): 476.85 |
| 206 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.22 (d, J = 2.4 Hz, 1H), 7.78-7.81 (m, 2H), 7.65 (dd, J = 7.7, 3.3 Hz, 2H), 7.53 (d, J = 8.1 Hz, 1H), 4.39 (d, J = 18.3 Hz, 1H), 4.31 (d, J = 18.6 Hz, 1H), 2.95-3.07 (m, 2H), 2.39 (s, 3H), 1.17 (t, J = 7.5 Hz, 3H); ; ESI MS (m/z): 508.80 (M-H) |
| 207 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(苯基亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.68 (s, 1H), 7.77-7.81 (m, 3H), 7.58-7.64 (m, 7H), 7.52 (d, J = 7.9 Hz, 1H), 4.38 (dd, J = 18.5, 2.3 Hz, 1H), 4.26-4.31 (dd, J = 18.5, 2.3 Hz, 1H), 2.40 (s, 3H) ); ; ESI MS (m/z): 539.00 (M-H) |
| 208 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異丙基亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.11 (s, 1H), 7.81 (t, J = 1.8 Hz, 1H), 7.66 (d, J = 7.9 Hz, 2H), 7.62 (d, J = 1.8 Hz, 2H), 7.50 (d, J = 7.9 Hz, 1H), 4.39 (d, J = 18.3 Hz, 1H), 4.30 (d, J = 18.6 Hz, 1H), 3.16-3.23 (m, 1H), 2.38 (s, 3H), 1.23 (d, J = 6.7 Hz, 3H), 1.16 (d, J = 6.7 Hz, 3H) ; ESI MS (m/z): 504.95 (M-H) |
| 209 | N-(丁基亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.24 (s, 1H), 7.81 (t, J = 1.8 Hz, 1H), 7.66 (d, J = 7.3 Hz, 2H), 7.62 (d, J = 1.7 Hz, 2H), 7.52 (d, J = 8.1 Hz, 1H), 4.40 (d, J = 18.3 Hz, 1H), 4.30 (d, J = 18.6 Hz, 1H), 2.96-3.08 (m, 2H), 2.39 (s, 3H), 1.52-1.64 (m, 2H), 1.37-1.46 (m, 2H), 0.91 (t, J = 7.3 Hz, 3H) ); ESI MS (m/z): 518.80 (M-H) |
| 210 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-((3-(三氟甲基)苯基)亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.77 (s, 1H), 8.11 (d, J = 6.8 Hz, 2H), 7.99 (d, J = 7.1 Hz, 1H), 7.83-7.87 (m, 1H), 7.80 (q, J = 1.6 Hz, 1H), 7.64 (d, J = 4.4 Hz, 1H), 7.59-7.62 (m, 3H), 7.53-7.56 (m, 1H), 4.38 (dd, J = 18.5, 2.1 Hz, 1H), 4.28 (dd, J = 18.5, 2.1 Hz, 1H), 2.41 (s, 3H) ); ESI MS (m/z): 607.15 (M-H) |
| 211 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-((4-(三氟甲氧基)苯基)亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.73 (s, 1H), 7.92-7.95 (m, 2H), 7.80 (t, J = 1.8 Hz, 1H), 7.60-7.64 (m, 6H), 7.51-7.54 (m, 1H), 4.38 (dd, J = 18.3, 2.7 Hz, 1H), 4.28 (dd, J = 18.6, 2.4 Hz, 1H), 2.41 (s, 3H) ); ESI MS (m/z): 623.15 (M-H) |
| 212 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-乙基苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.62 (s, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.69 (d, J = 8.3 Hz, 2H), 7.60-7.63 (m, 4H), 7.51 (d, J = 7.9 Hz, 1H), 7.45 (d, J = 8.3 Hz, 2H), 4.37 (dd, J = 18.5, 2.3 Hz, 1H), 4.28 (dd, J = 18.5, 2.3 Hz, 1H), 2.69 (q, J = 7.6 Hz, 2H), 2.40 (s, 3H), 1.19 (t, J = 7.6 Hz, 3H) ; ESI MS (m/z): 566.75 (M-H) |
| 213 | N-((4-(叔丁基)苯基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.64 (s, 1H), 7.80 (t, J = 6.4 Hz, 2H), 7.71 (t, J = 9.0 Hz, 2H), 7.59-7.65 (m, 4H), 7.51 (d, J = 7.9 Hz, 1H), 4.36 (dd, J = 18.3, 2.2 Hz, 1H), 4.32 (dd, J = 18.3, 2.2 Hz, 1H), 2.41 (s, 3H), 1.32 (s, 9H) ); ESI MS (m/z): 613.05 (M-H) |
| 214 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-乙基苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.62 (s, 1H), 7.79 (d, J = 6.4 Hz, 2H), 7.70 (t, J = 7.8 Hz, 2H), 7.58-7.62 (m, 2H), 7.51 (d, J = 7.9 Hz, 1H), 7.45 (d, J = 8.3 Hz, 2H), 4.36 (dd, J = 18.5, 2.3 Hz, 1H), 4.29 (dd, J = 18.5, 2.3 Hz, 1H), 2.68 (q, J = 7.5 Hz, 2H), 2.40 (s, 3H), 1.19 (t, J = 7.6 Hz, 3H) ); ESI MS (m/z): 585.00 (M-H) |
| 215 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.75 (s, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.60-7.70 (m, 7H), 7.54 (d, J = 7.8 Hz, 1H), 7.43-7.48 (m, 1H), 4.38 (dd, J = 18.3, 2.2 Hz, 1H), 4.28 (dd, J = 18.3, 2.2 Hz, 1H), 2.41 (s, 3H) ); ESI MS (m/z): 556.95 (M-H) |
| 216 | N-((4-(叔丁基)苯基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.64 (s, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.70 (d, J = 8.6 Hz, 2H), 7.60-7.65 (m, 6H), 7.51 (d, J = 7.9 Hz, 1H), 4.38 (dd, J = 18.5, 3.2 Hz, 1H), 4.28 (dd, J = 18.8, 3.5 Hz, 1H), 2.41 (s, 3H), 1.32 (s, 9H) ; ESI MS (m/z): 595.05 (M-H) |
| 217 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二甲基苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.56 (s, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.59-7.63 (m, 4H), 7.54 (s, 1H), 7.49 (q, J = 7.9 Hz, 2H), 7.35-7.38 (m, 1H), 4.37 (dd, J = 18.3, 2.0 Hz, 1H), 4.28 (d, J = 20.3 Hz, 1H), 2.40 (s, 3H), 2.31 (s, 3H), 2.29 (s, 3H); ESI MS (m/z): 569.05 (M-H) |
| 218 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-乙基苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.61 (s, 1H), 7.91 (dd, J = 7.8, 1.4 Hz, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.60-7.63 (m, 4H), 7.51 (dtd, J = 24.1, 7.5, 1.4 Hz, 2H), 7.42 (t, J = 7.8 Hz, 2H), 4.37 (d, J = 18.6 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 2.72 (q, J = 7.4 Hz, 2H), 2.38 (s, 3H), 1.20 (t, J = 7.5 Hz, 3H) ); ESI MS (m/z): 567.05 (M-H) |
| 219 | N-((3-溴苯基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.73 (s, 1H), 7.94 (t, J = 1.7 Hz, 1H), 7.78-7.82 (m, 3H), 7.53-7.64 (m, 6H), 4.38 (dd, J = 18.5, 2.1 Hz, 1H), 4.28 (d, J = 18.8 Hz, 1H), 2.41 (s, 3H) ; ESI MS (m/z): 619.00 (M-H) |
| 220 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.75 (s, 1H), 7.79 (d, J = 6.1 Hz, 2H), 7.58-7.72 (m, 5H), 7.53-7.56 (m, 1H), 7.43-7.48 (m, 1H), 4.37 (dd, J = 18.3, 2.1 Hz, 1H), 4.30 (d, J = 18.3 Hz, 1H), 2.41 (s, 3H) ); ESI MS (m/z): 574.95 (M-H) |
| 221 | N-(丁基亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.24 (s, 1H), 7.80 (d, J = 6.1 Hz, 2H), 7.65 (d, J = 7.1 Hz, 2H), 7.52 (d, J = 7.8 Hz, 1H), 4.39 (d, J = 18.6 Hz, 1H), 4.31 (d, J = 18.6 Hz, 1H), 2.96-3.08 (m, 2H), 2.39 (s, 3H), 1.53-1.64 (m, 2H), 1.36-1.46 (m, 2H), 0.91 (t, J = 7.3 Hz, 3H) ; ESI MS (m/z): 537.00 (M-H) |
| 222 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(丙基亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.26 (s, 1H), 7.80 (d, J = 6.1 Hz, 2H), 7.65 (d, J = 7.3 Hz, 2H), 7.52 (d, J = 7.9 Hz, 1H), 4.38 (d, J = 19.0 Hz, 1H), 4.31 (d, J = 19.0 Hz, 1H), 2.98-3.02 (m, 2H), 2.39 (s, 3H), 1.57-1.69 (m, 2H), 1.00 (t, J = 7.3 Hz, 3H) ); ESI MS (m/z): 522.75 (M-H) |
| 223 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(3-(甲基氨基)-3-氧丙基)(氧代)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.26 (s, 1H), 7.80 (d, J = 6.1 Hz, 2H), 7.65 (d, J = 7.3 Hz, 2H), 7.52 (d, J = 7.9 Hz, 1H), 4.38 (d, J = 19.0 Hz, 1H), 4.31 (d, J = 19.0 Hz, 1H), 2.98-3.02 (m, 2H), 2.39 (s, 3H), 1.57-1.69 (m, 2H), 1.00 (t, J = 7.3 Hz, 3H) )ESI MS (m/z): 522.75 (M-H) |
| 224 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-(異丙基氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.02 (d, J = 4.0 Hz, 1H), 7.85 (d, J = 8.6 Hz, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.62 (d, J = 1.5 Hz, 2H), 7.58 (d, J = 6.4 Hz, 2H), 4.38 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.6 Hz, 1H), 3.71-3.84 (m, 2H), 3.45 (s, 3H), 2.67 (m, 2H), 2.57 (d, J= 4.8 Hz, 3H), 2.52 (s, 3H) ESI MS (m/z): 564.00 (M+H) |
| 225 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-甲氧基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.96 (d, J = 7.3 Hz, 1H), 7.84-7.86 (m, 1H), 7.80 (t, J = 2.0 Hz, 1H), 7.62 (d, J = 1.8 Hz, 2H), 7.58 (d, J = 6.7 Hz, 2H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.70-3.86 (m, 3H), 3.45 (s, 3H), 2.60-2.70 (m, 2H), 2.52 (s, 3H), 1.03 (dd, J = 6.4, 1.2 Hz, 6H) ESI MS (m/z): 592.30 (M+H) |
| 226 | N-((3-(環丙基氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.93 (dd, J = 7.8, 1.7 Hz, 1H), 7.79-7.82 (m, 2H), 7.71-7.75 (m, 1H), 7.56-7.62 (m, 4H), 7.31 (d, J = 7.8 Hz, 1H), 7.22-7.26 (m, 1H), 4.37 (d, J = 18.3 Hz, 1H), 4.27 (d, J = 18.3 Hz, 1H), 3.91 (s, 3H), 3.54 (s, 3H), 2.43 (s, 3H) ESI MS (m/z): 584.80 (M+H) |
| 227 | N-((3-(環丁基氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.15 (d, J = 4.0 Hz, 1H), 7.84-7.86 (m, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.54-7.62 (m, 4H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.70-3.83 (m, 2H), 3.38-3.50 (m, 3H), 2.57-2.70 (m, 3H), 2.52 (s, 3H), 0.61-0.57 m, 2H), 0.34-0.42 (m, 2H) ESI MS (m/z): 589.85 (M+H) |
| 228 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-((2,2-二氟乙基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.33 (d, J = 7.6 Hz, 1H), 7.85 (d, J = 8.6 Hz, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.62 (d, J = 1.8 Hz, 2H), 7.58 (d, J = 7.0 Hz, 2H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.6 Hz, 1H), 4.14-4.22 (m, 1H), 3.69-3.82 (m, 2H), 3.45 (s, 3H), 2.58-2.71 (m, 2H), 2.52 (s, 3H), 2.08-2.16 (m, 2H), 1.78-1.89 (m, 2H), 1.55-1.63 (m, 2H) ESI MS (m/z): 603.80 (M+H) |
| 229 | N-((3-(環丙基氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.52 (t, J = 5.8 Hz, 1H), 7.85 (d, J = 8.9 Hz, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.62 (d, J = 1.5 Hz, 2H), 7.59 (d, J = 7.3 Hz, 2H), 5.98 (tt, J = 55.7, 3.8 Hz, 1H), 4.37 (d, J = 18.6 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.80 (ddd, J = 30.9, 14.2, 7.9 Hz, 2H), 3.44-3.55 (m, 5H), 2.71-2.84 (m, 2H), 2.52 (s, 3H) ESI MS (m/z): 613.85 (M+H) |
| 230 | N-((3-(環丁基氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.15 (d, J = 3.7 Hz, 1H), 7.85 (d, J = 8.8 Hz, 1H), 7.80 (d, J = 6.1 Hz, 2H), 7.57 (d, J = 7.1 Hz, 2H), 4.36 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.3 Hz, 1H), 3.70-3.83 (m, 2H), 3.45 (s, 3H), 2.57-2.68 (m, 3H), 2.51 (s, 3H), 0.55-0.62 (m, 2H), 0.34-0.38 (m, 2H) ESI MS (m/z): 607.85 (M+H) |
| 231 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-((2,2-二氟乙基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.33 (d, J = 11.2 Hz, 1H), 7.85 (dd, J = 7.9, 2.3 Hz, 1H), 7.80 (dd, J = 6.2, 1.8 Hz, 2H), 7.56-7.59 (m, 2H), 4.36 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.3 Hz, 1H), 4.15-4.22 (m, 1H), 3.69-3.83 (m, 2H), 3.45 (s, 3H), 2.60-2.71 (m, 2H), 2.52 (s, 3H), 2.10-2.14 (m, 2H), 1.81-1.86 (m, 2H), 1.56-1.62 (m, 2H) ESI MS (m/z): 621.95 (M+H) |
| 232 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-氧代-3-((2,2,2-三氟乙基)氨基)丙基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.54 (t, J = 5.7 Hz, 1H), 7.87 (d, J = 7.8 Hz, 1H), 7.81 (t, J = 6.2 Hz, 2H), 7.60 (d, J = 7.8 Hz, 2H), 6.00 (tt, J = 55.7, 3.7 Hz, 1H), 4.38 (d, J = 18.3 Hz, 1H), 4.31 (d, J = 18.6 Hz, 1H), 3.82 (ddd, J = 30.9, 14.2, 7.9 Hz, 2H), 3.45-3.57 (m, 5H), 2.74-2.86 (m, 2H), 2.54 (s, 3H) ESI MS (m/z): 632.00 (M+H) |
| 233 | N-((3-((1-氰基環丙基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.81 (t, J = 6.5 Hz, 1H), 7.87 (d, J = 8.6 Hz, 1H), 7.82 (t, J = 1.8 Hz, 1H), 7.64 (d, J = 1.7 Hz, 2H), 7.61 (d, J = 7.3 Hz, 2H), 4.39 (d, J = 18.3 Hz, 1H), 4.30 (d, J = 18.3 Hz, 1H), 3.80-3.97 (m, 4H), 3.48 (s, 3H), 2.80-2.86 (m, 2H), 2.54 (s, 3H) ESI MS (m/z): 631.80 (M+H) |
| 234 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-氧代-3-(丙基氨基)丙基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 9.03 (s, 1H), 7.87 (d, J = 8.8 Hz, 1H), 7.82 (t, J = 1.8 Hz, 1H), 7.64 (d, J = 1.7 Hz, 2H), 7.61 (d, J = 7.3 Hz, 2H), 4.39 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.3 Hz, 1H), 3.75-3.89 (m, 2H), 3.48 (s, 3H), 2.67-2.82 (m, 2H), 2.53 (s, 3H), 1.48 (dd, J = 8.2, 5.3 Hz, 2H), 1.12 (dd, J = 8.3, 5.6 Hz, 2H) ESI MS (m/z): 614.85 (M+H) |
| 235 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-(乙基(甲基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.06 (t, J = 5.3 Hz, 1H), 7.85 (dd, J = 6.7, 2.1 Hz, 1H), 7.80 (t, J = 2.0 Hz, 1H), 7.62 (d, J = 1.8 Hz, 2H), 7.58 (d, J = 6.7 Hz, 2H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.71-3.84 (m, 2H), 3.47 (s, 3H), 3.00 (dd, J = 12.6, 7.0 Hz, 2H), 2.62-2.75 (m, 2H), 2.52 (s, 3H), 1.32-1.42 (m, 2H), 0.80-0.87 (m, 3H) ESI MS (m/z): 591.80 (M+H) |
| 236 | N-(苄基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.85 (dd, J = 8.8, 1.5 Hz, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.62 (d, J = 1.7 Hz, 2H), 7.58 (d, J = 6.6 Hz, 2H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.73-3.85 (m, 2H), 3.48-3.46 (m, 3H), 3.28-3.37 (m,2H), 2.81-2.95 (m, 5H), 2.52 (s, 3H), 1.09-0.97 (m, 3H) ESI MS (m/z): 591.95 (M+H) |
| 237 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-氧代-3-((2,2,2-三氟乙基)氨基)丙基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.77-7.80 (m, 3H), 7.57 (d, J = 6.7 Hz, 2H), 7.40-7.48 (m, 5H), 4.99 (s, 2H), 4.36 (d, J = 18.3 Hz, 1H), 4.29 (d, J = 18.3 Hz, 1H), 3.32 (s, 3H), 2.48 (s, 3H) ESI MS (m/z): 586.75 (M+H) |
| 238 | N-(苄基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.81 (t, J = 6.2 Hz, 1H), 7.87 (d, J = 7.8 Hz, 1H), 7.75-7.83 (m, 2H), 7.60 (d, J = 8.3 Hz, 2H), 4.39 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.77-4.00 (m, 4H), 3.50 (s, 3H), 2.76-2.88 (m, 2H), 2.54 (s, 3H) ESI MS (m/z): 651.65 (M+H) |
| 239 | N-((3-((1-氰基環丙基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.77-7.81 (m, 2H), 7.62 (d, J = 1.8 Hz, 2H), 7.57-7.58 (m, 2H), 7.40-7.48 (m, 5H), 4.98 (s, 2H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.32 (s, 3H), 2.49 (s, 3H) ESI MS (m/z): 568.85 (M+H) |
| 240 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-氧代-3-(丙基氨基)丙基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 9.01 (s, 1H), 7.85 (d, J = 7.9 Hz, 1H), 7.80 (d, J = 6.1 Hz, 2H), 7.58 (d, J = 8.3 Hz, 2H), 4.36 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.6 Hz, 1H), 3.74-3.87 (m, 2H), 3.48 (s, 3H), 2.65-2.80 (m, 2H), 2.52 (s, 3H), 1.40-1.49 (m, 2H), 1.06-1.16 (m, 2H) ESI MS (m/z): 634.85 (M+H) |
| 241 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-(乙基(甲基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.06 (t, J = 5.3 Hz, 1H), 7.85 (d, J = 8.6 Hz, 1H), 7.80 (d, J = 6.1 Hz, 2H), 7.57 (d, J = 7.3 Hz, 2H), 4.36 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.70-3.82 (m, 2H), 3.45 (s, 3H), 3.00 (dd, J = 12.7, 6.9 Hz, 2H), 2.62-2.75 (m, 2H), 2.52 (s, 3H), 1.32-1.42 (m, 2H), 0.82 (t, J = 7.5 Hz, 3H) ESI MS (m/z): 609.90 (M+H) |
| 242 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(5-(三氟甲基)吡啶-2-基)-l6-亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.84-7.86 (m, 1H), 7.80 (d, J = 6.1 Hz, 2H), 7.57 (d, J = 7.3 Hz, 2H), 4 4.38 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.6 Hz, 1H), 3.75-3.85 (m, 2H), 3.48 (d, J = 1.8 Hz, 3H), 3.35-3.30 (m, 2H), 2.95-2.81 (m, 5H), 2.52 (s, 3H), 1.08-0.99 (m, 3H) ESI MS (m/z): 609.90 (M+H) |
| 243 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-甲氧基吡啶-2-基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 9.25 (t, J = 0.9 Hz, 1H), 8.67 (dd, J = 8.4, 2.1 Hz, 1H), 8.46 (d, J = 8.3 Hz, 1H), 7.92 (d, J = 8.1 Hz, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.60-7.62 (m, 3H), 7.57 (s, 1H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.62 (s, 3H), 2.43 (s, 3H) ESI MS (m/z): 623.95 (M+H) |
| 244 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-甲氧基乙基)(2-甲氧基苯基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.59 (d, J = 5.8 Hz, 1H), 7.89 (d, J = 7.9 Hz, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.69 (d, J = 2.4 Hz, 1H), 7.59-7.62 (m, 3H), 7.57 (s, 1H), 7.33 (q, J = 2.6 Hz, 1H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.97 (s, 3H), 3.53 (s, 3H), 2.44 (s, 3H) ESI MS (m/z): 585.95 (M+H) |
| 245 | N-((4-氰基苄基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.90 (dd, J = 7.9, 1.8 Hz, 1H), 7.83 (d, J = 8.3 Hz, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.69-7.73 (m, 1H), 7.60 (dd, J = 10.2, 1.7 Hz, 3H), 7.56 (s, 1H), 7.28 (d, J = 7.9 Hz, 1H), 7.20-7.24 (m, 1H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.98 (t, J = 5.8 Hz, 2H), 3.89 (s, 3H), 3.65-3.74 (m, 2H), 3.03 (s, 3H), 2.44 (s, 3H) ESI MS (m/z): 629.00 (M+H) |
| 246 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((6-氟吡啶-2-基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 7.91 (d, J = 8.3 Hz, 2H), 7.80 (t, J = 1.8 Hz, 1H), 7.78 (d, J = 8.6 Hz, 1H), 7.66 (d, J = 8.3 Hz, 2H), 7.62 (d, J = 1.8 Hz, 2H), 7.59 (d, J = 7.3 Hz, 2H), 5.11 (dd, J = 17.7, 13.4 Hz, 2H), 4.37 (d, J = 18.3 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.38 (s, 3H), 2.48 (s, 3H) ESI MS (m/z): 594.05 (M+H) |
| 247 | N-((3-溴苯基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 8.62 (td, J = 2.8, 1.5 Hz, 1H), 8.08-8.13 (m, 1H), 7.86-7.91 (m, 2H), 7.80 (t, J = 1.8 Hz, 1H), 7.60-7.62 (m, 3H), 7.58 (s, 1H), 4.37 (d, J = 18.6 Hz, 1H), 4.28 (d, J = 18.3 Hz, 1H), 3.66 (s, 3H), 2.43 (s, 3H) ESI MS (m/z): 572.00 (M-H) |
| 248 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二甲基苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.72 (s, 1H), 8.42 (s, 1H), 8.14 (dd, J = 8.7, 5.0 Hz, 2H), 8.04-8.06 (m, 1H), 7.79-7.82 (m, 2H), 7.54-7.69 (m, 7H), 4.37 (q, J = 18.4 Hz, 1H), 4.27 (q, J = 18.4 Hz, 1H), 2.41 (s, 3H) ESI MS (m/z): 636.75 (M-H) |
| 249 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(苯基亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.38 (s, 1H), 7.80 (d, J = 6.4 Hz, 2H), 7.65 (d, J = 8.1 Hz, 2H), 7.45 (t, J = 9.0 Hz, 5H), 4.29-4.42 (m, 4H), 2.28 (s, 3H) ESI MS (m/z): 584.80 (M-H) |
| 250 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-乙基苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.78 (s, 1H), 7.87 (t, J = 1.8 Hz, 1H), 7.83 (d, J = 2.0 Hz, 2H), 7.79 (d, J = 6.1 Hz, 2H), 7.62 (d, J = 7.6 Hz, 2H), 7.57 (d, J = 8.1 Hz, 1H), 4.37 (dd, J = 18.5, 1.8 Hz, 1H), 4.30 (d, J = 18.2 Hz, 1H), 2.42 (s, 3H) ESI MS (m/z): 556.90 (M-H) |
| 251 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-((4-(三氟甲氧基)苯基)亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.56 (s, 1H), 7.79 (d, J = 6.4 Hz, 2H), 7.59-7.61 (m, 2H), 7.47-7.53 (m, 3H), 7.37 (d, J = 8.1 Hz, 1H), 4.36 (dd, J = 18.6, 1.7 Hz, 1H), 4.29 (d, J = 18.1 Hz, 1H), 2.40 (s, 3H), 2.31 (s, 3H), 2.29 (s, 3H) ESI MS (m/z): 584.85 (M-H) |
| 252 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-甲氧基苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.78 (s, 1H), 7.88 (t, J = 1.8 Hz, 1H), 7.83 (d, J = 1.7 Hz, 2H), 7.80 (t, J = 2.0 Hz, 1H), 7.61-7.65 (m, 4H), 7.57 (d, J = 7.8 Hz, 1H), 4.38 (dd, J = 18.5, 2.1 Hz, 1H), 4.28 (d, J = 18.6 Hz, 1H), 2.42 (s, 3H) ESI MS (m/z): 640.85 (M-H) |
| 253 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(萘-2-基亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.38 (s, 1H), 7.81 (t, J = 1.8 Hz, 1H), 7.61-7.66 (m, 4H), 7.45 (t, J = 8.9 Hz, 5H), 4.27-4.42 (m, 4H), 2.24 (s, 3H) ESI MS (m/z): 568.75 (M-H) |
| 254 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-氟苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.43 (s, 1H), 7.89 (s, 1H), 7.82-7.85 (m, 1H), 7.81 (t, J = 1.8 Hz, 1H), 7.78 (d, J = 7.8 Hz, 1H), 7.60-7.65 (m, 5H), 7.41 (s, 1H), 4.37-4.44 (m, 3H), 4.30 (d, J = 18.6 Hz, 1H), 2.23 (s, 3H) ESI MS (m/z): 588.75 (M-H) |
| 255 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二氟苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.41 (s, 1H), 7.79 (t, J = 6.0 Hz, 2H), 7.60-7.64 (m, 2H), 7.56 (t, J = 8.3 Hz, 2H), 7.38-7.44 (m, 3H), 4.28-4.45 (m, 4H), 2.32 (s, 3H) ESI MS (m/z): 556.75 (M-H) |
| 256 | N-((4-氰基苯基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.38 (s, 1H), 7.81 (t, J = 1.8 Hz, 1H), 7.61-7.64 (m, 4H), 7.32-7.43 (m, 6H), 4.27-4.42 (m, 4H), 2.25 (s, 3H) ESI MS (m/z): 574.75 (M-H) |
| 257 | N-((4-氰基苯基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.73 (s, 1H), 8.03 (d, J = 2.1 Hz, 1H), 7.89 (t, J = 4.3 Hz, 1H), 7.77-7.81 (m, 2H), 7.60-7.65 (m, 4H), 7.55 (d, J = 7.9 Hz, 1H), 4.38 (dd, J = 18.3, 2.1 Hz, 1H), 4.28 (d, J = 18.6 Hz, 1H), 2.41 (s, 3H) ESI MS (m/z): 582.00 (M-H) |
| 258 | N-(苄基亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.35 (s, 1H), 7.81 (t, J = 1.8 Hz, 1H), 7.61-7.63 (m, 4H), 7.40 (d, J = 8.3 Hz, 3H), 7.33 (d, J = 8.3 Hz, 2H), 4.27-4.41 (m, 4H), 2.21 (s, 2H), 1.28 (s, 9H) ESI MS (m/z): 563.75 (M-H) |
| 259 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-甲氧基苄基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.69 (s, 1H), 7.82 (dt, J = 8.9, 2.2 Hz, 2H), 7.79 (d, J = 6.1 Hz, 2H), 7.72-7.75 (m, 2H), 7.60-7.63 (m, 2H), 7.53 (d, J = 8.1 Hz, 1H), 4.27-4.39 (m, 2H), 2.40 (s, 3H) ESI MS (m/z): 570.80 (M-H) |
| 260 | N-(苄基亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.68 (s, 1H), 7.78 (q, J = 2.9 Hz, 4H), 7.57-7.62 (m, 5H), 7.52-7.54 (m, 1H), 4.36 (dd, J = 18.5, 2.1 Hz, 1H), 4.29 (d, J = 18.6 Hz, 1H), 2.40 (s, 3H) ESI MS (m/z): 582.90 (M-H) |
| 261 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二氯苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.68 (s, 1H), 7.77-7.79 (m, 4H), 7.59-7.61 (m, 5H), 7.52 (d, J = 8.1 Hz, 1H), 4.36 (dd, J = 18.2, 1.8 Hz, 1H), 4.29 (d, J = 18.3 Hz, 1H), 2.41 (s, 3H) ESI MS (m/z): 552.90 (M-H) |
| 262 | N-((3-氰基苯基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.54 (s, 1H), 7.80 (t, J = 1.8 Hz, 1H), 7.69-7.73 (m, 2H), 7.60-7.63 (m, 4H), 7.50 (d, J = 7.9 Hz, 1H), 7.15 (dt, J = 9.4, 2.5 Hz, 2H), 4.37 (dd, J = 18.3, 1.8 Hz, 1H), 4.28 (d, J = 19.9 Hz, 1H), 3.85 (s, 3H), 2.40 (s, 3H) ESI MS (m/z): 608.65 (M-H) |
| 263 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二氯苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.82 (s, 1H), 8.09 (dt, J = 8.4, 1.8 Hz, 2H), 7.99 (dd, J = 6.8, 2.0 Hz, 2H), 7.79 (d, J = 6.4 Hz, 2H), 7.60-7.64 (m, 2H), 7.55 (d, J = 8.1 Hz, 1H), 4.36 (dd, J = 18.5, 2.1 Hz, 1H), 4.28 (d, J = 18.6 Hz, 1H), 2.41 (s, 3H) ESI MS (m/z): 563.80 (M-H) |
| 264 | N-((4-氯苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.82 (s, 1H), 8.09 (dd, J = 6.7, 1.8 Hz, 2H), 7.98-8.00 (m, 2H), 7.80 (t, J = 1.8 Hz, 1H), 7.60-7.65 (m, 4H), 7.55 (d, J = 7.9 Hz, 1H), 4.38 (dd, J = 18.3, 2.1 Hz, 1H), 4.28 (d, J = 18.6 Hz, 1H), 2.41 (s, 3H) ESI MS (m/z): 608.85 (M-H) |
| 265 | N-((4-溴苯基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.92 (s, 1H), 7.82-7.86 (m, 1H), 7.79 (d, J = 6.1 Hz, 2H), 7.61-7.71 (m, 3H), 7.45-7.51 (m, 2H), 7.39-7.44 (m, 1H), 4.36 (dd, J = 18.5, 1.8 Hz, 1H), 4.29 (d, J = 18.2 Hz, 1H), 2.39 (s, 3H) ESI MS (m/z): 588.75 (M-H) |
| 266 | N-((4-(叔丁基)苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.61 (s, 1H), 7.90 (d, J = 6.7 Hz, 1H), 7.79 (t, J = 5.8 Hz, 2H), 7.57-7.60 (m, 2H), 7.53 (t, J = 7.5 Hz, 1H), 7.47 (t, J = 7.2 Hz, 1H), 7.43 (d, J = 7.9 Hz, 1H), 7.39 (d, J = 7.6 Hz, 1H), 4.35 (d, J = 18.6, 1H), 4.28 (d, J = 18.6, 1H), 2.65-2.79 (m, 2H), 2.38 (s, 3H), 1.15-1.22 (m, 4H) ESI MS (m/z): 618.65 (M-H) |
| 267 | N-((4-氯代-3-氟苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.32 (s, 1H), 7.81 (t, J = 1.8 Hz, 1H), 7.61-7.64 (m, 4H), 7.33-7.41 (m, 3H), 6.94 (d, J = 8.6 Hz, 2H), 4.23-4.41 (m, 4H), 3.74 (s, 3H), 2.26 (s, 3H) ESI MS (m/z): 609.00 (M-H) |
| 268 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((5-氟-2-甲基苄基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.69 (s, 1H), 7.80-7.84 (m, 3H), 7.73 (dt, J = 9.0, 2.1 Hz, 2H), 7.60-7.64 (m, 4H), 7.53 (d, J = 8.1 Hz, 1H), 4.38 (dd, J = 18.3, 2.0 Hz, 1H), 4.28 (d, J = 18.6 Hz, 1H), 2.41 (s, 3H) ESI MS (m/z): 606.65 (M-H) |
| 269 | N-((3-氯代-5-氟苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.42 (s, 1H), 7.79 (d, J = 6.1 Hz, 2H), 7.64 (d, J = 7.8 Hz, 2H), 7.41-7.47 (m, 3H), 7.33 (d, J = 9.5 Hz, 1H), 4.29-4.43 (m, 4H), 2.24 (s, 3H) ESI MS (m/z): 584.85 (M-H) |
| 270 | N-((3-氯代-5-氟苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.72 (s, 1H), 7.90-7.94 (m, 1H), 7.79 (d, J = 6.1 Hz, 2H), 7.67-7.75 (m, 2H), 7.62 (d, J = 9.8 Hz, 2H), 7.55 (d, J = 8.1 Hz, 1H), 4.37 (dd, J = 18.5, 1.8 Hz, 1H), 4.29 (d, J = 18.2 Hz, 1H), 2.41 (s, 3H) ESI MS (m/z): 604.75 (M-H) |
| 271 | N-((3-氯代-4-氟苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.40 (s, 1H), 7.79 (d, J = 6.4 Hz, 2H), 7.64 (s, 2H), 7.27-7.46 (m, 4H), 7.16-7.21 (m, 1H), 4.29-4.43 (m, 4H), 2.24 (s, 3H) ESI MS (m/z): 624.60 (M-H) |
| 272 | N-((4-氯苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.47 (s, 1H), 7.81 (t, J = 1.8 Hz, 1H), 7.65 (d, J = 8.3 Hz, 2H), 7.62 (d, J = 1.7 Hz, 2H), 7.45 (d, J = 8.8 Hz, 1H), 7.28 (dd, J = 8.3, 6.1 Hz, 1H), 7.20 (dd, J = 9.8, 2.7 Hz, 1H), 7.09 (td, J = 8.5, 2.9 Hz, 1H), 4.36-4.47 (m, 3H), 4.30 (d, J = 18.8 Hz, 1H), 2.44 (s, 3H), 2.27 (s, 3H) ESI MS (m/z): 624.95 (M-H) |
| 273 | N-((4-(叔丁基)苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.73 (s, 1H), 7.91-7.95 (m, 2H), 7.78 (d, J = 6.4 Hz, 2H), 7.60-7.63 (m, 4H), 7.54 (d, J = 8.1 Hz, 1H), 4.37 (dd, J = 18.6, 2.4 Hz, 1H), 4.28 (d, J = 18.6, 1H), 2.41 (s, 3H) ESI MS (m/z): 606.90 (M-H) |
| 274 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二氟苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.94 (s, 1H), 7.81-7.88 (m, 2H), 7.62-7.73 (m, 5H), 7.41-7.53 (m, 3H), 4.39 (dd, J = 18.3, 1.7 Hz, 1H), 4.30 (d, J = 18.2 Hz, 1H), 2.41 (s, 3H) ESI MS (m/z): 627.20 (M-H) |
| 275 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二氯苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.38 (s, 1H), 7.79 (d, J= 6.4 Hz, 2H), 7.60-7.64 (m, 2H), 7.32-7.43 (m, 6H), 4.29-4.42 (m, 4H), 2.24-2.32 (m, 3H) ESI MS (m/z): 592.90 (M-H) |
| 276 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-甲氧基苄基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.77 (s, 1H), 8.26 (d, J = 1.5 Hz, 1H), 8.13 (d, J = 7.9 Hz, 1H), 8.08 (dt, J = 7.7, 1.2 Hz, 1H), 7.80-7.84 (m, 2H), 7.56-7.65 (m, 5H), 4.38 (dd, J = 18.5, 2.3 Hz, 1H), 4.28 (d, J = 19.0 Hz, 1H), 2.42 (s, 3H) ESI MS (m/z): 626.90 (M-H) |
| 277 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二氯苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.44 (s, 1H), 7.84 (t, J = 2.0 Hz, 1H), 7.64-7.68 (m, 5H), 7.53 (dd, J = 10.2, 1.7 Hz, 1H), 7.44 (s, 1H), 7.33 (dd, J = 8.3, 1.2 Hz, 1H), 4.40-4.46 (m, 3H), 4.33 (d, J = 18.3 Hz, 1H), 2.27 (s, 3H) ESI MS (m/z): 603.00 (M-H) |
| 278 | N-((4-溴苯基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.41 (s, 1H), 7.80 (d, J = 6.4 Hz, 2H), 7.61-7.65 (m, 3H), 7.50 (d, J = 10.3 Hz, 1H), 7.41 (s, 1H), 7.31 (d, J = 8.3 Hz, 1H), 4.29-4.43 (m, 4H), 2.28 (s, 3H) ESI MS (m/z): 626.90 (M-H) |
| 279 | N-((4-氰基苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.42 (s, 1H), 7.81 (t, J = 1.8 Hz, 1H), 7.65 (d, J = 8.3 Hz, 2H), 7.61 (d, J = 1.5 Hz, 2H), 7.41-7.47 (m, 3H), 7.33 (d, J = 9.5 Hz, 1H), 4.37-4.43 (m, 3H), 4.30 (d, J = 18.6 Hz, 1H), 2.25 (s, 3H) ESI MS (m/z): 636.85 (M-H) |
| 280 | N-((3-氰基苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.44 (s, 1H), 7.87 (d, J = 8.1 Hz, 2H), 7.81 (t, J = 1.8 Hz, 1H), 7.64 (dd, J = 11.1, 7.9 Hz, 6H), 7.40 (s, 1H), 4.48 (s, 2H), 4.39 (d, J = 18.3 Hz, 1H), 4.30 (d, J = 18.1 Hz, 1H), 2.24 (s, 3H) ESI MS (m/z): 578.00 (M-H) |
| 281 | N-((3-氰基苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.72 (s, 1H), 8.41 (s, 1H), 8.14 (dd, J = 8.7, 4.8 Hz, 2H), 8.04-8.06 (m, 1H), 7.77-7.81 (m, 3H), 7.59-7.69 (m, 4H), 7.55 (d, J = 8.1 Hz, 1H), 4.37 (m, 1H), 4.28 (d, J = 19.2 Hz, 1H), 2.43 (s, 3H) ESI MS (m/z): 596.78 (M-H) |
| 282 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(萘-2-基亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.44 (s, 1H), 7.87 (d, J = 7.8 Hz, 2H), 7.80 (d, J = 6.4 Hz, 2H), 7.64 (t, J = 7.9 Hz, 4H), 7.41 (s, 1H), 4.49 (s, 2H), 4.37 (d, J = 18.3 Hz, 1H), 4.30 (d, J = 18.1 Hz, 1H), 2.23 (s, 3H) ESI MS (m/z): 577.80 (M-H) |
| 283 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-氟苯基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.69 (s, 1H), 7.86-7.91 (m, 1H), 7.78-7.80 (m, 1H), 7.61-7.73 (m, 6H), 7.55 (d, J = 7.9 Hz, 1H), 4.37 (dd, J = 18.5, 2.0 Hz, 1H), 4.28 (d, J = 19.0 Hz, 1H), 2.41 (s, 3H) ESI MS (m/z): 607.05 (M-H) |
| 284 | N-((4-氰基苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.34 (s, 1H), 7.79 (d, J = 6.4 Hz, 2H), 7.62 (s, 2H), 7.40 (d, J = 8.1 Hz, 3H), 7.33 (d, J = 8.3 Hz, 2H), 4.28-4.40 (m, 4H), 2.27 (s, 3H), 1.27 (s, 9H) ESI MS (m/z): 575.00 (M-H) |
| 285 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苄基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.73 (s, 1H), 8.03 (d, J = 2.0 Hz, 1H), 7.89 (d, J = 8.3 Hz, 1H), 7.79 (dd, J = 8.2, 2.1 Hz, 3H), 7.62 (d, J = 10.3 Hz, 2H), 7.55 (d, J = 7.8 Hz, 1H), 4.37 (dd, J = 18.5, 1.8 Hz, 1H), 4.29 (d, J = 18.3 Hz, 1H), 2.41 (s, 3H) ESI MS (m/z): 596.15 (M-H) |
| 286 | 4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-((4-(三氟甲氧基)苄基)亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.36 (s, 1H), 7.80 (d, J = 6.4 Hz, 2H), 7.63 (d, J = 7.3 Hz, 2H), 7.43 (s, 1H), 7.33 (d, J = 8.6 Hz, 2H), 6.94 (d, J = 8.3 Hz, 2H), 4.28-4.40 (m, 3H), 4.23 (d, J = 18.5 Hz, 1H), 3.74 (s, 3H), 2.22 (s, 3H) ESI MS (m/z): 589.10 (M-H) |
| 287 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-((4-(三氟甲氧基)苄基)亞磺醯基)苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.45 (s, 1H), 7.88 (s, 1H), 7.76-7.84 (m, 4H), 7.61 (t, J = 7.8 Hz, 3H), 7.41 (s, 1H), 4.44 (s, 2H), 4.38 (d, J = 18.6 Hz, 1H), 4.31 (d, J = 18.3 Hz, 1H), 2.23 (s, 3H) ESI MS (m/z): 655.00 (M-H) |
| 288 | 4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苄基)亞磺醯基)-2-甲基苯甲醯胺 | 1 H-NMR (400 MHz, DMSO-d6 ) δ 11.39 (s, 1H), 7.79-7.81 (m, 1H), 7.61-7.65 (m, 4H), 7.54-7.58 (m, 2H), 7.38-7.44 (m, 3H), 4.27-4.45 (m, 4H), 2.23 (s, 3H) ESI MS (m/z): 637.00 (M-H) |
例
A
:棉鈴蟲
使用食物摻入法,將所需量的實驗化合物稱量並溶解在含有溶劑溶液的試管中。將試管以2000 rpm的速度渦旋90分鐘以進行適當混合,然後用水稀釋至所需的實驗濃度。當生物測定容器中的溫度達到約50o
C時,將半合成飲食添加到特定溶液中。將飲食和溶液充分攪拌使其充分混合,然後冷卻30分鐘。將凝固的飲食均勻切成幾塊,然後將這些塊放到生物測定託盤的儲存格。將單個三齡饑餓的幼蟲釋放到生物測定託盤的這些儲存格中,每個託盤蓋上蓋子。將生物測定託盤保持在溫度為25o
C,相對濕度為70%的實驗室條件下。放幼蟲96小時後記錄觀察到的死亡、瀕死和活著的幼蟲。通過將死亡的和瀕死的幼蟲相加計算死亡率,並將結果與一個未處理的對照組進行比較。根據記錄,濃度為300ppm的化合物 2 5 19 21 22 23 24 27 29 31 32 33 34 35 36 37 38 39 44 45 51 52 53 55 56 60 61 63 64 65 66 68 69 70 71 72 74 76 77 78 79 81 84 86 89 90 92 93 95 96 97 98 99 101 102 103 105 113 114 115 121 125 128 130 133 134 136 151 154 155 156 160 162 173 196 198 199 201 202 203 204 205 206 207 208 209 210 211 212 213 214 215 216 217 218 219 220 221 222 226 229 230 231 235 236 237 238 239 240 241 242 245 246 247 248 249 250 251 252 253 254 255 256 257 258 259 261 262 263 265 267 270 271 275 276 277 278 282 283 284 285 286 287 和 288 能造成超過 70% 的死亡率。
例
B
:斜紋夜蛾
使用食物摻入法,將所需量的實驗化合物稱量並溶解在含有溶劑溶液的試管中。將試管以2000 rpm的速度渦旋90分鐘以進行適當混合。當生物測定容器中的溫度達到約50o
C時,將半合成飲食添加到特定溶液中。將飲食和溶液充分攪拌使其充分混合,然後冷卻30分鐘。將凝固的飲食均勻切成幾塊,然後將這些塊放到生物測定託盤的儲存格。將單個三齡饑餓的幼蟲釋放到生物測定託盤的這些儲存格中,每個託盤蓋上蓋子。將生物測定託盤保持在溫度為25o
C,相對濕度為70%的實驗室條件下。放幼蟲96小時後記錄觀察到的死亡、瀕死和活著的幼蟲。通過將死亡的和瀕死的幼蟲相加計算死亡率,並將結果與一個未處理的對照組進行比較。根據記錄,濃度為300ppm的化合物 2 5 19 21 22 23 24 27 29 31 32 33 34 35 36 37 38 39 40 44 45 49 50 51 52 53 55 56 57 60 61 63 64 65 66 68 69 70 71 74 76 77 78 79 81 82 86 89 90 92 93 96 97 98 99 100 101 103 105 113 114 115 125 128 129 130 133 134 136 137 151 154 156 158 160 162 173 196 198 199 201 202 203 204 205 206 207 208 209 210 211 212 213 214 215 216 217 218 219 220 221 222 223 226 229 230 233 235 236 238 239 240 241 242 243 245 246 247 248 249 250 251 252 253 254 255 256 257 258 259 260 261 262 263 264 265 266 267 268 269 270 271 272 273 274 275 276 277 278 279 280 281 282 283 284 285 286 287 和 288 能造成超過 70% 的死亡率。
例
C
:小菜蛾
使用葉片浸漬法,將所需量的化合物稱量並溶解在含有溶劑溶液的試管中,放在轉速為2000 rpm的攪拌器攪拌90分鐘進行適當混合,然後用0.01% Triton-X溶液稀釋至所需的實驗濃度。將白菜葉浸入溶液中10秒鐘,遮陰乾燥20分鐘,然後轉移到生物測定託盤中。將單個二齡幼蟲釋放到生物測定託盤的這些儲存格中,每個託盤蓋上蓋子。將生物測定託盤保持在溫度為25o
C,相對濕度為70%的實驗室條件下。放幼蟲72小時後記錄觀察到的死亡、瀕死和活著的幼蟲。通過將死亡的和瀕死的幼蟲相加計算死亡率,並將結果與一個未處理的對照組進行比較。根據記錄,濃度為300ppm的化合物 2 3 5 6 7 8 9 10 15 16 17 19 20 21 22 23 24 27 29 30 31 32 33 34 35 36 37 38 39 40 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 61 63 64 65 66 67 68 69 70 71 72 73 74 75 76 77 78 79 81 82 83 84 85 86 88 89 90 91 92 93 94 95 96 97 98 99 100 101 102 103 105 113 114 115 121 124 125 126 128 130 133 136 137 145 146 151 152 154 156 158 159 160 162 163 166 167 168 170 173 176 177 178 179 180 181 182 184 185 187 188 191 196 199 200 202 203 204 205 206 207 208 210 211 212 213 214 215 216 217 218 219 220 221 222 223 224 225 226 227 228 229 230 231 232 233 234 235 236 237 238 239 240 241 242 243 246 247 248 249 250 251 252 253 254 255 256 257 258 259 260 261 262 263 264 265 266 267 268 269 270 271 272 273 274 275 276 277 278 279 280 281 282 283 284 285 286 287 和 288 能造成超過70%的死亡率。
例
D
:煙粉虱
使用葉片浸漬法,將所需量的化合物稱量並溶解在含有溶劑溶液的試管中,放在轉速為2000 rpm的攪拌器攪拌90分鐘進行適當混合,然後用0.01% Triton-X溶液稀釋至所需的實驗濃度。將棉葉浸入溶液中10秒鐘,陰涼乾燥20分鐘,然後將葉保存在玻璃單元中,將葉柄浸入水中。釋放已知數量的活力滿滿的羽化成蟲,並將其保存在溫度為25o
C,相對濕度為70%植物生長室中。放蟲72小時後記錄觀察到的死亡、瀕死和活著的幼蟲。通過將死亡的和瀕死的幼蟲相加計算死亡率,並將結果與一個未處理的對照組進行比較。
例
E
:桃蚜
使用葉片浸漬法進行試驗,將所需量的實驗化合物稱量並溶解在含有溶劑溶液的試管中,放在轉速為2000 rpm的攪拌器攪拌90分鐘進行適當混合,然後用0.01% Triton-X溶液稀釋至所需的實驗濃度。將辣椒葉浸入溶液中10秒鐘,陰涼乾燥20分鐘,然後將葉子的背面朝上放置在含有4 ml 1%瓊脂溶液的生物測定託盤的儲存格中。釋放已知數量的三齡若蟲,並將其保存在溫度為25o
C,相對濕度為70%植物生長室中。放蟲72小時後記錄觀察到的死亡、瀕死和活著的幼蟲。通過將死亡的和瀕死的幼蟲相加計算死亡率,並將結果與一個未處理的對照組進行比較。根據記錄,濃度為300ppm的化合物 77 118 131 229 235 236 249 251 和 256 能造成超過 70% 的死亡率。
例
F
:褐飛虱
採用浸苗法進行試驗,將所需量的化合物稱量並溶解在含有溶劑溶液的試管中,放在轉速為2000 rpm的攪拌器攪拌90分鐘進行適當混合,然後用0.01%Triton-X 溶液稀釋至所需的實驗濃度。將水稻幼苗浸入溶液中10秒鐘,陰涼乾燥20分鐘,然後將幼苗保存在玻璃試管,將根浸入水中,將該試管放入玻璃容器中。釋放已知數量的三齡若蟲,並將其保存在溫度為25o
C,相對濕度為75%的植物生長室中。放蟲72小時後記錄觀察到的死亡、瀕死和活著的幼蟲。通過將死亡的和瀕死的幼蟲相加計算死亡率,並將結果與一個未處理的對照組進行比較。根據記錄,濃度為300ppm的化合物213 能造成超過70%的死亡率。
在參考某些優選實施例描述本發明後,本領域技術人員應該很熟悉其他技術參數。對於本領域技術人員而言,可以在不脫離本發明範圍的情況下實施對材料和方法的許多修改。
無
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Claims (15)
- 一種式(I)化合物, 式(I) 其中, R1 選自C1- C6 -烷基、C1- C6 -鹵代烷基、C3 -C6 -環烷基和C3 -C6 -鹵代環烷基; R2a 、R2b 和R2c 獨立地選自氫、X、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基和C3 -C8 -環烷基; A選自苯基和C5 -C6 -雜環基,其可以任選地被一個或多個R3 基團取代; R3 選自氫、X、氰基、SCN、硝基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C2 -C6 -鹵代炔基、C3 -C8 -環烷基、C4 -C8 -環烯基、C4 -C8 -環炔基、SF5 、N(R′′)2 、OR4 、S(O)n R″、C(=O)-R″、C1 -C8 -烷基-S(O)n R″、C1 -C8 -烷基-C(=O)-R″和CR′=NR″; T代表-N=S(O)0-1 R7 -、-(CR5 R6 )p N=S(O)0-1 R7 -、-C(O)N=S(O)0-1 R7 -、-C(O)(CR5 R6 )p N=S(O)0-1 R7 - 和-C(O)NR9 S(O)-; 其中,片段T的LHS附著在A上,片段T的RHS附著在Z上; R4 選自氫、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、C6 -C10 -芳基和C3 -C8 -雜環基; R5 和R6 獨立地選自氫、X、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C1 -C6 -鹵代烷基、OR4 、C3 -C8 -環烷基;其中環狀環系統中的一個或多個碳原子可以被選自N、O、S基團,並且可以任選包括1-3個選自C(=O)、C(=S)、S(O)m 和Si(R′)2 的環成員的雜原子取代;或者 R5 和R6 與它們所連接的原子一起或與選自C、N、O、S基團,並且可以任選包括1-3個選自C(=O)、C(=S)、S(O)m 和Si(R′)2 的環成員的原子一起可以形成三至七元環,其本身可以被X、CN、R′、OR′、SR′、N(R′)2 、Si(R′)3 、COOR′和CON(R′)2 基團取代; R7 和Z獨立地選自C1 -C6 -烷基、C1 -C6 -氰基烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C2 -C6 -鹵代炔基、C(=O)-R″、C1 -C8 -烷基-C(=O)-R″、C(=O)-N(R′R″)、C1 -C8 -烷基-C(=O)-N(R′R″)、C2 -C8 -烯基-C(=O)-N(R′R″)、C3 -C8 -環烷基、C4 -C8 -環烯基、C4 -C8 -環炔基、C6 -C10 -芳基、C7 -C15 -芳烷基、雙環C5 -C12 -烷基、雙環C7 -C12 -烯基、稠合或非稠合或雙環C3 -C18 -碳環;其中環狀環系統中的一個或多個碳原子可以被選自N、O、S基團,並且可以任選包括1-3個選自C(=O)、C(=S)、S(O)m 和Si(R′)2 的環成員的雜原子取代;其中每個R7 或Z基團可任選地被一個或多個R8 基團取代; R8 選自氫、X、氰基、SCN、硝基、C1 -C6 -烷基、C2- C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C2 -C6 -鹵代炔基、SF5 、OR4 、N(R′′)2 、Si(R′)3 、(C=O)-R″、S(O)n R″、C1- C8 -烷基-S(O)n R″、C1 -C8 -烷基-(C=O)-R″、CR′=NR″、C3 -C8 -環烷基、C4 -C8 -環烯基;其中環狀環系統中的一個或多個碳原子可以被選自N、O、S基團,並且可以任選包括1-3個選自C(=O)、C(=S)、S(O)m 和Si(R′)2 的環成員的雜原子取代; R9 選自氫、C1 -C12 -烷基、C2 -C12 -烯基、C2 -C12 -炔基、C1 -C12 -鹵代烷基、C2 -C12 -鹵代烯基、C2 -C12 -鹵代炔基、C3 -C8 -環烷基、Si(R′)3 、OR4 、(C=O)-R″; R5 或R6 和R7 、R7 和R3 、R8 和Z或R7 和Z與它們所連接的原子一起或與選自C、N、O、S基團,並且可以任選包括1-3個選自C(=O)、C(=S)、S(O)m 和Si(R′)2 的環成員的原子一起可以形成三至七元環,其本身可以被X、CN、R′、OR′、SR′、N(R′)2 、Si(R′)3 、COOR′和CON(R′)2 基團取代; 每個R1 、R2a 、R2b 、R2c 、R3 、R4 、R5 、R6 、R7 、R8 和R9 可以任選地被一個或多個選自X、CN、R″、OR″、SR″、N(R′R″)、Si(R′)3 、COOR′和CON(R′R″)的基團取代; X代表鹵素; R′代表氫、C1- C6 -烷基或C3 -C8 -環烷基;其中烷基和環烷基可任選被一個或多個X取代; R″代表氫、C1- C6 -烷基、C1- C6 -鹵代烷基、C3 -C8 -環烷基、N(R′)2 、OR′和C6- C10 -芳基;其中環狀環系統中的一個或多個碳原子可以被選自N、O、S基團,並且可以任選包括1-3個選自C(=O)、C(=S)、S(O)m 和Si(R′)2 的環成員的雜原子取代,並且每個R″可以任選地被一個或多個選自X、R″、CN、OR″、SR″、N(R′)2 ,、Si(R′)3 、COOR′和CON(R′)2 的基團取代; R′″選自氫、R″、CN、C1 -C6 -烷基、C1 -C6 -鹵代烷基、C2 -C6 -烯基、C2 -C6 -炔基、C3 -C8 -環烷基、C4 -C8 -環烯基、C4 -C8 -環炔基、OR4 、(C=O)-R′、COOR′、CON(R′)2 、C6 -C10 -芳基、C7 -C15 -芳烷基和C5 -C10 -雜環基基團;其中環狀環系統中的一個或多個碳原子可以被選自N、O、S基團,並且可以任選包括1-3個選自C(=O)、C(=S)、S(O)m 和Si(R′)2 的環成員的雜原子取代,並且每個R′″可以任選地被一個或多個選自X、R′、CN、OR′、SR′、N(R′)2 、Si(R′)3 、COOR′或CON(R′)2 的基團取代; p代表整數1或2; q代表整數0或1; m和n代表整數0、1或2; 或其農業上可接受的鹽、異構體/結構異構體、立體異構體、非對映異構體、對映異構體、互變異構體、金屬絡合物、多晶型物或N-氧化物。
- 如請求項1所述的式(I)化合物,其中 R1 選自C1- C6 -烷基、C1- C6 -鹵代烷基; R2a 、R2b 和R2c 獨立地選自氫、X、氰基、C1 -C6 -烷基、C1 -C6 -鹵代烷基和C3 -C8 -環烷基; A選自苯基、噻吩基和吡啶基,其可以任選地被一個或多個R3 基團取代; R3 選自氫、X、氰基、C1 -C6 -烷基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基; T選自、、、和其中,#表示與A鍵合,箭頭表示與Z鍵合; R4 選自氫、C1 -C6 -烷基、C1 -C6 -鹵代烷基、C2 -C6 -C3 -C8 -環烷基、苯基和C3 -C6 -雜環基; R5 選自氫、X、C1 -C6 -烷基、C1 -C6 -鹵代烷基、C3 -C8 -環烷基; R6 選自氫、X、C1 -C6 -烷基; R7 和Z獨立地選自C1 -C6 -烷基、C1 -C6 -氰基烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C2 -C6 -鹵代炔基、C(=O)-R″、C1 -C8 -烷基-C(=O)-R″、C(=O)-N(R′R″)、C1 -C8 -烷基-C(=O)-N(R′R″)、C2 -C8 -烯基-C(=O)-N(R′R″)、C3 -C8 -環烷基、C4 -C8 -環烯基、C4 -C8 -環炔基、苯基、萘基、噻吩基和吡啶基;其中每個R7 或Z基團可任選地被一個或多個R8 基團取代; R8 選自氫、X、氰基、C1 -C6 -烷基、C2- C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C2 -C6 -鹵代炔基、SF5 、OR4 、N(R′′)2 、Si(R′)3 、(C=O)-R″、S(O)n R″、C1- C8 -烷基-S(O)n R″、C1 -C8 -烷基-(C=O)-R″、CR′=NR″、C3 -C8 -環烷基、C4 -C8 -環烯基;其中環狀環系統中的一個或多個碳原子可以被選自N、O、S基團,並且可以任選包括1-3個選自C(=O)、C(=S)、S(O)m 和Si(R′)2 的環成員的雜原子取代; R9 選自氫、C1 -C12 -烷基、C3 -C8 -環烷基、OR4 、(C=O)-R″;或農業上可接受的鹽、異構體/結構異構體、立體異構體、非對映異構體、對映異構體、互變異構體、金屬絡合物、多晶型物或其N-氧化物。
- 如請求項1所述的式(I)化合物,其中所述式(I)化合物選自((2-氯代-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-6-甲基苯基)氨基)二甲基-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)二甲基-l6-磺胺酮;1-((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)四氫-1H-1l6-噻吩1-氧化物;1-((2-氯代-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-6-甲基苯基)氨基)四氫-1H-1l6-噻吩1-氧化物;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)二甲基-l6-磺胺酮;1-((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)四氫-1H-1l6-噻吩 1-氧化物;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(3-氟苯基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(3-氟苯基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(3,5-二甲基苯基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)二乙基-l6-磺胺酮;環己基((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(甲基)(苯基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(4-甲氧基苯基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(2,6-二甲基苯基)(甲基)-l6-磺胺酮;1-((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)六氫-1l6-噻喃1-氧化物;(2-氯代-6-甲基苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)(2-甲氧基苯基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯基)氨基)二苯基-l6-磺胺酮;N-(環戊基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-(叔丁基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-甲氧基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((2-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-(烯丙基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;甲基3-(N-(4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯)-S-甲基磺醯亞胺基)丙酸酯;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(氧二苯基-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧化四氫-1l6-噻吩-1-基亞基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(二乙基(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((2-氰丙烷-2-基)(異丙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((2-氰丙烷-2-基)(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((2-氰丙烷-2-基)(異丙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異丙基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(氧代)(丙基)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(丙基)-l6-亞磺醯基)苯甲醯胺;N-((2-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-溴苯基)(環丙基甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((2-氯代-6-甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧化四氫-1l6-噻吩-1-基亞基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧化四氫-2H-1l6-噻喃-1-基亞基)苯甲醯胺;N-(環戊基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-溴苯基)(環丙基甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-(環己基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異丙基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((2-氰丙烷-2-基)(氧代)(丙基)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異丁基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異戊基(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(二甲基(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧化四氫-2H-1l6-噻喃-1-基亞基)苯甲醯胺;N-((3-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((3-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧負離子基-1l6-硫雜環丁烷基-1-基亞基)苯甲醯胺;N-((2-氰丙烷-2-基)(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異戊基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-(仲丁基(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-(環己基(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-(仲丁基(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異丁基(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(二甲基(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((2-氰丙烷-2-基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(苯基)-l6-亞磺醯基)苯甲醯胺;N-(叔丁基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-(三氟甲基)苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(4-(三氟甲氧基)苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異丁基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;2-(4-(N-(4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯)-S-甲基磺醯亞胺基)苯基)乙酸甲酯;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(4-(三氟甲氧基)苯基)-l6-亞磺醯基)苯甲醯胺;N-((2-氰丙烷-2-基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(二乙基(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(丙基)-l6-亞磺醯基)苯甲醯胺;N-(烯丙基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(異戊基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-(環己基(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異戊基(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-(三氟甲基)苯基)-l6-亞磺醯基)苯甲醯胺;2-(4-(N-(4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯)-S-甲基磺醯亞胺基)苯基)乙酸甲酯;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異丁基(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(氧二苯基-l6-亞磺醯基)苯甲醯胺;N-((3-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(2-甲氧基乙基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(1-氧負離子基-1l6-硫雜環丁烷基-1-基亞基)苯甲醯胺;N-((2-氰丙烷-2-基)(氧代)(丙基)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(氧代)(丙基)-l6-亞磺醯基)-2-甲基苯甲醯胺;甲基3-(N-(4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯)-S-甲基磺醯亞胺基)丙酸酯;N-((2-氰基乙基)(4-乙基苯基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((2-氰基乙基)(4-甲氧基苯基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((2-氰基乙基)(氧代)(間甲苯基)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((2-氰基乙基)(4-乙基苯基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(對甲苯基)-l6-亞磺醯基)苯甲醯胺;N-((4-氰基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(4-氧負離子基-1,4l6-惡噻烷-4-基亞基)苯甲醯胺;N-((4-氰基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(4-((4-(三氟甲基)吡啶-2-基)氧基)苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4,5-二甲基噻唑-2-基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(3-氟苯基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(3-氟苯基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(氧代)(間甲苯基)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基(氧代)(間甲苯基)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(4-((4-(三氟甲基)吡啶-2-基)氧基)苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((4-氰基苯基)(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-氰基苯基)(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二甲基苯基)(乙基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4,5-二甲基噻唑-2-基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;N-((4-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;N-((4-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(甲基(氧代)(苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(甲基(氧代)(間甲苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(甲基(氧代)(對甲苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,4-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;N-((4-氰基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-甲氧基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(氧二苯基-l6-亞磺醯基)苯甲醯胺;N-((2-氰丙烷-2-基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;N-((2-氰丙烷-2-基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;N-((3-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;N-((2-氯代-6-甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(甲基(氧代)(苯基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;N-((2-氯代-6-甲基苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;N-(叔丁基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;N-((2-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;N-((2-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(1-氧化四氫-2H-1l6-噻喃-1-基亞基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(氧二苯基-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-甲氧基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二甲基苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;N-((3-氯苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2,6-二氟苯基)(甲基)(氧代)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(1-氧化四氫-2H-1l6-噻喃-1-基亞基)苯甲醯胺;N-((2,6-二氯苯基)(乙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;N-((2,6-二氯苯基)(異丙基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(甲基(氧代)(4-(三氟甲基)苯基)-l6-亞磺醯基)苯甲醯胺;N-((3-溴苯基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苯甲醯胺;(4-溴苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮;(2-氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(3,5-二甲基苯基)(甲基)-l6-磺胺酮;(3-溴苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(2,6-二甲基苯基)(甲基)-l6-磺胺酮;(4-溴苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(2,6-二甲基苯基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(2,6-二氟苯基)(甲基)-l6-磺胺酮;(3-氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮;(3-氯苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮;(3-溴苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)(苯基)-l6-磺胺酮;(2-氯代-6-甲基苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)-l6-磺胺酮;(3-溴苯基)(環丙基甲基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)-l6-磺胺酮;2-(N-(4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)-S-甲基磺醯亞胺基)-2-甲基丙腈;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(吡啶-2-基)-l6-磺胺酮;(2-氯苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(4-(三氟甲基)苯基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)二苯基-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(對甲苯基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二氯苯基)(乙基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二甲基苯基)(甲基)-l6-磺胺酮;4-(N-(4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)-S-甲基磺醯亞胺基)苄腈;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(3,5-二甲基苯基)(甲基)-l6-磺胺酮;(2-氯代-6-甲基苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(3-氟苯基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(苯基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二氯苯基)(異丙基)-l6-磺胺酮;(4-溴苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮;(3-溴苯基)((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮;(3-氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮;(2-氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)二苯基-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二氟苯基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二甲基苯基)(甲基)-l6-磺胺酮;(4-溴苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(苯基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(4-(三氟甲基)苯基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(3-氟苯基)(甲基)-l6-磺胺酮; (2,6-二氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(乙基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)(吡啶-2-基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(3,5-二甲基苯基)(甲基)-l6-磺胺酮;(2,6-二氯苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(異丙基)-l6-磺胺酮;((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(2,6-二氟苯基)(乙基)-l6-磺胺酮;(3-溴苯基)((4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)苄基)氨基)(甲基)-l6-磺胺酮;4-(N-(4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)-S-甲基磺醯亞胺基)苄腈;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(甲基)(對甲苯基)-l6-磺胺酮;((4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苄基)氨基)(2,6-二氯苯基)(乙基)-l6-磺胺酮;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(丙基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(間甲苯基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(間甲苯基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異丁基亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(乙基亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(苯基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-(異丙基亞磺醯基)-2-甲基苯甲醯胺;N-(丁基亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-((3-(三氟甲基)苯基)亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-((4-(三氟甲氧基)苯基)亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-乙基苯基)亞磺醯基)-2-甲基苯甲醯胺;N-((4-(叔丁基)苯基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-乙基苯基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苯基)亞磺醯基)-2-甲基苯甲醯胺;N-((4-(叔丁基)苯基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二甲基苯基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-乙基苯基)亞磺醯基)-2-甲基苯甲醯胺;N-((3-溴苯基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苯基)亞磺醯基)-2-甲基苯甲醯胺;N-(丁基亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(丙基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(3-(甲基氨基)-3-氧丙基)(氧代)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-(異丙基氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-甲氧基苯基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((3-(環丙基氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-(環丁基氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-((2,2-二氟乙基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((3-(環丙基氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-(環丁基氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-((2,2-二氟乙基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-氧代-3-((2,2,2-三氟乙基)氨基)丙基)-l6-亞磺醯基)苯甲醯胺;N-((3-((1-氰基環丙基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-氧代-3-(丙基氨基)丙基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-(乙基(甲基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-(苄基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-氧代-3-((2,2,2-三氟乙基)氨基)丙基)-l6-亞磺醯基)苯甲醯胺;N-(苄基(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-((1-氰基環丙基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(3-氧代-3-(丙基氨基)丙基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-(乙基(甲基)氨基)-3-氧丙基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(甲基(氧代)(5-(三氟甲基)吡啶-2-基)-l6-亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-甲氧基吡啶-2-基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-甲氧基乙基)(2-甲氧基苯基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((4-氰基苄基)(甲基)(氧代)-l6-亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((6-氟吡啶-2-基)(甲基)(氧代)-l6-亞磺醯基)-2-甲基苯甲醯胺;N-((3-溴苯基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二甲基苯基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(苯基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-乙基苯基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-((4-(三氟甲氧基)苯基)亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-甲氧基苯基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(萘-2-基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-氟苯基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二氟苯基)亞磺醯基)-2-甲基苯甲醯胺;N-((4-氰基苯基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-氰基苯基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-(苄基亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-甲氧基苄基)亞磺醯基)-2-甲基苯甲醯胺;N-(苄基亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二氯苯基)亞磺醯基)-2-甲基苯甲醯胺;N-((3-氰基苯基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二氯苯基)亞磺醯基)-2-甲基苯甲醯胺;N-((4-氯苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-溴苯基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-(叔丁基)苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-氯代-3-氟苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((5-氟-2-甲基苄基)亞磺醯基)-2-甲基苯甲醯胺;N-((3-氯代-5-氟苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-氯代-5-氟苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-氯代-4-氟苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-氯苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-(叔丁基)苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二氟苯基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,4-二氯苯基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((4-甲氧基苄基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3,5-二氯苯基)亞磺醯基)-2-甲基苯甲醯胺;N-((4-溴苯基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((4-氰基苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-氰基苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;N-((3-氰基苄基)亞磺醯基)-4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-(萘-2-基亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((2-氟苯基)亞磺醯基)-2-甲基苯甲醯胺;N-((4-氰基苄基)亞磺醯基)-4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苄基)亞磺醯基)-2-甲基苯甲醯胺;4-(5-(3,5-二氯-4-氟苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-((4-(三氟甲氧基)苄基)亞磺醯基)苯甲醯胺;4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-2-甲基-N-((4-(三氟甲氧基)苄基)亞磺醯基)苯甲醯胺和4-(5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫異惡唑-3-基)-N-((3-氟苄基)亞磺醯基)-2-甲基苯甲醯胺。
- 一種控制或預防昆蟲和/或蟎蟲害的組合物,其包含生物有效量的式(I)化合物或其農學上可接受的鹽、異構體/結構異構體、立體異構體、非對映異構體、對映異構體、互變異構體、多晶型物、金屬絡合物或N-氧化物以及至少另外一種選自表面活性劑和助劑的成分。
- 如請求項5所述的組合物,其中所述組合物還包含至少一種選自殺真菌劑、殺蟲劑、殺線蟲劑、殺蟎劑、生物農藥、除草劑、植物生長調節劑、抗生素、肥料或營養素的一種生物活性相容化合物。
- 如請求項5所述的組合物,其中所述的式(I)化合物的生物學有效量的範圍為組合物總重量的0.1%-99%,優選組合物總重量的5%-50%。
- 一種組合,其包含生物有效量的如請求項1所述的化合物和至少一種選自殺真菌劑、殺蟲劑、殺線蟲劑、殺蟎劑、殺生物劑、除草劑、植物生長調節劑、抗生素、肥料和營養素的生物活性相容化合物。
- 一種對抗昆蟲和蟎類害蟲的方法,其包括用生物有效量的如請求項1或5或8所述的式(I)化合物或其鹽、金屬絡合物、N-氧化物、異構體、多晶型物、組合物或組合接觸昆蟲和蟎蟲、其棲息地、繁殖地、食物、植物、種子、土壤、無脊椎動物害蟲生長或可能生長的區域、材料或環境,或希望免受蟲害或侵擾的材料、植物、種子、土壤、表面或空間使其免受害蟲侵擾或侵染。
- 一種保護農作物免受昆蟲和蟎蟲侵襲或侵擾的方法,其包括用生物有效量的如請求項1或5或8所述的化合物或其鹽、金屬絡合物、N-氧化物、異構體、多晶型物、組合物或組合接觸農作物。
- 如請求項9或10所述的方法,其中所述方法包括在農業或園藝作物中施用有效劑量的式(I)化合物,其量為1g至5000g/公頃。
- 一種保護種子、植物和植物部分免受土壤昆蟲,以及保護幼苗根和芽免受土壤和葉面昆蟲侵擾的方法,其包括在播種前和/或在催芽後用如請求項1或5或8所述的式(I)化合物或其鹽、金屬絡合物、N-氧化物、異構體、多晶型物、組合物或組合接觸種子。
- 如請求項1或5或8所述的式(I)化合物或其鹽、金屬絡合物、N-氧化物、異構體、多晶型物、組合物或組合用於對抗農作物、園藝作物、住宅的昆蟲和蟎害蟲或控制動物細菌和寄生蟲的用途。
- 如請求項13所述的式(I)化合物的用途,其中所述農作物是穀物、玉米、高粱、八角、大米、大豆、油籽和其他豆科植物、果實和果樹、葡萄、堅果和堅果樹、柑橘和柑橘樹、任何園藝植物、葫蘆科植物、含油植物、煙草、咖啡、茶、可可、甜菜、甘蔗、棉花、土豆、番茄、洋蔥、辣椒、其他蔬菜和觀賞植物。
- 一種種子,其包含如請求項1或5或8所述的式(I)化合物或其鹽、金屬絡合物、N-氧化物、異構體、多晶型物、組合物或組合,其中式(I)化合物的量約占所述種子的重量的0.0001%-1%。
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| EP (1) | EP4021897A1 (zh) |
| AR (1) | AR119790A1 (zh) |
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| WO (1) | WO2021038501A1 (zh) |
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| CN115210221B (zh) | 2019-12-18 | 2025-03-18 | 礼蓝动物保健有限公司 | 作为农药的异噁唑啉衍生物 |
| CN115246795B (zh) * | 2021-04-26 | 2024-01-02 | 瑞普(天津)生物药业有限公司 | 4-苯基对位含有醚结构的异噁唑啉类化合物及其制备和作为杀虫、杀菌剂的应用 |
| CN115677605B (zh) * | 2021-07-21 | 2024-02-27 | 瑞普(天津)生物药业有限公司 | 一种s构型-氟雷拉纳的制备方法 |
| CN113512007A (zh) * | 2021-08-20 | 2021-10-19 | 江苏君若药业有限公司 | 氟雷拉纳的合成 |
| CN116425693B (zh) * | 2021-12-30 | 2025-06-13 | 洛阳惠中兽药有限公司 | 氟雷拉纳的制备方法、氟雷拉纳新晶型及其制备方法和应用 |
| CN117186023B (zh) * | 2023-09-18 | 2026-01-20 | 河北圣雪大成制药有限责任公司 | 一种高纯度氟雷拉纳的制备方法 |
| CN119219565B (zh) * | 2024-09-25 | 2026-02-10 | 辽宁孚音生物科技有限公司 | 一种阿福拉纳的合成方法 |
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- 2020-08-19 AR ARP200102338A patent/AR119790A1/es unknown
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- 2020-08-28 TW TW109129661A patent/TW202114999A/zh unknown
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