TWI801380B - 一種非環狀吡啶醯胺化合物作為殺真菌劑以防治在果園、葡萄藤園及農園作物中的植物病原性真菌之用途 - Google Patents
一種非環狀吡啶醯胺化合物作為殺真菌劑以防治在果園、葡萄藤園及農園作物中的植物病原性真菌之用途 Download PDFInfo
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Classifications
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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
- A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
- A01N43/40—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
-
- 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
- A01N37/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
- A01N37/18—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N<, e.g. carboxylic acid amides or imides; Thio analogues thereof
-
- 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
- A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
- A01N43/54—1,3-Diazines; Hydrogenated 1,3-diazines
-
- 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
- A01N43/64—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with three nitrogen atoms as the only ring hetero atoms
- A01N43/647—Triazoles; Hydrogenated triazoles
- A01N43/653—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
Landscapes
- Life Sciences & Earth Sciences (AREA)
- Agronomy & Crop Science (AREA)
- Pest Control & Pesticides (AREA)
- Plant Pathology (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Dentistry (AREA)
- General Health & Medical Sciences (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Environmental Sciences (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Abstract
本案揭露內容係有關於農業化學的領域,包括化合物I及其於防治在農業上有用的果園、葡萄藤園及農園中的作物之真菌疾病的用途。
Description
本申請案係請求於2017年5月2日提出申請之美國臨時專利申請案第62/500,175號之權益,其全文係以引用方式明確併入本文中。
本案揭露內容係有關於(S)-1,1-雙(4-氟苯基)丙烷-2-基(3-乙醯氧基-4-甲氧基吡啶甲醯基)-L-丙胺酸鹽用於防治在果園、葡萄藤園及農園作物中真菌疾病的用途之領域
殺真菌劑是天然或合成來源之化合物,其作用係保護與治療植物,對抗農業相關真菌引起之傷害。一般而言,沒有單一的殺真菌劑可用於所有的情況。因而持續進行製造能夠表現更好、更容易使用且成本更低的殺真菌劑之研究。
本案揭露內容是關於(S)-1,1-雙(4-氟苯基)丙烷-2-基(3-乙醯氧基-4-甲氧基吡啶甲醯基)-L-丙胺酸鹽(化合物I)及其作為殺真菌劑之用途。化合物I可提供抵抗子囊菌綱、擔子菌綱及半知菌綱的保護。
本案揭露內容之一實施例包括一種防治在植物中由病原體引發之疾病的方法,其中該植物因該病原體而有患病之風險,該方法包含將植物或植物之鄰近區域接觸一包括化合物I的組成物。
本案揭露內容之另一實施例係為化合物I用於保護植物免於植物病原性生物體侵害或是治療受到植物病原性生物體感染的植物之用途,包含施用化合物I,或是施用包括化合物I的組成物至土壤、植物、植物的一部分、葉子及/或種子。
此外,本案揭露內容之另一實施例為一種適用於保護植物免於植物病原性生物體侵害及/或治療受到植物病原性生物體感染的植物之組成物,其包含式I化合物及一植物學上可接受之載體材料。
本案揭露之化合物I可藉由各種習知技術中任一者之施用,不論是以化合物I或是以包含化合物I的製劑施用。舉例而言,化合物I可以施用至植物的根、莖、種子、花或葉子以防治各種真菌而不傷害到植物的商業價值。化合物I也可以葉面噴施、化學灌溉、土壤施灌、土壤注射、土壤噴施、土壤混合或種子處理的方式來施用。該材料可以任何一般所使用之製劑類型的形式施用,例如以溶液、粉劑、可濕性粉劑、可懸浮性濃縮劑或乳劑形式施用。
較佳地,本案揭露之化合物I係以一種包括化合物I與一植物學上可接受的載體之製劑形式施用。濃縮製劑可分散於水中或其他施用液體中,或者製劑可為粉塵狀或顆粒,其可在不進一步處理之情況下施用。該製劑可根據農業化學領域中的習用程序製備。
本案揭露內容預期使用所有的載劑,可經由該載劑配製化合物I以用於投藥並作為殺真菌劑使用。一般而言,製劑係以水懸液或乳液形式施用。這類懸浮液或乳液可由水溶性、水可懸浮性或可乳化性之製劑製作,所述製劑為固體時通常稱為可濕性粉末;或所述製劑為液體時通常稱為乳劑、水懸液或懸浮劑。應容易瞭解到,任何能將化合物I添加於其中之材料皆可使用,只要其產生所期望之效用,且不顯著干擾化合物I作為抗真菌劑的活性。
可壓製成水分散性粒劑之可濕性粉劑包含一密接混合物,其包括化合物I、一惰性載劑及表面活性劑。在可濕性粉劑中的化合物I濃度可自約10重量百分比至約90重量百分比,較佳的為約25重量百分比至約 75重量百分比,以該可濕性粉劑之總重量計。在可濕性粉劑製劑的製備中,可將化合物I與任何微細粉碎固體混配,所述固體為諸如葉蠟石、滑石、白堊、石膏、漂白土、膨潤土、鎂質膨土、澱粉、酪蛋白、麩質、蒙脫石黏土、矽藻土、純化矽酸鹽或其類似物。在此操作中,所述微細粉碎載體與表面活性劑通常是與化合物I摻合且研磨。
化合物I的乳劑可在一合適的液體中包含一慣用濃度,諸如自約10重量百分比至約50重量百分比的化合物I,以該乳劑之總重量計。化合物I可溶於一惰性載體中,所述惰性載體為水混溶性溶劑或為水不混溶性有機溶劑與乳化劑的混合物。該濃縮物可用水及油稀釋,以形成水包油乳液形式之噴灑混合物。適用的有機溶劑包括芳香族,特別是石油的高沸點萘與烯烴部分,諸如重芳族石油腦。亦可使用其他有機溶劑,例如包括松香衍生物之萜烯溶劑、脂族酮類(諸如環己酮),以及複合醇類(諸如2-乙氧基乙醇)。
在本文中可有利地採用之乳化劑,可輕易由熟習此項技術者來判定,包括各種非離子、陰離子、陽離子及兩性乳化劑,或者是二種或二種以上的乳化劑之摻合物。對製備乳劑有用的非離子乳化劑實例,包括聚烯烴二醇醚,以及烷基和芳基酚、脂族醇、脂族胺或脂肪酸與乙烯氧化物、丙烯氧化物的縮合產物,諸如乙氧基化烷基酚以及用多元醇或聚氧伸烷溶解之羧酸酯。陽離子性乳化劑包括四級銨化合物及脂肪胺鹽。陰離子性乳化劑包括烷芳基磺酸之油溶性鹽類(例如,鈣)、硫酸化聚乙二醇醚之油溶性鹽類,及磷酸化聚乙二醇醚之適宜鹽類。
可用於製備本發明化合物I乳劑之代表性有機液體為芳香族 液體,諸如二甲苯、丙基苯餾分;或混合的萘餾分、礦物油、經取代的芳香族有機液體諸如酞酸二辛酯;煤油;各種脂肪酸之二烷基醯胺,特別是脂肪二醇類以及乙二醇衍生物之二甲基醯胺,諸如二甘醇之n-丁基醚、乙基醚或甲基醚,和三甘醇之甲基醚及類似物等等。兩種或兩種以上有機液體之混合物亦可用於製備乳劑。有機液體包括二甲苯及丙基苯餾份,其中在一些情況下二甲苯是最佳的。界面活性分散劑一般用於液體製劑中,劑量自0.1至20重量百分比,以分散劑與化合物I結合的重量計。所述製劑亦可含有其他相容的添加物,例如植物生長調節劑及其他農業中的生物學上之活性化合物。
包括化合物I的水懸液,可分散於水性載劑中,濃度範圍自約5至約50重量百分比,以該水懸液之總重量計。懸浮液的製備是藉由磨細化合物I,並劇烈地將磨碎之材料混合於包含水及選自上述相同類型之表面活性劑的載劑中。亦可添加諸如無機鹽類與合成或天然膠類之其它組成成份,以增加該水性載劑的密度與黏度。
化合物I亦可以顆粒狀製劑形式施用,所述顆粒狀製劑特別適用於施用至土壤。顆粒狀製劑通常含有自約0.5至約10重量百分比之化合物I(以顆粒狀製劑之總重量計),分散於惰性載體中,該惰性載劑全部或大部分係由粗糙粉碎之惰性材料所組成,諸如鎂質膨土、膨潤土、矽藻土、黏土或相似的廉價物質。這類製劑的製備通常係將化合物I溶解於一適宜溶劑中,且將其施用至已預先製成合適粒度(自約0.5至約3mm範圍內)的顆粒狀載體。適宜溶劑為化合物I可基本上或完全溶於其中之溶劑。這類製劑的製備亦可將載體及化合物I及溶劑製成糊狀或膏狀,且壓碎並乾燥以 獲得所需的顆粒狀粒子。
含有化合物I之粉劑的製備可將呈粉末形式的化合物I與一適宜粉狀農業用載體(舉例而言諸如高嶺土、研磨火山岩及類似物)均勻混合。粉劑可合適地含有自約1至約10重量百分比的化合物I,以粉劑之總重量計。
該製劑可額外地含有輔助表面活性劑以加強化合物I的沈積、潤濕以及在目標作物與生物上之穿透力。此等輔助表面活性劑可選擇性地作為製劑組成成份或作為藥桶混合物使用。輔助表面活性劑的劑量通常在自0.01至1.0體積百分比、較佳地為0.05至0.5體積百分比之範圍內變化(以水之噴霧體積計)。合適的輔助表面活性劑包括但不限於乙氧基化壬基酚、乙氧基化合成或天然醇、酯類或磺基琥珀酸之鹽類、乙氧化基有機矽酮、乙氧基化脂肪胺以及表面活性劑與礦物或植物油之摻合物。製劑亦可包括水包油乳液,諸如在美國專利申請案第11/495,228號中所揭露者,其揭露內容係以引用方式明確併入本文中。
在某些情況中,使用飛機或直升機以空中施用的方式噴灑化合物I的製劑是有益的。這些空中施用確切的組成成份取決於要作處理的作物。對穀物作空中施用所使用的噴灑體積,較佳的係自15至50L/ha,伴隨標準散佈或穿透型的佐劑諸如非離子表面活性劑、有機矽酮或作物油,以水的噴灑體積計是以自0.05至15百分比為較佳。對長有水果之作物諸如香蕉作空中施用時,可以用較低的施用體積與較高的佐劑濃度,以黏附佐劑(sticker adjuvant)的形式施用是比較好的,諸如脂肪酸、乳膠、脂族醇、作物油和無機油。一般對結果作物的噴灑體積較佳係自15至30L/ha,伴隨高達 30%的佐劑濃度,以水的噴灑體積計。一代表性的實例可包括但不限於一23L/ha的施用體積,伴隨著30%的石蠟油黏附佐劑濃度(例如Spraytex CT)。
所述製劑可選擇性地包括含有其他農藥化合物之結合物。此等額外的農藥化合物可為殺真菌劑、殺蟲劑、除草劑、殺線蟲劑、殺蟎劑、殺節肢動物劑、殺菌劑或其之組合,其在選擇施用之介質中可與本發明之化合物相容,而不會與本案化合物的活性拮抗。因此,在這類實施例中,所述其他農藥化合物係作為增補毒劑使用,以用於相同或不同的農藥用途。化合物I及農藥化合物之結合通常可以自1:100至100:1之重量比存在。
本案揭露內容之化合物I亦可與其他殺真菌劑結合以形成殺真菌混合物及其之協同混合物。本案揭露內容之化合物I常與一或多種其他殺真菌劑結合施用以防治更廣泛多種非所欲的疾病。當與其他殺真菌劑結合使用時,本案所主張之化合物I可與其他殺真菌劑配製在一起、與其他殺真菌劑於藥桶中混合或與其他殺真菌劑依序施用。此種其他的殺真菌劑可包括2-(硫氰酸酯基甲基硫基)-苯並噻唑、2-苯酚、8-羥基奎林硫酸鹽、唑嘧菌胺(ametoctradin)、安美速(amisulbrom)、抗黴素(antimycin)、白粉寄生孢(Ampelomyces quisqualis)、阿扎康唑(azaconazole)、亞托敏(azoxystrobin)、枯草桿菌(Bacillus subtilis)、枯草桿菌菌株QST713、本達樂(benalaxyl)、免賴得(benomyl)、苯噻菌胺(benthiavalicarb-isopropyl)、苄胺基苯-磺酸(BABS)鹽、碳酸氫鹽、聯苯、葉枯唑(bismerthiazol)、比多農(bitertanol)、必殺芬(bixafen)、保米黴素(blasticidin-S)、硼砂、波爾多液(Bordeaux mixture)、白克列(boscalid)、溴克座(bromuconazole)、布瑞莫(bupirimate)、石灰硫磺(calcium polysulfide)、 四氯丹(captatol)、蓋普丹(captan)、貝芬替(carbendazim)、萎銹靈(carboxin)、加普胺(carpropamid)、香旱芹酮(carvone)、氯美查諾(chlazafenone)、地茂散(chloroneb)、四氯異苯腈(chlorothalonil)、克氯得(chlozolinate)、小盾殼黴(Coniothyrium minitans)、氫氧化銅、辛酸銅、氧氯化銅(copper oxychloride)、硫酸銅、硫酸銅(三元)、氧化亞銅、賽座滅(cyazofamid)、賽弗芬米(cyflufenamid)、克絕(cymoxanil)、環克座(cyproconazole)、環普洛(cyprodinil)、邁隆(dazomet)、咪菌威(debacarb)、亞乙基雙-(二硫胺基甲酸)二銨(diammonium ethylenebis-(dithiocarbamate))、益發靈(dichlofluanid)、二氯芬(dichlorophen)、德賽美(diclocymet)、德美井(diclomezine)、氯硝胺(dichloran)、乙黴威(diethofencarb)、待克利(difenoconazole)、野燕枯(difenzoquat ion)、二氟林(diflumetorim)、達滅芬(dimethomorph)、醚菌胺(dimoxystrobin)、戴尼唑(diniconazole)、達克利(diniconazole-M)、大脫蟎(dinobuton)、白粉克(dinocap)、二苯胺、硫醌(dithianon)、嗎菌靈(dodemorph)、嗎菌靈醋酸鹽、多果定(dodine)、多果定游離鹼、護粒松(edifenphos)、因司唑賓(enestrobin)、烯肟菌酯(enestroburin)、依普座(epoxiconazole)、噻唑菌胺(ethaboxam)、乙氧基喹因(ethoxyquin)、依得利(etridiazole)、凡殺同(famoxadone)、咪唑菌酮(fenamidone)、芬瑞莫(fenarimol)、芬克座(fenbuconazole)、甲呋醯胺(fenfuram)、環醯菌胺(fenhexamid)、腈菌胺(fenoxanil)、拌種咯(fenpiclonil)、苯鏽啶(fenpropidin)、芬普福(fenpropimorph)、胺苯吡菌酮(fenpyrazamine)、三苯錫(fentin)、三苯醋錫(fentin acetate)、三苯羥錫(fentin hydroxide)、二甲胺甲硫羥羰酸鐵(ferbam)、嘧菌腙(ferimzone)、扶吉胺(fluazinam)、護汰寧(fludioxonil)、氟嗎啉(flumorph)、氟比來(fluopicolide)、氟吡菌醯胺(fluopyram)、氟醯亞胺(fluoroimide)、氟嘧菌 酯(fluoxastrobin)、氟喹唑(fluquinconazole)、護矽得(flusilazole)、氟硫滅(flusulfamide)、氟噻菌淨(flutianil)、福多寧(flutolanil)、護汰芬(flutriafol)、氟苯吡菌胺(fluxapyroxad)、福爾培(folpet)、甲醛(formaldehyde)、福賽得(fosetyl)、福賽得鋁(fosetyl-aluminium)、麥穗寧(fuberidazole)、呋霜靈(furalaxyl)、福拉比(furametpyr)、克熱淨(guazatine)、克熱淨醋酸鹽類、GY-81六氯苯、菲克利(hexaconazole)、殺紋寧(hymexazol)、依滅列(imazalil)、依滅列硫酸鹽、易胺座(imibenconazole)、克熱淨(iminoctadine)、克熱淨三醋酸鹽、克熱淨三(烷苯磺酸鹽(albesilate))、愛得寶(iodocarb)、種菌唑(ipconazole)、愛芬吡唑酮(ipfenpyrazolone)、丙基喜樂松(iprobenfos)、依普同(iprodione)、丙森辛(iprovalicarb)、亞賜圃(isoprothiolane)、萘吡菌胺(isopyrazam)、異噻菌胺(isotianil)、嘉賜黴素(kasugamycin)、嘉賜黴素鹽酸水合物、克收欣(kresoxim-methyl)、昆布醣(laminarin)、代森錳銅(mancopper)、鋅錳乃浦(mancozeb)、曼普胺(mandipropamid)、錳乃浦(maneb)、高效甲霜靈(mefenoxam)、滅派林(mepanipyrim)、滅普寧(mepronil)、消蟎多(meptyl-dinocap)、氯化汞、氧化汞、氯化亞汞、滅達樂(metalaxyl)、右滅達樂(metalaxyl-M)、威百畝(metam)、威百畝-銨、威百畝-鉀、威百畝-鈉、滅特座(metconazole)、磺菌威(methasulfocarb)、碘甲烷(methyl iodide)、異硫氰酸甲酯(methyl isothiocyanate)、代森聯(metiram)、苯氧菌胺(metominostrobin)、美錯芬儂(metrafenone)、滅粉黴素(mildiomycin)、邁克尼(myclobutanil)、那班(nabam)、酞菌酯(nitrothal-isopropyl)、尼瑞莫(nuarimol)、辛異噻啉酮(octhilinone)、呋醯胺(ofurace)、油酸(脂肪酸類)、歐沙戳賓(orysastrobin)、歐殺斯(oxadixyl)、快得寧(oxine-copper)、咪唑反丁烯二酸鹽(oxpoconazole fumarate)、嘉保信 (oxycarboxin)、稻瘟酯(pefurazoate)、平克座(penconazole)、賽克隆(pencycuron)、戊苯吡菌胺(penflufen)、五氯酚(pentachlorophenol)、月桂酸五氯苯酯(pentachlorophenyl laurate)、吡噻菌胺(penthiopyrad)、醋酸苯基汞(phenylmercury acetate)、膦酸(phosphonic acid)、酞內酯(phthalide)、啶氧菌酯(picoxystrobin)、保粒黴素(甲)(polyoxin B)、保粒黴素(polyoxins)、保粒黴素(丁)(polyoxorim)、碳酸氫鉀(potassium bicarbonate)、羥基喹啉硫酸鉀(potassium hydroxyquinoline sulfate)、撲殺熱(probenazole)、撲克拉(prochloraz)、撲滅寧(procymidone)、普拔克(propamocarb)、普拔克鹽酸、普克利(propiconazole)、甲基鋅乃浦(propineb)、普昆日(proquinazid)、普塞康唑(prothioconazole)、百克敏(pyraclostrobin)、唑胺菌酯(pyrametostrobin)、唑菌酯(pyraoxystrobin)、白粉松(pyrazophos)、吡菌苯威(pyribencarb)、稗草畏(pyributicarb)、比芬諾(pyrifenox)、派美尼(pyrimethanil)、甲氧苯啶菌(pyriofenone)、百快隆(pyroquilon)、莫克草(quinoclamine)、快諾芬(quinoxyfen)、五氯硝基苯(quintozene)、虎杖(Reynoutria sachalinensis)萃取物、環丙吡菌胺(sedaxane)、矽噻菌胺(silthiofam)、矽氟唑(simeconazole)、2-苯基苯氧化鈉(sodium 2-phenylphenoxide)、碳酸氫鈉(sodium bicarbonate)、五氯苯氧化鈉(sodium pentachlorophenoxide)、史羅沙敏(spiroxamine)、硫、SYP-Z048、焦油類、得克利(tebuconazole)、異丁乙氧喹啉(tebufloquin)、四氯硝基苯(tecnazene)、四克利(tetraconazole)、腐絕(thiabendazole)、賽氟滅(thifluzamide)、甲基多保淨(thiophanate-methyl)、得恩地(thiram)、泰汀尼(tiadinil)、脫克松(tolclofos-methyl)、甲基益發靈(tolylfluanid)、三泰芬(triadimefon)、三泰隆(triadimenol)、咪唑(triazoxide)、三賽唑(tricyclazole)、三得芬(tridemorph)、三氟敏(trifloxystrobin)、賽福座 (triflumizole)、賽福寧(triforine)、、氫氧化三苯錫(triphenyltin hydroxide)、滅菌唑(triticonazole)、維利黴素(validamycin)、伐利芬那雷特(valifenalate)、霜黴滅(valiphenal)、免克寧(vinclozolin)、代森鋅(zineb)、福美鋅(ziram)、座賽胺(zoxamide)、嗜油假絲酵母(Candida oleophila)、尖鐮孢菌(Fusarium oxysporum)、膠狀青黴菌(Gliocladium)種、大格孢伏革菌(Phlebiopsis gigantea)、淺灰綠鏈黴菌(Streptomyces griseovirids)、木真菌屬(Trichoderma)種、(RS)-N-(3,5-二氯苯基)-2-(甲氧基甲基)-琥珀醯亞胺、1,2-二氯丙烷、1,3-二氯-1,1,3,3-四氟丙酮水合物、1-氯-2,4-二硝萘、1-氯-2-硝基丙烷、2-(2-十七基-2-咪唑啉-1-基)乙醇、2,3-二氫-5-苯基-1,4-噻1,1,4,4-四氧化物、醋酸2-甲氧基乙基汞(2-methoxyethylmercury acetate)、氯化2-甲氧基乙基汞(2-methoxyethylmercury chloride)、矽酸2-甲氧基乙基汞(2-methoxyethylmercury silicate)、3-(4-氯苯基)-5-甲基若丹林、硫氰酸4-(2-硝基丙-1-烯基)苯酯、亞米諾皮瑞芬(aminopyrifen)、胺丙膦酸(ampropylfos)、敵菌靈(anilazine)、氧化福美雙(azithiram)、多硫化鋇、拜耳(Bayer)32394、麥銹靈(benodanil)、敵菌腙(benquinox)、苯噻菌脲(bentaluron)、苯馬克(benzamacril);苯馬克-異丁基、抑菌啉(benzamorf)、苯並烯氟菌唑(benzovindiflupyr)、百蟎克(binapacryl)、硫酸雙(甲基汞)、氧化雙(三丁基錫)、得滅多(buthiobate)、鎘鈣銅鋅的鉻酸硫酸鹽(cadmium calcium copper zinc chromate sulfate)、嗎菌威(carbamorph)、CECA、克氯綜(chlobenthiazone)、雙胺靈(chloraniformethan)、克羅芬唑(chlorfenazole)、四氯喹喔啉(chlorquinox)、甘寶素(climbazole)、雙(3-苯基柳酸)銅、銅鋅的鉻酸鹽、丁香菌酯(coumoxystrobin)、硫雜靈(cufraneb)、硫酸肼銅(cupric hydrazinium sulfate)、福美銅氯(cuprobam)、環菌胺(cyclafuramid)、伏賜丁 (cypendazole)、酯菌胺(cyprofuram)、癸磷錫(decafentin)、戴克羅本提亞薩克斯(dichlobentiazox)、二氯萘醌(dichlone)、賜克滅(dichlozoline)、苄氯三唑醇(diclobutrazol)、二甲嘧酚(dimethirimol)、敵菌死消(dinocton)、硝辛酯(dinosulfon)、硝丁酯(dinoterbon)、大芬滅替松(dipymetitrone)、雙吡硫翁(dipyrithione)、普得松(ditalimfos)、多地辛(dodicin)、肼菌酮(drazoxolon)、EBP、烯肟菌酯(enoxastrobin)、ESBP、乙環唑(etaconazole)、益地安(etem)、乙嘧酚(ethirim)、敵磺鈉(fenaminosulf)、烯肟菌胺(fenaminstrobin)、咪菌腈(fenapanil)、種衣酯(fenitropan)、芬皮卡克斯米德(fenpicoxamid)、氟茚唑菌胺(fluindapyr)、氟醚菌醯胺(fluopimomide)、三氟苯唑(fluotrimazole)、氟菌蟎酯(flufenoxystrobin)、二甲呋醯胺(furcarbanil)、呋菌唑(furconazole)、順式呋菌唑、拌種胺(furmecyclox)、呋甲硫菌靈(furophanate)、果綠定(glyodine)、灰黃黴素(griseofulvin)、丙烯酸喹啉酯(halacrinate)、海克力斯(Hercules)3944、海西硫弗(hexylthiofos)、ICIA0858、英皮若浮樂森(inpyrfluxam)、依普芬三氟康納唑(ipfentrifluconazole)、伊皮浮樂芬諾金(ipflufenoquin)、異丙噻菌胺(isofetamid)、艾索浮樂賽普瑞(isoflucypram)、艾索帕夫(isopamphos)、異醯菌酮(isovaledione)、曼德斯綽賓(mandestrobin)、巴斯丹(mebenil)、苯并威(mecarbinzid)、氯氟醚菌唑(mefentrifluconazole)、間氯敵菌酮(metazoxolon)、呋菌胺(methfuroxam)、甲基汞雙氰胺(methylmercury dicyandiamide)、噻菌胺(metsulfovax)、美透帖綽波(metyltetraprole)、代森環(milneb)、黏氯酸酐(mucochloric anhydride)、滅克寧(myclozolin)、N-3,5-二氯苯基-琥珀醯亞胺、N-3-硝苯基伊康醯亞胺(nitrophenylitaconimide)、納他黴素(natamycin)、N-乙基汞基-4-甲苯磺醯苯胺、雙(二甲基二硫代胺基甲酸)鎳、OCH、氟噻唑吡乙酮 (oxathiapiprolin)、二甲基二硫代胺基甲酸苯基汞、(phenylmercury dimethyldithiocarbamate)、硝酸苯基汞(phenylmercury nitrate)、氯瘟磷(phosdiphen)、皮卡布西(picarbutrazox)、菌威(prothiocarb);硫菌威鹽酸、氟唑菌醯羥胺(pydiflumetofen)、吡喃靈(pyracarbolid)、派瑞頗波因(pyrapropoyne)、必記福敏(pyraziflumid)、派瑞達奇拉米堤(pyridachlometyl)、定菌腈(pyridinitril)、啶菌唑(pyrisoxazole)、氯甲氧吡啶(pyroxychlor)、氯吡呋醚(pyroxyfur)、喹烯酮(quinacetol);喹烯酮硫酸鹽、醌菌腙(quinazamid)、氯苯喹唑(quinconazole)、昆諾浮美林(quinofumelin)、吡咪唑(rabenzazole)、柳醯胺苯(salicylanilide)、SSF-109、戊苯碸(sultropen)、福美雙聯(tecoram)、氟噻亞菌胺(thiadifluor)、噻菌腈(thicyofen)、硫氯苯亞胺(thiochlorfenphim)、苯硫脲酯(thiophanate)、克殺蟎(thioquinox)、替歐西密(tioxymid)、威菌磷(triamiphos)、嘧菌醇(triarimol)、丁三唑(triazbutil)、水楊菌胺(trichlamide)、氯啶菌酯(triclopyricarb)、三氟苯嘧啶(triflumezopyrim)、毋紋(urbacid)、氰菌胺(zarilamid)以及任何其之結合。
此外,本發明之化合物I可與其他農藥結合,包括在選擇施用之介質中可與本發明之化合物I相容而不拮抗化合物I之活性的殺蟲劑、殺線蟲劑、殺蟎劑、殺節肢動物劑、殺菌劑或其之組合,以形成農藥混合物及其之協同混合物。本案揭露內容之化合物I可與一或多種其他農藥結合施用,以防治更廣泛多種非所欲的害蟲。當與其他農藥結合使用時,本案主張之化合物I可與其他農藥配製在一起、與其他農藥在藥桶中混合或與其他農藥依序施用。常見的殺蟲劑包括但不限於:抗生素類殺蟲劑,諸如阿洛胺菌素(allosamidin)及蘇力菌素(thuringiensin);巨環內酯殺蟲劑殺蟲劑,諸 如賜諾殺(spinosad)及賜諾特(spinetoram);艾維美丁(avermectin)殺蟲劑,諸如阿維菌素(abamectin)、多拉菌素(doramectin)、埃瑪菌素(emamectin)、依普菌素(eprinomectin)、伊維菌素(ivermectin)和西拉菌素(selamectin);密滅汀(milbemycin)殺蟲劑,諸如雷匹美汀(lepimectin)、密滅汀(milbemectin)、倍脈心肟(milbemycin oxime)及莫昔克丁(moxidectin);胺基甲酸鹽類殺蟲劑,諸如免敵克(bendiocarb)及加保利(carbaryl);苯並呋喃甲基胺基甲酸鹽類殺蟲劑,諸如免扶克(benfuracarb)、加保扶(carbofuran)、丁基加保扶(carbosulfan)、一甲呋喃丹(decarbofuran)及呋線威(furathiocarb);二甲基胺基甲酸鹽殺蟲劑氮芥(dimitan)、敵蠅威(dimetilan)、亥喹卡(hyquincarb)及比加普(pirimicarb);肟類胺基甲酸鹽殺蟲劑,諸如棉鈴威(alanycarb)、得滅克(aldicarb)、碸滅威(aldoxycarb)、佈嘉信(butocarboxim)、氧丁叉威(butoxycarboxim)、納乃得(methomyl)、戊腈威(nitrilacarb)、歐殺滅(oxamyl)、噻蟎威(tazimcarb)、抗蟲威(thiocarboxime)、硫敵克(thiodicarb)及硫伐隆(thiofanox);苯甲酸胺基甲酸類殺蟲劑,諸如除害威(allyxycarb)、滅害威(aminocarb)、合殺威(bufencarb)、畜蟲威(butacarb)、氯滅殺威(carbanolate)、除線威(cloethocarb)、聯甲苯(dicresyl)、二氧威(dioxacarb)、EMPC、乙硫苯威(ethiofencarb)、雙乙威(fenethacarb)、丁基滅必蝨(fenobucarb)、滅必虱(isoprocarb)、滅賜克(methiocarb)、治滅蝨(metolcarb)、茲克威(mexacarbate)、蜱虱威(promacyl)、猛殺威(promecarb)、安丹(propoxur)、混滅威(trimethacarb)、XMC及滅爾蝨(xylylcarb);乾燥劑類殺蟲劑,諸如硼酸、矽藻土(diatomaceous earth)及矽膠(silica gel);醯二胺類殺蟲劑,諸如溴蟲氟苯雙醯胺(broflanilide)、剋安勃(chlorantraniliprole)、氰蟲醯胺(cyantraniliprole)、環溴蟲醯胺(cyclaniliprole)、氯氟氰蟲醯胺 (cyhalodiamide)、福本胺(flubendiamide)、四氯蟲醯胺(tetrachlorantraniliprole)及氟氰虫酰胺(tetraniliprole);二芳基異噁唑(diarylisoxazoline)殺蟲劑,諸如氟米塔麥(fluxametamide;二硝基酚類殺蟲劑,諸如消蟎酚(dinex)、硝丙酚(dinoprop)、戊硝酚(dinosam)及DNOC;氟類殺蟲劑,諸如六氟矽酸鋇(barium hexafluorosilicate)、冰晶石(cryolite)、氟化鈉、六氟矽酸鈉及氟蟲胺(sulfluramid);甲脒類殺蟲劑,諸如三亞蟎(amitraz)、殺蟲脒(chlordimeform)、複滅蟎(formetanate)及藻蟎滅(formparanate);燻蒸類殺蟲劑,諸如烯腈(acrylonitrile)、二硫化碳(carbon disulfide)、四氯化碳(carbon tetrachloride)、氯仿(chloroform)、氯化苦(chloropicrin)、對-二氯苯(para-dichlorobenzene)、1,2-二氯丙烷、甲酸乙酯(ethyl formate)、二溴乙烯(ethylene dibromide)、二氯乙烷(ethylene dichloride)、環氧乙烷(ethylene oxide)、氰化氫(hydrogen cyanide)、碘甲烷(iodomethane)、溴甲烷(methyl bromide)、甲基氯仿(methylchloroform)、二氯甲烷(methylene chloride)、萘(naphthalene)、膦(phosphine)、硫醯氟(sulfuryl fluoride)及四氯乙烷(tetrachloroethane);無機類殺蟲劑,諸如硼砂、多硫化鈣(calcium polysulfide)、油酸銅、氯化亞汞(mercurous chloride)、硫氰酸鉀(potassium thiocyanate)及硫氰酸鈉(sodium thiocyanate);幾丁質合成抑制劑,諸如雙三氟蟲脲(bistrifluron)、佈芬淨(buprofezin)、克福隆(chlorfluazuron)、賽滅淨(cyromazine)、二福隆(diflubenzuron)、氟環脲(flucycloxuron)、氟芬隆(flufenoxuron)、六伏隆(hexaflumuron)、祿芬隆(lufenuron)、諾瓦隆(novaluron)、紐伏隆(noviflumuron)、氟幼脲(penfluron)、得福隆(teflubenzuron)及殺蟲隆(triflumuron);青春激素類似物,諸如保幼醚(epofenonane)、苯氧威(fenoxycarb)、烯蟲乙酯(hydroprene)、烯蟲炔酯(kinoprene)、美賜平 (methoprene)、百利普芬(pyriproxyfen)及烯蟲硫酯(triprene);青春激素(juvenile hormones),諸如青春激素I、青春激素II及青春激素III;介離子(mesoionic)類殺蟲劑,諸如二氯滅座替(dicloromezotiaz)及三氟苯嘧啶(triflumezopyrim);脫皮激素結合劑,諸如可芬諾(chromafenozide)、氯蟲醯肼(halofenozide)、滅芬諾(methoxyfenozide)及得芬諾(tebufenozide);脫皮激素,諸如α-蛻皮激素及蛻皮甾酮(ecdysterone);脫皮抑制劑(moulting inhibitors),諸如如二苯丙醚(diofenolan);早熟素類劑(precocenes),諸如早熟素I、早熟素II及早熟素III;未分類的昆蟲生長調節劑,諸如環蟲腈(dicyclanil);沙蠶毒類似物(nereistoxin analogue)殺蟲劑,諸如免速達(bensultap)、培丹(cartap)、硫賜安(thiocyclam)及殺蟲雙(thiosultap);吡啶基吡唑(pyridylpyrazole)殺蟲劑,諸如泰可羅皮拉則浮羅(tyclopyrazoflor);尼古丁類殺蟲劑,諸如氟尼胺(flonicamid);硝基胍類殺蟲劑,諸如可尼丁(clothianidin)、達特南(dinotefuran)、益達胺(imidacloprid)及賽速安(thiamethoxam);硝基亞甲基類殺蟲劑,諸如烯啶蟲胺(nitenpyram)及硝基亞秦(nithiazine);胺甲基吡啶類殺蟲劑,諸如亞滅培(acetamiprid)、環氧蟲啶(cycloxaprid)、益達胺(imidacloprid)、烯啶蟲胺(nitenpyram)及賽果培(thiacloprid);有機氯類殺蟲劑,諸如溴-DDT、殺芬(camphechlor)、DDT、pp′-DDT、乙基-DDD、HCH、γ-HCH(gamma-HCH)、林丹(lindane)、甲氧氯(methoxychlor)、五氯苯酚(pentachlorophenol)及TDE;環雙烯類殺蟲劑,諸如阿特靈(aldrin)、保滿丹(bromocyclen)、冰片丹(chlorbicyclen)、氯丹(chlordane)、開蓬(chlordecone)、狄氏劑(dieldrin)、滴露(dilor)、安殺番(endosulfan)、α-安殺番(alpha-endosulfan)、異狄氏劑(endrin)、HEOD、七氯(heptachlor)、HHDN、碳氯靈(isobenzan)、異艾氏劑(isodrin)、氯 戊環(kelevan)和滅蟻靈(mirex);有機磷類殺蟲劑,諸如溴苯烯磷(bromfenvinfos)、氯芬松(chlorfenvinphos)、丁烯磷(crotoxyphos)、二氯松(dichlorvos)、雙特松(dicrotophos)、二甲基毒蟲畏(dimethylvinphos)、福司吡酯(fospirate)、庚烯磷(heptenophos)、蟲殺乙烯磷(methocrotophos)、美文松(mevinphos)、亞素靈(monocrotophos)、乃力松(naled)、萘肽磷(naftalofos)、福賜米松(phosphamidon)、丙蟲磷(propaphos)、TEPP及樂本松(tetrachlorvinphos);有機硫磷類殺蟲劑,諸如蔬果磷(dioxabenzofos)、丁苯硫磷(fosmethilan)及賽達松(phenthoate);直鏈烷有機硫代磷酸鹽類殺蟲劑,諸如家蠅磷(acethion)、胺吸磷(amiton)、硫線磷(cadusafos)、壤土氯磷(chlorethoxyfos)、氯甲磷(chlormephos)、田樂磷(demephion)、田樂磷-O、田樂磷-S、內吸磷(demeton)、內吸磷-O、內吸磷-S、內吸磷-甲基、內吸磷-O-甲基、內吸磷-S-甲基、內吸磷-S-甲基硫、二硫松(disulfoton)、愛殺松(ethion)、普伏松(ethoprophos)、IPSP、獲賜松(isothioate)、馬拉松(malathion)、蟲蟎畏(methacrifos)、碸吸磷-甲基(oxydemeton-methyl)、異亞碸磷(oxydeprofos)、碸拌磷(oxydisulfoton)、福瑞松(phorate)、治螟磷(sulfotep)、託福松(terbufos)及硫滅松(thiometon);直鏈胺有機硫代磷酸鹽殺蟲劑,諸如賽果(amidithion)、果蟲磷(cyanthoate)、大滅松(dimethoate)、益硫磷-甲基(ethoate-methyl)、安果(formothion)、滅加松(mecarbam)、毆滅松(omethoate)、發果(prothoate)、蘇果(sophamide)及繁米松(vamidothion);肟基有機硫代磷酸鹽類殺蟲劑,諸如氯腈肟磷(chlorphoxim)、巴賽松(phoxim)及巴賽松-甲基(phoxim-methyl);雜環有機硫代磷酸鹽類殺蟲劑,諸如唑啶磷(azamethiphos)、蠅毒磷(coumaphos)、畜蟲磷(coumithoate)、敵殺磷(dioxathion)、內毒磷(endothion)、滅蚜松(menazon)、茂果(morphothion)、 裕必松(phosalone)、吡唑硫磷(pyraclofos)、必芬松(pyridaphenthion)及畜寧磷(quinothion);苯並噻喃有機硫代磷酸鹽類殺蟲劑,諸如苯噻乙雙硫磷(dithicrofos)及苯噻硫磷(thicrofos);苯並三嗪有機硫代磷酸鹽類殺蟲劑,諸如益棉磷(azinphos-ethyl)及保棉磷(azinphos-methyl);異吲哚有機硫代磷酸鹽類殺蟲劑,諸如氯亞磷(dialifos)及益滅松(phosmet);異噁唑有機硫代磷酸鹽類殺蟲劑,諸如加福松(isoxathion)及丙硫噁唑磷(zolaprofos);吡唑並嘧啶有機硫代磷酸鹽類殺蟲劑,諸如氯吡唑磷(chlorprazophos)及白粉松(pyrazophos);吡啶有機硫代磷酸鹽類殺蟲劑,諸如陶斯松(chlorpyrifos)及陶斯松-甲基(chlorpyrifos-methyl);嘧啶有機硫代磷酸鹽類殺蟲劑,諸如特嘧硫磷(butathiofos)、大利松(diazinon)、乙氧嘧啶磷(etrimfos)、丙嘧啶磷(lirimfos)、蟲蟎磷-乙基(pirimiphos-ethyl)、蟲蟎磷-甲基(pirimiphos-methyl)、乙醯嘧啶磷(primidophos)、嘧硫磷(pyrimitate)及丁基嘧啶磷(tebupirimfos);苯並吡嗪有機硫代磷酸鹽類殺蟲劑,諸如拜裕松(quinalphos)及拜裕松-甲基(quinalphos-methyl);噻二唑有機硫代磷酸鹽類殺蟲劑,諸如艾噻達松(athidathion)、噻唑磷(lythidathion)、滅大松(methidathion)及乙噻唑磷(prothidathion);三唑有機硫代磷酸鹽類殺蟲劑,諸如依殺松(isazofos)及三落松(triazophos);苯基有機硫代磷酸鹽類殺蟲劑,諸如偶氮磷(azothoate)、溴硫磷(bromophos)、溴硫磷-乙基(bromophos-ethyl)、三硫磷(carbophenothion)、氯甲硫磷(chlorthiophos)、氰乃松(cyanophos)、賽滅磷(cythioate)、異氯磷(dicapthon)、除線磷(dichlofenthion)、丙硫磷(etaphos)、伐滅磷(famphur)、皮蠅磷(fenchlorphos)、撲滅松(fenitrothion)、繁福松(fensulfothion)、芬殺松(fenthion)、芬殺松-乙基(fenthion-ethyl)、速殺硫磷(heterophos)、碘硫磷 (jodfenphos)、倍硫磷亞碸(mesulfenfos)、巴拉松(parathion)、巴拉松-甲基(parathion-methyl)、芬硫磷(phenkapton)、對氯硫磷(phosnichlor)、佈飛松(profenofos)、普硫松(prothiofos)、硫丙磷(sulprofos)、亞培松(temephos)、三氯偏磷酸-3(trichlormetaphos-3)及三氯丙氧磷(trifenofos);膦酸鹽類殺蟲劑,諸如丁酯磷(butonate)及三氯松(trichlorfon);硫代磷酸鹽類殺蟲劑,諸如甲基滅蚜磷(mecarphon);苯基乙基硫代磷酸鹽類殺蟲劑,諸如地蟲磷(fonofos)及壤蟲磷(trichloronat);苯基苯基硫代磷酸鹽類殺蟲劑,諸如苯腈磷(cyanofenphos)、EPN及福賜松(leptophos);胺基磷酸鹽類殺蟲劑,諸如克蘆磷酯(crufomate)、芬滅松(fenamiphos)、丁硫環磷(fosthietan)、二噻磷(mephosfolan)、棉安磷(phosfolan)及甲胺基嘧啶磷(pirimetaphos);硫磷醯胺類殺蟎劑殺蟲劑,諸如歐殺松(acephate)、水胺硫磷(isocarbophos)、亞芬松(isofenphos)、亞芬松-甲基(isofenphos-methyl)、達馬松(methamidophos)及巴胺磷(propetamphos);磷醯胺類殺蟲劑,諸如甲氟磷(dimefox)、疊氮磷(mazidox)、丙胺氟磷(mipafox)及八甲磷(schradan);噁二嗪類殺蟲劑,諸如因得克(indoxacarb);噁二唑啉(oxadiazoline)殺蟲劑,諸如噁蟲酮(metoxadiazone);鄰苯二甲醯亞胺類殺蟲劑,諸如氯亞磷(dialifos)、益滅松(phosmet)及胺菊酯(tetramethrin);吡唑類殺蟲劑,諸如吡蟎胺(tebufenpyrad)、唑蟲醯胺(tolefenpyrad);苯吡唑類殺蟲劑,諸如乙醯蟲腈(acetoprole)、乙蟲清(ethiprole)、芬普尼(fipronil)、吡氟普羅(pyrafluprole)、皮瑞普(pyriprole)及萬尼普(vaniliprole);除蟲菊酯類殺蟲劑,諸如阿納寧(acrinathrin)、亞列寧(allethrin)、反式丙烯除蟲菊(bioallethrin)、熏蟲菊(barthrin)、畢芬寧(bifenthrin)、κ-畢芬寧(kappa-bifenthrin)、生物乙酸次甲酯(bioethanomethrin)、右旋反式氯丙炔菊酯(chloroprallethrin)、環蟲菊 (cyclethrin)、乙氰菊酯(cycloprothrin)、賽扶寧(cyfluthrin)、β-賽扶寧(beta-cyfluthrin)、賽洛寧(cyhalothrin)、γ-賽洛寧(gamma-cyhalothrin)、λ-賽洛寧(lambda-cyhalothrin)、賽滅寧(cypermethrin)、α-賽滅寧、β-賽滅寧、θ-賽滅寧、ζ-賽滅寧、賽酚寧(cyphenothrin)、第滅寧(deltamethrin)、四氟甲醚菊酯(dimefluthrin)、苄菊酯(dimethrin)、烯炔菊酯(empenthrin)、芬氟司林(fenfluthrin)、吡氯氰菊酯(fenpirithrin)、芬普寧(fenpropathrin)、芬化利(fenvalerate)、高氰戊菊酯(esfenvalerate)、護賽寧(flucythrinate)、氟胺氰菊酯(fluvalinate)、福化利(tau-fluvalinate)、糠醛菊酯(furethrin)、右旋七氟甲醚菊酯(heptafluthrin)、炔咪菊酯(imiprothrin)、氯氟醚菊酯(meperfluthrin)、甲氧苄氟菊酯(metofluthrin)、ε-甲氧苄氟菊酯(epsilon-metofluthrin)、麻浮落羅西(momfluorothrin)、ε-麻浮落羅西(epsilon-momfluorothrin)、百滅寧(permethrin)、生物氯菊酯(biopermethrin)、反氯菊酯(transpermethrin)、酚丁滅蝨(phenothrin)、炔丙菊酯(prallethrin)、丙氟菊酯(profluthrin)、苄呋菊酯(pyresmethrin)、苄呋菊酯(resmethrin)、生物苄呋菊酯(bioresmethrin)、順式苄呋菊酯(cismethrin)、七氟菊酯(tefluthrin)、κ-七氟菊酯(kappa-tefluthrin)、環戊烯丙菊酯(terallethrin)、胺菊酯(tetramethrin)、四氟醚菊酯(tetramethylfluthrin)、泰滅甯(tralomethrin)及四氟苯菊酯(transfluthrin);合成除蟲菊醚殺蟲劑,諸如依芬寧(etofenprox)、三氟醚菊酯(flufenprox)、合芬寧(halfenprox)、丙苯烴菊酯(protrifenbute)及矽護芬(silafluofen);嘧啶胺殺蟲劑,諸如氟芬林(flufenerim)及畢汰芬(pyrimidifen);吡咯殺蟲劑,諸如克凡派(chlorfenapyr);季酮酸(tetramic acid)殺蟲劑,諸如斯拜羅皮地恩(spiropidion)及賜派滅(spirotetramat);酮基丁內酯(tetronic acid)殺蟲劑,諸如螺甲蟎酯(spiromesifen);硫脲類殺蟲劑,諸如汰芬隆 (diafenthiuron);尿素類殺蟲劑,諸如氟氰戊菊酯(flucofuron)及舒可夫隆(sulcofuron);未分類的殺線蟲劑(unclassified nematicides),諸如衛絡星(fluazaindolizine)及替奧沙芬(tioxazafen);及未分類的殺蟲劑,諸如本茲皮瑞麻克森(benzpyrimoxan)、氯生太爾(closantel)、烷酸銅(copper naphthenate)、克羅米通(crotamiton)、EXD、抗蟎唑(fenazaflor)、嘧醯蟲胺(fenoxacrim)、氰基硫醚類殺蟲劑(fluhexafon)、福勒皮理名(flupyrimin)、伏蟻腙(hydramethylnon)、亞賜圃(isoprothiolane)、丁苄腈(malonoben)、美氟腙(metaflumizone)、伏蟻靈(nifluridide)、亞西茲歐縮浮(oxazolsulfyl)、三氯殺蟲酯(plifenate)、畢達本(pyridaben)、啶蟲丙醚(pyridalyl)、哌氟喹腙(pyrifluquinazon)、碘醚柳胺(rafoxanide)、氟啶蟲胺腈(sulfoxaflor)、苯蟎噻(triarathene)及唑蚜威(triazamate)及任何其之結合。
此外,本發明之化合物I可與其他除草劑結合以形成農藥混合物以及其之協同混合物,其中該其他除草劑在選擇施用之介質中可與本發明之化合物I相容而不與化合物I之活性拮抗。本案揭露之殺真菌性化合物I可與一或多種除草劑結合施用,以防治更廣泛多種之非所欲的植物。當與其他除草劑結合使用時,本申請主張之化合物I可與其他除草劑配製在一起、與其他除草劑於藥桶中混合或與其他除草劑依序施用。代表性的除草劑包括但不限於:醯胺類除草劑諸如草毒死(allidochlor)、氟丁醯草胺(beflubutamid)、胺酸殺(benzadox)、苄草胺(benzipram)、溴丁醯草胺(bromobutide)、苯酮唑(cafenstrole)、CDEA、三環噻草胺(cyprazole)、汰草滅(dimethenamid)、汰草滅-P(dimethenamid-P)、大芬滅(diphenamid)、三唑磺(epronaz)、艾尼丙密(etnipromid)、四唑醯草胺(fentrazamide)、氟胺草唑 (flupoxam)、氟磺胺草醚(fomesafen)、鹵索芬(halosafen)、丁脒醯胺(isocarbamid)、異噁草胺(isoxaben)、滅落脫(napropamide)、納得爛(naptalam)、烯草胺(pethoxamid)、戊炔草胺(propyzamide)、氯藻胺(quinonamid)、胺草磷(tebutam)及氟丙嘧草酯(tiafenacil);苯甲醯胺類除草劑諸如地快樂(chloranocryl)、咯草隆(cisanilide)、稗草胺(clomeprop)、環草胺(cypromid)、吡氟醯草胺(diflufenican)、乙氧苯草胺(etobenzanid)、芬磺草靈(fenasulam)、氟噻草胺(flufenacet)、氟芬尼康(flufenican)、滅芬草(mefenacet)、氟磺醯胺草(mefluidide)、噁唑醯草胺(metamifop)、庚草利(monalide)、萘普草(naproanilide)、蔬草滅(pentanochlor)、氟吡草胺(picolinafen)及除草靈(propanil);苯丙胺酸類除草劑諸如新燕靈(benzoylprop)、麥草伏(flamprop)及麥草伏-M(flamprop-M);氯乙醯苯胺類除草劑,諸如乙草胺(acetochlor)、拉草(alachlor)、丁基拉草(butachlor)、丁烯草胺(butenachlor)、異丁草胺(delachlor)、乙醯甲草胺(diethatyl)、二甲草胺(dimethachlor)、滅草胺(metazachlor)、莫多草(metolachlor)、S-莫多草(S-metolachlor)、普拉草(pretilachlor)、雷蒙得(propachlor)、異丙草胺(propisochlor)、丙炔草胺(prynachlor)、特丁草胺(terbuchlor)、欣克草(thenylchlor)及二甲苯草胺(xylachlor);硫代苯甲醯胺類除草劑,諸如氟磺胺草(benzofluor)、黃草伏(perfluidone)、嘧啶硫蕃(pyrimisulfan)及氟唑草胺(profluazol);磺胺類除草劑諸如亞速爛(asulam)、卡巴草靈(carbasulam)、芬磺草靈(fenasulam)及毆拉靈(oryzalin);硫代醯胺類除草劑諸如草克樂(chlorthamid);抗生素類除草劑諸如畢拉草(bilanafos);苯甲酸類除草劑諸如克爛本(chloramben)、汰克草(dicamba)、2,3,6-TBA及殺草畏(tricamba);嘧氧苯甲酸類除草劑諸如雙草醚(bispyribac)及嘧草醚(pyriminobac);嘧啶硫代苯 甲酸類除草劑諸如嘧硫草醚(pyrithiobac);鄰苯二酸類除草劑諸如敵草索(chlorthal);甲酸吡啶類除草劑諸如氯胺基吡啶酸(aminopyralid)、畢克草(clopyralid)、氯氟吡啶酯(florpyrauxifen)、氟氯吡啶酯(halauxifen)及畢克爛(picloram);喹啉羧酸類除草劑諸如快克草(quinclorac)及喹草酸(quinmerac);砷類除草劑諸如二甲胂酸(cacodylic acid)、CMA、DSMA、六氟砷(hexaflurate)、MAA、MAMA、MSMA、亞砷酸鉀(potassium arsenite)及亞砷酸鈉(sodium arsenite);苯甲醯環己二酮類除草劑諸如芬昆諾三酮(fenquinotrione)、藍三酮(lancotrione)、甲基磺草酮(mesotrione)、磺草酮(sulcotrione)、特糠酯酮(tefuryltrione)及環磺酮(tembotrione);烷基磺酸苯並呋喃類除草劑,諸如呋草磺(benfuresate)及益覆滅(ethofumesate);苯併噻唑類除草劑諸如草除靈(benzazolin);胺基甲酸鹽類除草劑諸如亞速爛(asulam)、異噁甲草威(carboxazole chlorprocarb)、苄胺靈(dichlormate)、芬磺草靈(fenasulam)、卡草靈(karbutilate)及芽根靈(terbucarb);苯基胺基甲酸類除草劑諸如燕麥靈(barban)、BCPC、卡巴草靈(carbasulam)、長殺草(carbetamide)、CEPC、氯炔靈(chlorbufam)、氯苯胺靈(chlorpropham)、CPPC、甜菜安(desmedipham)、棉胺寧(phenisopham)、甜菜寧(phenmedipham)、甜菜寧-乙基(phenmedipham-ethyl)、苯胺靈(propham)及滅草靈(swep);環己烯肟類除草劑,諸如亞汰草(alloxydim)、丁苯草酮(butroxydim)、克草同(clethodim)、氯丙氧定(cloproxydim)、環殺草(cycloxydim)、環苯草酮(profoxydim)、西殺草(sethoxydim)、得殺草(tepraloxydim)及苯草酮(tralkoxydim);環丙基異噁唑類除草劑,諸如異噁氯妥(isoxachlortole)及異噁唑草酮(isoxaflutole);二甲醯亞胺類除草劑,諸如吲哚酮草酯(cinidon-ethyl)、氟默嗪(flumezin)、氟胺草酯 (flumiclorac)、丙炔氟草胺(flumioxazin)及炔草胺(flumipropyn);二硝基苯胺類除草劑,諸如倍尼芬(benfluralin)、比達寧(butralin)、撻乃安(dinitramine)、丁氟消草(ethalfluralin)、氟消草(fluchloralin)、異樂靈(isopropalin)、美索丙鉑林(methalpropalin)、滅殺草(nitralin)、毆拉靈(oryzalin)、施得圃(pendimethalin)、苯胺靈(prodiamine)、環丙氟靈(profluralin)及三福林(trifluralin);二硝基酚類除草劑,諸如消草酯(dinofenate)、硝丙酚(dinoprop)、戊硝酚(dinosam)、達諾殺(dinoseb)、特樂酚(dinoterb)、DNOC、硝草酚(etinofen)及地樂施(medinoterb);二苯醚類除草劑,諸如氯氟草醚(ethoxyfen);硝基苯醚類除草劑,諸如亞喜芬(acifluorfen)、苯草醚(aclonifen)、必芬諾(bifenox)、甲氧基護穀(chlomethoxyfen)、草枯醚(chlornitrofen)、艾尼丙密(etnipromid)、消草醚(fluorodifen)、乙羧氟草醚(fluoroglycofen)、氟除草醚(fluoronitrofen)、氟磺胺草醚(fomesafen)、呋氧草醚(furyloxyfen)、鹵索芬(halosafen)、乳氟禾草靈(lactofen)、除草醚(nitrofen)、三氟甲草醚(nitrofluorfen)及復祿芬(oxyfluorfen);二硫代胺基甲酸鹽類除草劑,諸如邁隆(dazomet及威百畝(metam);鹵化烷類除草劑,諸如五氯戊酮酸(alorac)、三氯丙酸(chloropon)、得拉本(dalapon)、氟丙酸(flupropanate)、六氯丙酮(hexachloroacetone)、碘甲烷(iodomethane)、溴甲烷(methyl bromide)、一氯乙酸、SMA及TCA;咪唑啉酮類除草劑,諸如咪草酸(imazamethabenz)、甲氧咪草酸(imazamox)、甲咪唑菸酸(imazapic)、依滅草(imazapyr)、滅草喹(imazaquin)及咪草菸(imazethapyr);無機類除草劑,諸如磺酸銨(ammonium sulfamate)、硼砂(borax)、氯酸鈣(calcium chlorate)、硫酸銅(copper sulfate)、硫酸亞鐵(ferrous sulfate)、疊氮鉀(potassium azide)、氰酸鉀(potassium cyanate)、疊氮化鈉(sodium azide)、氯酸鈉(sodium chlorate)及硫酸 (sulfuric acid);腈類除草劑,諸如糠草腈(bromobonil)、溴苯腈(bromoxynil)、羥敵草腈(chloroxynil)、環吡瑞諾(cyclopyranil)、二氯苯腈(dichlobenil)、碘保諾(iodobonil)、碘苯腈(ioxynil)及雙唑草腈(pyraclonil);有機磷類除草劑,諸如甲基胺草磷(amiprofos-methyl)、莎稗磷(anilofos)、地散磷(bensulide)、畢拉草(bilanafos)、抑草膦(butamifos)、2,4-DEP、DMPA、EBEP、調節膦(fosamine)、固殺草(glufosinate)、固殺草-P(glufosinate-P)、嘉磷塞(glyphosate)及哌草磷(piperophos);苯氧類除草劑,諸如殺草全(bromofenoxim)、稗草胺(clomeprop)2,4-DEB、2,4-DEP、戊味禾草靈(difenopenten)、賽松(disul)、抑草蓬(erbon)、艾尼丙密(etnipromid)、芬特拉科(fenteracol)及三氟禾草肟(trifopsime);噁二唑啉(oxadianoline)除草劑,諸如滅草唑(methazole)、丙炔噁草酮(oxadiargyl)、樂滅草(oxadiazon);噁唑類除草劑,諸如酚奧薩碸(fenoxasulfone);苯氧乙酸類除草劑,諸如4-CPA、2,4-D、3,4-DA、MCPA、脫禾草(MCPA-thioethyl)及2,4,5-T;苯氧丁酸類除草劑,諸如4-CPB、2,4-DB、3,4-DB、MCPB及2,4,5-TB;苯氧丙酸類除草劑,諸如調果酸(cloprop)、4-CPP、2,4-滴丙酸(dichlorprop)、高2,4-滴丙酸(dichlorprop-P)、3,4-DP、2,4,5-涕丙酸(fenoprop)、甲氯丙酸(mecoprop)及甲氯丙酸-P(mecoprop-P);芳氧苯氧丙酸類除草劑,諸如炔禾靈(chlorazifop)、炔草酯(clodinafop)、氯伏草(clofop)、氰氟草酯(cyhalofop)、禾草靈(diclofop)、、噁唑禾草靈(fenoxaprop)、噁唑禾草靈-P(fenoxaprop-P)、噻唑禾草靈(fenthiaprop)、伏寄普(fluazifop)、伏寄普-P(fluazifop-P)、吡氟氯禾靈(haloxyfop)、精吡氟氯禾靈(haloxyfop-P)、異噁草醚(isoxapyrifop)、噁唑醯草胺(metamifop)、普拔草(propaquizafop)、快伏草(quizalofop)、快伏草-P(quizalofop-P)及特立弗(trifop);苯二胺除草劑,諸如撻 乃安(dinitramine)及苯胺靈(prodiamine);吡唑類除草劑,諸如派羅克殺草碸(pyroxasulfone);苯醯吡唑類除草劑,諸如吡草酮(benzofenap)、磺醯草吡唑(pyrasulfotole)、比拉唑諾(pyrazolynate)、普芬草(pyrazoxyfen)、硝黃草酮(tolpyralate)及苯吡唑草酮(topramezone);苯吡唑類除草劑,諸如異丙吡草酯(fluazolate)、尼平拉芬(nipyraclofen)、唑啉草酯(pioxaden)及吡草醚(pyraflufen);噠嗪類除草劑,諸如噠草醚(credazine)、環吡瑞莫(cyclopyrimorate)、吡啶達醇(pyridafol)及必汰草(pyridate);噠嗪酮類除草劑,諸如殺莠敏(brompyrazon)、氯草敏(chloridazon)、敵米達松(dimidazon)、氟噠嗪草酯(flufenpyr)、美氟拉隆(metflurazon)、氟草敏(norflurazon)、草噠松(oxapyrazon)及皮丹能(pydanon);吡啶類除草劑,諸如氯胺基吡啶酸(aminopyralid)、一氯吡啶酯(cliodinate)、畢克草(clopyralid)、汰硫草(dithiopyr)、氯氟吡啶酯(florpyrauxifen)、氯氟吡氧乙酸(fluroxypyr)、氟氯吡啶酯(halauxifen)、氟啶草(haloxydine)、畢克爛(picloram)、氟吡草胺(picolinafen)、氯草定(pyriclor)、噻草啶(thiazopyr)及三氯比(triclopyr);二胺基嘧啶類除草劑,諸如氯胺草啶鹼(iprymidam)及賽克林(tioclorim);四級胺類除草劑,諸如牧草快(cyperquat)、迭森刈(diethamquat)、野燕枯(difenzoquat)、敵草快(diquat)、伐草快(morfamquat)及巴拉刈(paraquat);硫代胺基甲酸鹽類除草劑,諸如拔敵草(butylate)、環草特(cycloate)、燕麥敵(di-allate)、EPTC、戊草丹(esprocarb)、抑草威(ethiolate)、異丙靈(isopolinate)、甲硫苯卡(methiobencarb)、稻得壯(molinate)、坪草丹(orbencarb)、克草敵(pebulate)、苄草丹(prosulfocarb)、稗草畏(pyributicarb)、菜草畏(sulfallate)、殺丹(thiobencarb)、仲草丹(tiocarbazil)、野麥畏(tri-allate)及萬隆(vernolate);硫代碳酸鹽類除草劑,諸如草滅散(dimexano)、EXD及撲滅生 (proxan);硫脲類除草劑,諸如滅草恆(methiuron);三嗪類除草劑,諸如異丙淨(dipropetryn)、三嗪茚草胺(indaziflam)、三嗪氟草胺(triaziflam)及三羥基三嗪(trihydroxytriazine);氯三嗪類除草劑,諸如草脫淨(atrazine)、可樂津(chlorazine)、氰乃淨(cyanazine)、環丙津(cyprazine)、甘草津(eglinazine)、依哌嗪(ipazine)、甲普拉嗪(mesoprazine)、丙噻嗪(procyazine)、甘撲津(proglinazine)、普拔根(propazine)、塞佈拉嗪(sebuthylazine)、草滅淨(simazine)、特丁津(terbuthylazine)及草達津(trietazine);甲氧三嗪類除草劑,諸如莠去通(atraton)、醚草通(methometon)、撲滅通(prometon)、密草通(secbumeton)、西默通(simeton)及莠去通(atraton)、醚草通(methometon)、撲滅通(prometon)、密草通(secbumeton)、西默通(simeton);甲基硫代三嗪類除草劑,諸如草殺淨(ametryn)、疊氮津(aziprotryne)、氰草淨(cyanatryn)、敵草淨(desmetryn)、戊草津(dimethametryn)、美保嗪(methoprotryne)、佈滅淨(prometryn)、西草淨(simetryn)及去草淨(terbutryn);三嗪酮除草劑,諸如如特津酮(ametridione)、特草嗪酮(amibuzin)、菲殺淨(hexazinone)、丁嗪草酮(isomethiozin)、苯嗪草酮(metamitron)、滅畢淨(metribuzin)及三氟草嗪(trifludimoxazin);三唑類除草劑,諸如殺草強(amitrole)、苯酮唑(cafenstrole)、三唑磺(epronaz)及氟胺草唑(flupoxam);三唑酮除草劑,諸如胺唑草酮(amicarbazone)、苯卡巴松(bencarbazone)、氟酮唑草(carfentrazone)、氟酮磺隆(flucarbazone)、三唑苯胺(ipfencarbazone)、丙氧磺隆(propoxycarbazone)、甲磺草胺(sulfentrazone)及噻酮磺隆-甲基(thiencarbazone-methyl);三唑嘧啶類除草劑,諸如氯酯磺草胺(cloransulam)、雙氯磺草胺(diclosulam)、雙氟磺草胺(florasulam)、唑嘧磺草胺(flumetsulam)、磺草唑胺(metosulam)、平速爛(penoxsulam)及甲氧磺草胺 (pyroxsulam);尿嘧啶類除草劑,諸如雙苯嘧草酮(benzfendizone)、克草(bromacil)、氟丙嘧草酯(butafenacil)、氟丙鉑秀(flupropacil)、異草定(isocil)、環草定(lenacil)、索氟納西(saflufenacil)及特草定(terbacil);尿素類除草劑,諸如噻草隆(benzthiazuron)、苄草隆(cumyluron)、環莠隆(cycluron)、氯雙脲(dichloralurea)、氟吡草腙(diflufenzopyr)、異草完隆(isonoruron)、愛速隆(isouron)、甲基苯噻隆(methabenzthiazuron)、莫尼索隆(monisouron)及草完隆(noruron);苯基脲除草劑,諸如疏草隆(anisuron)、炔草隆(buturon)、滅落寧(chlorbromuron)、乙氧苯隆(chloreturon)、綠麥隆(chlorotoluron)、枯草隆(chloroxuron)、香草隆(daimuron)、枯莠隆(difenoxuron)、噁唑隆(dimefuron)、達有龍(diuron)、非草隆(fenuron)、可奪草(fluometuron)、氟速隆(fluothiuron)、異丙隆(isoproturon)、理有龍(linuron)、滅草恆(methiuron)、甲基汰草龍(methyldymron)、吡喃隆(metobenzuron)、撲奪草(metobromuron)、甲氧隆(metoxuron)、綠穀隆(monolinuron)、滅草隆(monuron)、草不隆(neburon)、對氟隆(parafluron)、醯草隆(phenobenzuron)、環草隆(siduron)、四氟隆(tetrafluron)及噻苯隆(thidiazuron);嘧啶硫醯脲類除草劑,諸如磺胺磺隆(amidosulfuron)、四唑磺隆(azimsulfuron)、苄嘧磺隆(bensulfuron)、氯嘧磺隆(chlorimuron)、環磺隆(cyclosulfamuron)、亞速隆(ethoxysulfuron)、伏速隆(flazasulfuron)、氟吡磺隆(flucetosulfuron)、氟啶嘧磺隆(flupyrsulfuron)、甲醯嘧磺隆(foramsulfuron)、氯吡嘧磺隆(halosulfuron)、依速隆(imazosulfuron)、甲基二磺隆(mesosulfuron)、嗪吡嘧磺隆(metazosulfuron)、菸嘧磺隆(nicosulfuron)、嘧苯胺磺隆(orthosulfamuron)、環氧嘧磺隆(oxasulfuron)、氟嘧磺隆(primisulfuron)、嗪咪唑嘧磺隆(propyrisulfuron)、吡嘧磺隆(pyrazosulfuron)、碸嘧磺隆(rimsulfuron)、 甲嘧磺隆(sulfometuron)、磺嘧磺隆(sulfosulfuron)及三氟啶磺隆(trifloxysulfuron);三嗪硫醯脲類除草劑,諸如綠磺隆(chlorsulfuron)、西速隆(cinosulfuron)、胺苯磺隆(ethametsulfuron)、碘磺隆(iodosulfuron)、碘芬磺隆(iofensulfuron)、甲磺隆(metsulfuron)、氟磺隆(prosulfuron)、噻吩磺隆(thifensulfuron)、醚苯磺隆(triasulfuron)、苯磺隆(tribenuron)、氟胺磺隆(triflusulfuron)及三氟甲磺隆(tritosulfuron);噻唑脲類除草劑,諸如丁噻隆(buthiuron)、磺噻隆(ethidimuron)、得匍隆(tebuthiuron)、噻氟隆(thiazafluron)及噻苯隆(thidiazuron);及未分類的除草劑,諸如丙烯醛(acrolein)、丙烯醇(allyl alcohol)、環丙嘧啶酸(aminocyclopyrachlor)、草芬定(azafenidin)、本達隆(bentazone)、苯並雙環酮(benzobicyclon)、雙環比隆(bicyclopyrone)、特咪唑草(buthidazole)、氰氨化鈣(calcium cyanamide)、克草胺酯(cambendichlor)、伐草克(chlorfenac)、燕麥酯(chlorfenprop)、氟嘧殺(chlorflurazole)、氯甲丹(chlorflurenol)、環庚草醚(cinmethylin)、可滅蹤(clomazone)、CPMF、甲酚(cresol)、氰胺(cyanamide)、環吡瑞莫(cyclopyrimorate)、鄰-二氯苯、哌草丹(dimepiperate)、草哆嗦(endothal)、唑啶草(fluoromidine)、氟啶草酮(fluridone)、氟咯草酮(flurochloridone)、呋草酮(flurtamone)、噠草氟(fluthiacet)、茚草酮(indanofan)、異硫氰酸甲酯(methyl isothiocyanate)、OCH、噁嗪草酮(oxaziclomefone)、五氯苯酚(pentachlorophenol)、環戊惡草酮(pentoxazone)、苯基汞乙酸鹽(phenylmercury acetate)、甲硫磺樂靈(prosulfalin)、嘧啶肟草醚(pyribenzoxim)、環酯草醚(pyriftalid)、滅藻醌(quinoclamine)、硫氰苯胺(rhodethanil)、蘇格力卡品(sulglycapin)、噻達茲明(thidiazimin)、滅草環(tridiphane)、三甲隆(trimeturon)、三丙丹(tripropindan)及草達克(tritac)。
本發明之化合物I亦可包含其它的活性化合物(active compounds),或可共同及/或依序與促進活性化合物施用。這些其它的活性化合物可為植物健康刺激物,諸如有機化合物、無機肥料、或微量元素供給劑,或是其他可影響植物生長的製備物,諸如接種劑。
在另一個實施例中,化合物I亦可包含其他生物學上的生物體,或可與其他生物學上的生物體共同及/或依序施用,諸如,但不限於由芽孢桿菌屬(Bacillus)菌株,例如解澱粉枯草芽孢桿菌變種(Bacillus subtilis var.amyloiquefaciens)FZB24(TAEGRP®)及芽孢枯草桿菌(Bacillus amyloiquefaciens)FZB42(RHIZOVITAL®)、VotiVoTM 堅強芽孢桿菌(Bacillus firmus)、Clariva TM (巴斯德氏芽菌(Pasteuria nishizawae))、蘇雲金芽孢桿菌(Bacillus thuringiensis)、木黴菌屬(Trichoderma)種,及/或展現出抗蟲、蟎、線蟲及/或植物病原體活性之各菌株突變體及代謝物所組成的群組。
本案揭露內容之一實施例係為一種用於防治或預防真菌侵襲的方法。此方法包括將一殺真菌有效量的化合物I施用於土壤、植物、根部、葉子、種子或真菌所在地、或欲預防感染的所在地(例如施用於穀物或葡萄植物)。化合物I適用於對多種植物在真菌等級上的治療,同時表現出低度的植物毒性。化合物I適宜用於保護劑以及/或治療劑。
已發現式I化合物具有顯著的殺真菌作用,特別是用於農業用途上。式I化合物對農業作物及園藝植物的用途上特別有效。額外的益處可包括但不限於改良植物健康狀況;改良植物產量(例如 增加生物質量及/或增加有價值成分之含量);改良植物活力(例如改良植物的生長及/或讓葉子更綠);改良植物品質(例如改良某些成分之含量或組成);及改良植物對非 生物及/或生物性逆境之耐受性。
尤其,該成分對防治多種感染果園、葡萄藤園及農園有用的作物之非所欲的真菌有效。該組成物可用於對抗多種子囊菌綱(Ascomycetes)及擔子菌綱(Basidiomycetes)真菌,包括例如以下代表性的真菌菌種:在核果與梨果上:葉斑病(leaf spot)(櫻桃球腔菌(Mycosphaerella cersella)、梨球腔菌(Mycosphaerella pyri)、紅染尾孢菌(Cercospora rubrotincta))、炭疽病(anthracnose)(圍小叢殼菌(Glomerella cingulata)、急尖炭疽刺盤孢菌(Glomerella acutata))、櫻桃葉斑病(leaf spot of cherry)(櫻桃葉斑病菌(Blumeriella jaapii))、白粉病(powdery mildew)(白叉絲單囊殼(Podosphaeria leucotricha)、桃絲單囊殼(Podosphaeria pannosa))、鏈隔孢菌屬腐病/黑斑病(Alternaria rot/black spot)(互生鏈隔孢菌(Alternaria alternata)、梨黑斑鏈格孢菌(A.gaisen)、流膠病(gummosis)(葡萄座腔菌屬(Botryosphaeria)種)、果腐病(fruit rot)(灰色葡萄孢菌(Botrytis cinerea))、瘡痂病(scab)(蘋果黑星菌(Venturia inequalis)、梨黑星病菌(V.pirinia)、櫻桃黑星菌(V.carpophila)、納雪黑星菌(V.nashicola)、黑星菌屬(Venturia)屬)、南方枯病(southern blight)(白絹病菌(Sclerotium rolfsii))、黑腐病(black rot)(葡萄座腔菌(Botryosphaeria obtusa))、鏈隔孢菌屬皰斑及腐病(Alternaria blotch and rot)(蘋果鏈隔孢菌(Alternaria mali)、鏈隔孢菌屬(Alternaria)屬)、雪松蘋果銹病(cedar apple rust)(龍柏銹病菌(Gymnosporangium juniper-virginianae))、美洲山楂銹病(American hawthorn rust)(球狀膠銹菌(Gymnosporagium globosum))、日本梨銹病(Japanese pear rust)(亞洲膠銹菌(Gymnosporangium asiaticum))、歐洲梨銹病(European pear rust)(褐色膠銹菌(Gymnosporangium sabinae))、肯恩氏梨銹病(Kern’spear rust)(肯恩尼亞那膠 銹菌(Gymnosporangium kernianum))、太平洋沿岸梨銹病(pacific coast pear rust)(理柏希德理膠銹菌(Gymnosporangium libocedri))、洛磯山脈梨銹病(Rocky Mountain pear rust)(尼爾蘇利膠銹菌(Gymnosporangium nelson))、苦腐病(bitter rot)(炭疽刺盤孢菌屬(Colletotrichum)種)、白腐病(white rot)(葡萄潰瘍病菌(Botryosphaeria dothidea))、黑腐病(black rot)(連續色二孢(Diplodia seriata))、煤汙病與蠅尿斑(sooty blotch and flyspeck)(病原體複合物包括座囊菌綱(Dothideomycetes)及糞殼菌綱(Sordariomycetes))、法布雷雅葉斑病(Fabraea leaf spot)(法布雷雅馬可拉塔(Fabraea maculate)、美斯皮里雙盤菌(Diplocarpon mespili))、褐班病(brown spot)(囊狀匐柄黴(Stemphylium vesicarium))、布魯克斯氏果斑病(Brooks fruit spot)(蘋果球腔菌(Mycosphaerella pomi))、莖點黴屬葉斑與果斑病(Phoma leaf and fruit spot)(莖點黴屬(Phoma)種)、皰斑病(blotch)(孤生葉點黴(Phyllosticta solitaria))、黑痘病與皰狀潰瘍(black pox and blister canker)(艾拉希比亞厄斯特里(Ellisembia asterinum))、蘋果環斑果病(apple ring spot)(葡萄座腔菌屬種)、萼端腐病(calyx-end rot)(油菜核盤黴(Sclerotinia sclerotiorum))、鏈核盤菌屬葉枯病與褐腐病(Monilinia leaf blight and brown rot)(鏈核盤菌屬(Moniliinia)種)、盤二孢黴屬皰斑病(Marssonina blotch)(蘋果雙盤菌(Diplocarpon mali))、藍黴病(blue mold)(青黴屬(Penicillium)種)、灰黴病(gray mold)(灰色葡萄孢菌(Botrytis cinerea)),以及潰瘍和木腐疾病(canker and wood rot diseases)(新叢赤殼菌屬(Neonectria)種、明孢盤菌屬(Neofabraea)種、間座殼菌屬(Diaporthe)種、黑腐皮殼菌屬(Valsa)種、葡萄座腔菌屬(Botryosphaeria)種、松口蜜環菌屬(Armillaria)種、軟靭革菌屬(Chondrostereum)種、裂褶菌屬(Schizophylum)種、靭革菌屬(Stereum)種、栓菌屬(Trametes)種); 在葡萄上:黑腐病(black rot)(葡萄球座菌(Guignardia bidwellii)、斐羅斯提克達阿美里其達(Phyllosticta ampelicida))、苦腐病(bitter rot)(葡萄生格林納爾黴(Greeneria uvicola))、彎孢殼菌屬頂枯病(Eutypa dieback)(葡萄藤猝倒病菌(Eutypa lata))、葡萄座腔菌屬頂枯病及大莖點菌黴屬腐病(Botryosphaeria dieback and Macrophoma rot)(葡萄座腔菌屬(Botryosphaeria)種)、葡萄孢菌屬串腐病及枯病(bunch rot and blight)(灰色葡萄孢菌(Botrytis cinerea))、擬莖點黴屬莖及葉斑病(Phomopsis cane and leaf spot)(葡萄生擬莖點黴(Phomopsis viticola)、葡萄生小隱孢殼(Cryptosporella viticola))、博萊納腐病(Rotbrenner)(葡萄角斑葉焦病菌(Pseudopezicula tracheiphila)、維管束假盤菌(Pseudopeziza tracheiphila))、炭疽病(anthracnose)(葡萄痂囊腔菌(Elsinoe ampelina))、銹病(rust)(葡萄層銹菌(Phakopsora ampelopsidis)、真葡萄亞屬層銹菌(Phakopsora euvitis))、殼針孢菌屬葉斑病(Septoria leaf spot)(葡萄壳针孢菌(Septoria ampelina))、葉枯病(leaf blight)(葡萄假尾孢菌(Pseudocercospora vitis))、葉皰斑病(leaf blotch)(葡萄褐斑葉枯病菌(Briosia ampelophaga))、白粉病(powdery mildew)(葡萄白粉病菌(Erysiphe necator))、白腐病(white rot)(矮狀小圓錐孢菌(Coniella diplodiella)、斐俐笛艾拉底皮勒帶拉(Pilidiella diplodiella))、晚腐病(ripe rot)(炭疽刺盤孢菌屬(Colletotrichum)種)、漿果腐病及黴病(berry rots and molds)(鏈隔孢菌屬(Alternaria)種、枝孢菌屬(Cladosporium)種、灰色葡菌孢菌(Botrytis cinerea)、炭疽刺盤孢菌屬(Colletotrichum)種、二孢黴屬(Diplodia)種、生格林納爾黴屬(Greeneria)種、擬莖點黴屬(Phomopsis)種、麴黴屬(Aspergillus)種、青黴屬(Penicillium)種、根黴屬(Rhizopus)種、鐮孢菌屬(Fusarium)種、匐柄黴屬(Stemphyilium)種、囊二孢菌(Ascochyta)種); 在草莓上:殼針孢菌屬硬腐病及葉斑病(Septoria hard rot and leaf spot)(殼針孢菌屬(Septoria)種)、白粉病(powdery mildew)(斑點單絲殼(Sphaerotheca macularis)、斑點絲單囊殼(Podosphaera macularis))、炭疽病(anthracnose)(炭疽刺盤孢菌屬(Colletotrichum)種)、常見葉斑病(common leaf spot)(草莓球控菌(Mycosphaerella fragariae))、尾孢菌屬葉斑病(Cercospora leaf spot)(尾孢菌屬(Cercospora)種)、葉銹病(leaf rust)(委陵菜多胞锈菌(Phragmidium potentillae)、芳美拉透美堤賴(Frommeëlla tormentillae))、核盤菌屬冠及果腐病(Sclerotinia crown and fruit rot)(油菜核盤黴(Sclerotinia sclerotiorum))、鏈隔孢菌屬果腐及黑葉斑病(Alternaria fruit rot and black leaf spot)(鏈隔孢菌屬(Alternaria)種)、花藥及雌蕊枯病/黑根腐病/硬褐腐病(anther and pistil blight/black root rot/hard brown rot)(絲核菌屬(Rhizoctonia)種)、炭腐病(charcoal rot)(甘薯絲核菌(Macrophomina phaseolina))、盾殼孢菌疾病(Coniothyrium diseases)(伏克盾殼黴(Coniothyrium fuckelii)、草莓小圓錐孢菌(Coniella fragariae))、黑柄孢菌屬冠及根腐病/白根腐病(Dematophora crown and root rot/white root rot)(棕墊炭豆菌(Rosellnia necatrix))、雙重孢菌屬腐病/葉及莖腐病(Diplodina rot/leaf and stalk rot)(番茄莖點黴(Phoma lycopersici))、果腐病(fruit rots)(亮黒麴黴(Aspergillus niger)、枝孢菌屬(Cladosporium)種、青黴屬(Penicillium)種)、絲衣黴屬腐病(Byssochlamys rot)(純黃絲衣黴(Byssochlamys fulva))、果皰斑病(Fruit blotch)(匍匐委陵菜霜霉(Peronospora potentillae)、仁果球殼孢(Sphaeropsis malorum)、白絹病菌(Sclerotium rolfsii)、草黃裂口菌(Schizoparme straminea))、灰黴葉枯病及乾冠腐病(Gray mold leaf blight and dry crown rot)(灰色葡萄孢菌(Botrytis cinerea))、葉焦枯病(leaf scorch)(安林那雙殼 菌(Diplocarpon earlianum))、盤多毛孢黴果腐病(Pestalotia fruit rot)(盤多毛孢黴(Pestalotia)種)、葉枯病(Leaf blight)(昏暗擬莖點黴(Phomopsis obscuans))、收成後腐病(Postharvest rots)(灰色葡萄孢菌(Botrytis cinerea)、畢赤酵母屬(Pichia)種、酵母屬(Saccharomyces)種)、南方枯病(southern blight)(白絹病菌(Sclerotium rolfsii));在香蕉上:炭疽病(anthracnose)(芭蕉科炭疽刺盤孢菌(Colletotrichum musae)、松口蜜環菌屬玉米腐病(Armillaria corn rot)(假蜜環菌(Armillaria mellea)、無環假蜜環菌(Armillaria tabescens))、黑十字病(Black cross)(芭蕉生黑痣菌(Phyllachora musicola))、黑根腐病(Black root rot)(錐孢炭豆菌(Rosellinia bunodes))、香蕉葉斑病(black Sigatoka)(斐濟球腔菌(Mycosphaerella fijiensis))、褐皰斑病(Brown blotch)(生屑擬盤多毛孢黴(Pestalotiopsis leprogena))、褐斑病(Brown spot)(香蕉褐斑尾孢菌(Cercospora hayi))、長喙黴屬果腐病(Ceratocystis fruit rot)(奇異長喙黴屬(Ceratocystis paradoxa))、雪茄尖病(Cigar-end)(可可輪刺孢菌(Verticillium theobromae)、塔吉球菌(Trachysphaera fructigena))、斑點枝孢菌(Cladosporium speckle)(芭蕉枝孢菌(Cladosporium musae))、球莖乾腐病(Corm dry rot)(亮松氏孔菌(Junghuhnia vincta))、細齒生雙孢菌屬葉斑病(Cordana leaf spot)(圓星病菌(Cordana johnstonii)、香蕉細齒生雙孢菌(Cordana musae))、冠腐病(Crown rot)(芭蕉科炭疽刺盤孢菌(Colletotrichum musae)、可可輪刺孢菌(Verticillium theobromae)、鐮孢菌屬(Fusarium)種、枝頂孢菌屬(Acremonium)種)、柱狀分歧孢菌屬根腐病(Cylindrocladium root rot)(柱狀分岐孢菌屬(Cylindrocladium)種)、小德佛同孢菌屬果斑病(Deightoniella fruit speckle)、猝倒病(damping off)、葉斑病及尖腐病 (leaf spot and tip rot)(無頸狀小德佛同孢菌(Deightoniella torulosa))、菱形斑病(Diamond spot)(香蕉褐斑尾孢菌(Cercospora hayi)、鐮孢菌屬(Fusarium)種)、矮稈香芽蕉尖腐病(Dwarf Cavendish tip rot)(芒果那特斯拉菌(Nattrassia mangiferae))、眼點病(eyespot)(巨大德雷克斯孢菌(Drechslera gigantean))、水果雀斑病(Fruit freckle)(香蕉球座腔菌(Guignardia musae))、果腐病(Fruit rot)(茶藨子葡萄座腔菌(Botryosphaeria ribis))、真菌性根腐病(Fungal root-rot)(鐮孢菌屬(Fusarium)種、絲核菌屬(Rhizoctonia)種)、真菌性雲紋病(Fungal scald)(芭蕉科炭疽刺盤孢菌(Colletotrichum musae))、葉銹病(Leaf rust)(芭蕉夏菌(Uredo musae)、芭蕉單胞銹菌(Uromyces musae))、葉斑點病(Leaf speckle)(單純子囊菌(Acrodontium simplex))、葉斑病(Leaf spot)(畫眉草彎孢菌(Curvularia eragrostidis)、、大蕉德雷克斯孢菌(Drechslera musae-sapientum)、芭蕉小球腔菌(Leptosphaeria musarun)、廣布擬盤多毛孢黴(Pestalotiopsis disseminata))、主莖腐病(Main stalk rot)(奇異長喙黴屬(Ceratocystis paradoxa))、馬來葉斑病(Malayan leaf spot)(芭蕉獨擔子黴(Haplobasidion musae))、微皮傘腐病(Marasmiellus rot)(馬拉斯麥黴菌(Marasmiellus inoderma))、香蕉巴拿馬病(Panama disease)(尖鐮孢菌古巴變型種(Fusarium oxysporum f.sp.cubense))、花梗腐病(Peduncle rot)(可可毛色二孢屬(Lasiodiplodia theobromae)、鐮孢菌屬(Fusarium)種、可可輪刺孢菌(Verticillium theobromae))、擬盤多毛孢黴屬葉斑病(Pestalotiopsis leaf spot)(棕櫚擬盤多毛孢黴(Pestalotiopsis palmarum))、殼褐針孢屬葉斑病(Phaeoseptoria leaf spot)(芭蕉殼褐針孢菌(Phaeoseptoria musae))、紋孔病(Pitting)(灰梨孢黴(Pyricularia grisea))、假莖心腐病(Pseudostem heart rot)(串珠鐮孢菌(Fusarium moniliforme)))、根及根莖腐病(Root & rhizome rot)(芭焦柱孢 菌(Cylindrocarpon musae))、核盤菌屬果腐病(Sclerotinia fruit rot)(油菜核盤黴(Sclerotinia sclerotiorum))、殼針孢菌屬葉斑病(Septoria leaf spot)(芭蕉殼針孢菌(Septoria eumusae))、鞘腐病(sheath rot)(叢赤殼菌(Nectria foliicola)、芭蕉生球腔菌(Mycosphaerella musicola))、煙黴病(sooty mold)(利馬新黴菌(Limacinula tenuis))、斑點病(Speckle)(芭蕉球腔菌(Mycosphaerella musae))、黑尖病(Black end disease)(球黑孢黴(Nigrospora sphaerica))、莖尖腐病(Stem-end rot)(芭蕉科炭疽刺盤孢菌(Colletotrichum musae))、熱帶斑點病(Tropical speckle)(芭蕉枝氯孢(Ramichloridium musae))、刺孢菌屬尖腐病(Verticillium tip rot)(可可輪刺孢菌(Verticillium theobromae)),及黃條葉斑病(Yellow Sigatoka)(芭蕉生球腔菌(Mycosphaerella musicola))。
化合物I已被發現在農業上果園、葡萄藤園及農園有用的作物之植物病原性真菌上具有顯著的殺真菌效果。這些疾病包括造成核果的花及果實褐腐病之核果鏈核盤菌(Monilinia laxa)及果生鏈核盤菌(Monilinia fructicola);造成核果的果腐病之匍枝根黴(Rhizopus stolonifera);造成蘋果白粉病的白叉絲單囊殼(Podosphaera leucotricha);造成蘋果葉斑病的蘋果鏈隔孢菌(Alternaria mali);造成梨瘡痂病的梨黑星病菌(Venturia pyrina);造成梨的煙黴病(sooty mold)之煤炱屬(Capnodium)種;造成葡萄白粉病的葡萄白粉病菌(Erysiphe necator);造成草莓及葡萄藤的灰黴病之灰色葡萄孢菌(Botrytis cinerea),以及造成香蕉之香蕉黑斑病(black sigatoka)的斐濟球腔菌(Mycosphaerella fijiensis),尤其是在農業的用途上。化合物I對於農業作物及園藝植物的用途上特別有效。
化合物I在作為殺真菌劑上具有範圍廣泛的效果。所施用的 活性材料確切量不僅取決於所施用之特定活性材料,也取決於所需的具體作用、欲防治之真菌物種及其生長階段,以及要與化合物接觸之植物部分或其他產物。因此,化合物I及含有化合物I的製劑在相似濃度時可能不會同樣的有效,或不能抵抗相同物種的真菌。
化合物I在以疾病抑制及植物學上可接受的量用於植物時為有效的。術語「疾病抑制及植物學上可接受的量」係指殺死或抑制所欲防治之植物疾病,但對植物無顯著毒性之化合物劑量。此數量通常為自約0.1至約1000ppm(百萬分之一),其中1至500ppm為較佳的。所需化合物之確切濃度隨著欲防治之真菌疾病、所採用之製劑類型、施用方法、具體植物物種、氣候條件等而變化。適宜的施用率通常在自約0.10至約4磅/英畝(約每平方公尺0.01至0.45公克,g/m2)範圍內。
只要熟習此項技術者對本文中之一教示的理解係明顯的,則可在不喪失所尋求之作用的情況下,擴展或改變本文中給定之任何範圍或所需值。
一含有化合物I之殺真菌性治療物,用於一5%的EC製劑中,且在藥桶中與一佐劑(Trycol,0.2% v/v之中的50% w/w)混合,在開花期於杏(apricots)(PRNAR,Protici變種)的樹冠噴灑兩次,施用率為每公頃50、100及150克的活性成份(g ai/ha)。以7天的間隔作此施用,在最後一次的施用中作疾病的接種(保護劑)。此處理為實驗性試驗之一部分,其為隨機完全區集設計,有四重複(replications)以及一約4.7 x 3.1公尺大小的土地,使用一MISTBLOW,Solo後背式施用器以500L/ha水量施用化合物I。
對每棵樹之10個預先標記的樹枝樣本上的花朵進行MONILIA病的評估。計算受感染的花朵數量,從而計算出發病率。在試驗期中第二次施用後的10、14及20天,評估3次目視感染(visual infection)。使用記錄下來的嚴重度資料集,為每塊土地計算病害發展曲線下面積(AUDPC)。相對AUDPC(基於AUDPC的防治率%),以未處理的控制組之百分比計算。結果給於表1中。
一含有化合物I之殺真菌性治療物,用於一5%的EC製劑中,且在藥桶中與一佐劑(Trycol,0.2% v/v之中的50% w/w)混合,在果實成熟期於油桃(PRNPN,Calfornia變種)的樹冠噴灑兩次,施用率為每公頃50、100及150克的活性成份(g ai/ha)。以8天的間隔作此施用,且在第一次的施用前12天作疾病的接種(治療劑)。此處理為實驗性試驗之一部分,其為隨機完全區集設 計,有四重複以及一約4.3 x 6.0公尺大小的土地,使用一MISTBLOW,Solo後背式施用器,以800L/ha水量施用化合物I。
已透過對從試驗中所採集的材料(乾塊)進行免疫分析及隨後的PCR測定的方式,證明病原體為果生鏈核盤菌(Monilinia fructicola)(MONIFC)。施用B之後8天(8DAAB)於收成時在每塊土地對100個隨機選取的水果評估褐腐疾病,計算果實的疾病發生率後,使用Abbotts法計算防治百分比。將每片土地60個目視健康的果實樣本放置在蜂巢板中,並在冷藏庫裡保存5天。接著將樣本維持在約20℃中14天(保質期(shelf life period))。進行數個評估以在模擬保質期的期間檢查疾病的發展。尤其是在從冷藏庫取出時(經過冷藏後的5天,13 DAAB),以及隨後的15、17、20和23 DAAB時檢查果實腐敗的百分比。計算患病的果實百分比(發病率),而後使用Abbotts法計算防治百分比。收成及保質期模擬結果給於表2中。
以田間小區(microplot)方法使用杏(apricots)來完成評估化合物I在核果腐病之效用的田野測試,實驗性試驗之一部分為隨機完全區集設計,有四重複。在一田間小區方法中,於每一份重複(共有10重複)內選用在一單枝上或果串上的兩個成熟果實,而不是使用整份重複。染色凋萎(colored flagging)辨識處理。一含有化合物I之殺真菌性治療物,用於一5%的EC製劑中,且在藥桶中與一佐劑(Trycol,0.2% v/v之中的50% w/w)混合,在果實成 熟時於杏(PRNAR)上噴灑,施用率為每公頃50、100及150克的活性成份(g ai/ha)。在收成前7天,使用一手持的手動噴灑瓶對所選的成熟杏(apricots)以500L/ha的水量作施用。在施用的一天後,將一ZipLoc塑膠袋置於果實或果串上,並將一MONIFC(根黴屬(Rhizopus)菌,來自於果園中的天然族群)的接種混合劑噴灑入內覆蓋果實。24小時後移除該塑膠袋。在收成時,收集田間的果實並置於一塑膠的Tupperware容器中。將150mL的去離子水倒進Tupperware容器的底部,並將果實噴灑上一層薄霧狀的水。將該容器帶回實驗室,用一大型垃圾袋封裝以保持高濕度,並在實驗台上以約23℃培養。在試驗期中於施用後的9及16天,評估目視疾病發生率。使用記錄下來的嚴重度資料集,為每塊土地計算病害發展曲線下面積(AUDPC)。相對AUDPC(基於AUDPC的防治率%),以未處理的控制組之百分比計算。結果給於表3中。
使用田間小區(microplot)方法在桃(peaches)上來完成評估化合物I在核果腐病之效用的田野測試,實驗性試驗之一部分為隨機完全區集設計,有四重複。在一田間小區方法中,於每一份重複(共有10重複)中選用在一單枝上或果串上的兩個成熟果實,而不是使用整份重複。染色凋萎(colored flagging)辨識處理。在第一次施用的前一天,將ZipLoc塑膠袋置於果實或果串上,並將一MONIFC的接種混合劑噴灑入內覆蓋果實。24小時後移除該塑膠袋。24小時後,將一含有化合物I之殺真菌性治療物,用於一5%的EC製 劑中,且在藥桶中與一佐劑(Trycol,0.2% v/v之中的50% w/w)混合,噴灑在桃(PRNPS)上兩次,施用率為每公頃50、100及150克的活性成份(g ai/ha)。在收成前14天與前7天,使用一CO2動力接種噴灑槍對所選的成熟桃(peaches)作施用,水量為500L/ha。在收成時,收集田間的果實並置於一塑膠的Tupperware容器中。將150mL的去離子水倒進Tupperware容器的底部,並將果實噴灑上一層薄霧狀的水。將該容器帶回實驗室,用一大型垃圾袋封裝以保持高度的濕度,並在實驗台上以約23℃培養。在試驗期中第一次施用後的17天,評估目視疾病發生率以及嚴重度的百分比。結果給於表4中。
化合物I於蘋果上的PODOLE之評估以兩個分別的田野試驗進行。在第一個試驗中,將一含有5%的化合物I之EC製劑之殺真菌性治療物,加上一佐劑(ETHOMEEN T18H,1.0% v/v之中的50%),在生長季於蘋果(MABSD,Imperatore Dallag變種)植物頂部上噴灑7次,第一次施用是在BBCH 61植物生長階段,在開放性的田野條件下自然感染白粉病。接下來的6次施用是以約10天的間隔施用。化合物I製劑的施用率為每公頃100、150及200克的活性成分(g ai/ha)。此處理為實驗性試驗之一部分,其為隨機完全區集設計,有四重複及一約4.2 x 7.5公尺大小的土地。使用一後背式土地噴灑器(TRACKSP,Andreoli Engineering)以800L/ha的水量施用化合物I製劑,噴壓為450kPa。
在第二個試驗中,將一含有5%化合物I之EC製劑的殺真菌性治療物,加上一佐劑(ETHOMEEN T18H,1.0% v/v之中的50%),在生長季於 蘋果(MABSD,Imperatore Dallag變種)植物頂部上噴灑7次,第一次施用是在BBCH 61植物生長階段,在開放性的田野條件下自然感染白粉病。接下來的6次施用是以約10天的間隔施用。化合物I製劑的施用率為每公頃100、150及200克的活性成分(g ai/ha)。此處理為實驗性試驗之一部分,其為隨機完全區集設計,有四重複及一約4.2 x 7.5公尺大小的土地。使用一自力推進的多地履帶式噴灑器(TRACKSP,Andreoli Engineering)以800L/ha的水量施用化合物I製劑,噴壓為450kPa。
隨機選擇100片葉子,以葉子發病率及葉子感染率百分比評估兩個試驗的疾病嚴重度。在第一個試驗中,於施用D之後的3天(3DAAD)、7DAAF及5DAAG評估白粉病的感染3次。在第2個試驗中,於6DAAB、2DAAD、7DAAF及5DAAG評估白粉病的感染4次。使用記錄下來的嚴重度資料集,為每塊土地計算病害發展曲線下面積(AUDPC)。相對AUDPC(基於AUDPC的防治率%),以未處理的控制組之百分比計算。結果給於表5中。
化合物I以保護劑及治療劑兩種方式使用在蘋果葉斑病(ALTEMA)上的評估,係以兩個分別的田野試驗進行。在保護劑試驗中,將一含有10%的化合物I之SC製劑之殺真菌性治療物,單獨或是與一佐劑(Agnique BP420,0.3% v/v之中的50% w/w;或者用ETHOMEEN T18H,0.2% v/v之中的50% w/w)在蘋果生長季於蘋果樹(Hongxing變種)的植物頂部上噴灑6次,每次以15天的間隔進行施用。化合物I的製劑,無論有無伴隨佐劑,是以每公頃100、125及150克活性成分(g ai/ha)的施用率以及4500L/ha的水量 為來作施用。實驗性土地以葉斑病原體接種3次,第一次接種是在第一次施用之後2天(施用A,2DAAA)進行,接下來在2DAAC及2DAAD施用。此處理為實驗性試驗之一部分,其為隨機完全區集設計,有三重複及一約3顆樹尺寸大小的土地。
在治療劑試驗中,將一含有10%的化合物I之SC製劑之殺真菌性治療物,單獨或是與一佐劑(Agnique BP420,0.3% v/v之中的50% w/w;或ETHOMEEN T18H,0.2% v/v之中的50% w/w),在蘋果生長季於蘋果樹(Hongxing變種)的植物頂部上噴灑6次,以15天的間隔進行每一次的施用。化合物I的製劑,無論有無伴隨佐劑,是以每公頃100、125及150克活性成分(g ai/ha)的施用率以及4500L/ha的水量為來作施用。實驗性土地以葉斑病原體接種3次,第一次接種是在第一次施用的5天前。第二次接種是在第三次施用的5天前,而第三次接種是在第四次施用的5天前。此處理為實驗性試驗之一部分,其為隨機完全區集設計,有三重複及一約3顆樹尺寸大小的土地。
疾病發生率以每棵植物患病的葉子之百分比作評估。評估6次蘋果葉斑的感染,最後一次的評估是在第一次施用的90天後。使用記錄下來的嚴重度資料集,為每塊土地計算病害發展曲線下面積(AUDPC)。相對AUDPC(基於AUDPC的防治率%),以未處理的控制組之百分比計算。結果給於表6中。
一10%的化合物I之SC製劑與三種不同的佐劑於藥桶中混合:Agnique BP420(0.3% v/v之中的50% w/w)、Ethomeen T18H(0.15% v/v之中的50% w/w)及Trycol(0.3% v/v之中的50% w/w)。將化合物I的製劑噴灑在梨樹(Highland變種)大約2.5公尺高的植物頂部上,施用率為每公頃100、150及200克活性成分(g ai/ha)。試驗是建立在開放性田野條件下,於生長季對自然感染的梨瘡痂病(pear scab)及煙黴病(sooty mold)以約12天的間隔進行6次葉面施用。此處理為實驗性試驗之一部分,其為隨機完全區集設計,有四重複及一約3 x 5公尺大小的土地。化合物I製劑以一SOLO噴霧噴灑器以1500L/ha的水量施用。
在VENTPI的評估中,防治百分比的計算是基於果實評估中的發病率及嚴重度,相對於自未治療的控制組每片土地隨機選取的50個果實之比較來計算。在CAPDSP的評估中,使用Abbotts法與未治療的控制組以葉子嚴重度百分比計算防治百分比。在11DAAE、7DAAF及15DAAF時計算兩種疾病的防治百分比。結果給於表7中。
一含有化合物I之殺真菌性治療物,用於一5%的EC製劑中,且在藥桶中與一佐劑(Trycol,0.2% v/v之中的50% w/w)混合,噴灑於葡萄植物(VITVI,Chardonnay變種)的植物頂部,施用率為每公頃50、100及150克的活性成份(g ai/ha)。試驗是建立在開放性田野條件下自然發生感染,於生長季以約10天的間隔進行6次葉面施用。此處理為實驗性試驗之一部分,其為隨機完全區集設計,有四重複及一約3.0 x 7.0公尺大小的土地。使用一自力 推進的多地履帶式噴灑器(TRACTAIR,Andreoli Engineering)以1000L/ha的水量施用化合物I製劑,噴壓為400kPa。
以患病的葉子與果實的百分比(發病率),以及葉子和果實上的患病區域百分比(嚴重度,使用100個隨機的葉子及果串紀錄疾病的評估。評估3次葡萄白粉病,最初的評估是在第四次施用的2天後。使用記錄下來的嚴重度資料集,為每塊土地計算病害發展曲線下面積(AUDPC)。相對AUDPC(基於AUDPC的防治率%),以未處理的控制組之百分比計算。結果給於表8中。
在草莓上:一含有化合物I之殺真菌性治療物,用於一5%的EC製劑中,且在藥桶中與一佐劑(Trycol,0.2% v/v之中的50% w/w)混合,噴灑在草莓(FRAAN,Candonga變種)植物上,施用率為每公頃50、150及200克的活性成份(g ai/ha)。試驗是建立於在生長季中以約10天的間隔進行4次撒播施用(broadcast appliction),於最後一次施用之後(植物生長階段B85)接種灰黴。此處理為實驗性試驗之一部分,其為隨機完全區集設計,有四重複及一約2.0 x 5.0公尺大小的土地。使用一後背式土地噴灑器(BKPCKENG,solo 433;HCSOLID-Albutz ATR80 Yellow噴嘴),以800L/ha的水量施用化合物I製劑,噴壓為300kPa。
以每片土地隨機的100個果實樣本中發生果實受損的百分比,記錄疾病嚴重度。在第三次施用的10天後(10DAAC)以及10DAAD評估灰黴病感染兩次。使用記錄下來的嚴重度資料集,為每塊土地計算病害發展曲線 下面積(AUDPC)。相對AUDPC(基於AUDPC的防治率%),以未處理的控制組之百分比計算。結果給於表9中。
草莓保質期的模擬(3反複(repetitions)):將殺真菌性治療物施用在長於一遮蔭房(shade house)的草莓植物,以獲得健康的果實。待成熟後,收成健康的果實並轉移到實驗室中進行模擬架上保質期研究。在實驗室中,以漂白劑除去果實上的汙染,以移除殘留的化學殘餘。將用於一5%的EC製劑中,且在藥桶中與一佐劑(Trycol,0.2% v/v之中的50% w/w)混合的之化合物I,噴灑在健康的草莓上,施用率為每公頃50、100及150克活性化合物(g ai/ha)並使其完全乾燥。隨後將果實接種灰黴病,並在實驗台上以20℃培養。
疾病嚴重度以果實感染評估的百分比記錄。在最初的接種之後評估兩次灰黴病的感染,感染後的4天(4DAI)及6DAI。使用記錄下來的嚴重度資料集,為每塊土地計算病害發展曲線下面積(AUDPC)。相對AUDPC(基於AUDPC的防治率%),以未處理的控制組之百分比計算。結果給於表9中。
在葡萄藤上:一含有化合物I之殺真菌性治療物,用於一5%的EC製劑中,且在藥桶中與一佐劑(Trycol,0.2% v/v之中的50% w/w)混合,僅噴灑在葡萄植物(VITVI,Pinot grey變種)中串的部份上,施用率為每公頃50、150及200克的活性成份(g ai/ha)。試驗是建立於兩個分隔28天的施用上,在一開放性田野條件下,於最後一次施用(植物生長階段B83)的3天後接種疾病。此處理為實驗性試驗之一部分,其為隨機完全區集設計,有四重複及一約2.5 x 7.0公尺大小的土地。使用一後背式土地噴灑器(AIRATOM,Solo 433;Airatom噴嘴),以500L/ha的水量施用化合物I的製劑。
以每片土地隨機的100個果串樣本中受損果串的發病率及感染率百分比,記錄疾病嚴重度。評估3次灰黴的感染,第一次評估是在最後一次施用的22天後(22DAAB),第二次及第三次評估是在28DAAB及36DAAB。使用記錄下來的嚴重度資料集,為每塊土地計算病害發展曲線下面積(AUDPC)。相對AUDPC(基於AUDPC的防治率%),以未處理的控制組之百分比計算。結果給於表9中。
將5%化合物I之EC製劑的等分樣品以水稀釋,並與Spraytex CT礦物油(6 L CP/Ha)混合,以達到活性成分率為25、50、100及150g ai/Ha。使用一Acrograph噴灑器,通過一模具將這些治療物投藥至單一葉子上的受影響葉片區域(施用體積為40L/Ha),施用區域為9 x 12公分。對葉子1(預防劑以及非常早期的治療劑)以及葉子3(治療劑效果)作一次單一施用的投藥。實驗的設計是基於一隨機完全區集以及4重複。MYCOFI的症狀是因為自然的接種以及傳染病的發展導致。
使用經處理的葉子上相對於未處理的葉子之疾病嚴重度比率,來計算疾病防治百分比。在試驗期間評估5次香蕉葉斑病(black Sigatoka)的感染:施用後的31天(31DAA)、38DAA、45DAA、52DAA及59DAA。使用記錄下來的嚴重度資料集,為每塊土地計算病害發展曲線下面積(AUDPC)。相對AUDPC(基於AUDPC的防治率%),以未處理的控制組之百分比計算。結果給於表10及表11中。
一含有化合物I的殺真菌性治療物,用於一SC製劑(內置MSO)中,且在藥桶中與一佐劑(Agnique BP-420,0.2% v/v之中的50% w/w,或者用Adsee C80W 80%)混合,噴灑在生長階段(中間花瓣脫落(mid petal fall)、花朵凋謝、花瓣脫落;BBCH 67-85)的櫻桃樹上(PRNAV,Sentennial變種),施用率為60、120、150及180g ai/ha。實驗的土地是用自然感染的方式運作。此處理為實驗性試驗之一部分,其為隨機完全區集(RCB)設計,有四重複及一約4 x 6公尺大小的土地。化合物I係使用一Airblast噴灑器,以1000L/ha的水量施用。
在施用5之後14天(14 DAA5)評估疾病嚴重度(整片土地上目視患病葉部(葉子)的百分比)及疾病發生率。將疾病的感染記錄下來。以患病葉子的百分比(發病率)、患病葉子區域百分比(嚴重度,為一計算出的疾病指數 (發病率百分比(%)x嚴重度百分比(%))作疾病的評估,然後使用Abbotts法從疾病指數數值計算出防治百分比(%)。結果給於表12中。
一含有化合物I之殺真菌性治療物,用於一SC製劑(內置MSO)中,且在藥桶中與一佐劑(Agnique BP-420,0.2% v/v之中的50% w/w,或者用Adsee C80W 80%)混合,自開花前到果仁變硬的時期噴灑在胡桃樹上(CYAIL,Desirable變種),施用率為60、120、150及180g ai/ha。實驗的土地是用自然感染的方式運作。此處理為實驗性試驗之一部分,其為隨機完全區集(RCB)設計,有四重複及一約40 x 40英尺大小的土地。在一個測試中,使用一Airblast噴灑器(Hollowcone實心墊片D10/45噴嘴),將化合物I以每英畝94-115加侖(加侖/英畝)的水量用於9個施用中,噴壓為46至54psi。在第二個測試中,使用一Handgun噴灑器(實心流束噴嘴),將化合物I以加侖/英畝的水量用於8個施用中,噴壓為300psi。兩個試驗皆訂定施用的間隔為14天。
以一個測試中的果仁發病率%及嚴重度%(各作3個評估,9個施用),以及以第二個測試中的果仁發病率%及葉片嚴重度%(分別作2和3個評估,8個施用),進行疾病的評估。使用記錄下來的嚴重度資料集,為每塊土地計算病害發展曲線下面積(AUDPC)。相對AUDPC(基於AUDPC的防治率%),以未處理的控制組之百分比計算。結果給於表13中。
一含有化合物I之殺真菌性治療物,用於一SC製劑(內置MSO)中,且在藥桶中與一佐劑(Agnique BP-420,0.2% v/v之中的50% w/w,或者用Adsee C80W 80%)混合,單次施用噴灑在扁桃樹(PRNDU,Winter變種)上,施用率為60、120、150及180g ai/ha。實驗的土地是以自然感染的方式運作。此處理為實驗性試驗之一部分,其為隨機完全區集(RCB)設計,有三重複及一約16 x 22英尺大小的土地。使用一Mistblower噴灑器(Orifice噴嘴,設定為2.3),將化合物I以100加侖/英畝的水量施用。
在施用A後的121天(121 DAAA)評估果仁發病率(整片土地中的每棵樹上每10個果仁的目視患病果仁數)。使用Abbotts法,利用治療組的果仁發病率%對上未處理組的果仁發病率來計算防治率%。結果給於表14中。
一含有化合物I之殺真菌性治療物,用於一SC製劑(內置MSO)中,且在藥桶中與一佐劑(Adsee C80W 80%)混合,在生長階段BBCH67及72作2個施用,噴灑在扁桃樹上(PRNDU,Butte變種),施用率為60、120、150及180g ai/ha。實驗的土地是以自然感染的方式運作。此處理為實驗性試驗之一部分,其為隨機完全區集(RCB)設計,有三重複及一約16 x 22英尺大小的土地。使用一機動化的後背式噴灑器(Orifice噴嘴,設定為2.3),將化合物I以100加侖/英畝的水量施用。
在施用A後的121天(121 DAAA)評估葉子發病率(整片土地中的每棵樹上每20片葉子的目視患病葉子數)結果給於表15中。
在施用A後的121天(121 DAAA)評估果仁發病率(整片土地中的每棵樹上每10個果仁的目視患病果仁數)。結果給於表16中。
一含有化合物I之殺真菌性治療物,用於一SC製劑(內置MSO)中,且在藥桶中與一佐劑(Agnique BP-420,0.2% v/v之中的50% w/w,或是用Adsee C80W 80%)混合,在兩個試驗中於生長階段BBCH71及72噴灑在扁桃樹上(PRNDU,Winters或Carmel變種),施用率為60、120、150及180g ai/ha。實驗的土地是以自然感染的方式運作。這些處理為實驗性試驗之一部分,其為隨機完全區集(RCB)設計,有三重複及一約14 x 20英尺大小的土地,兩個試驗皆然。使用一Mistblower噴灑器(Orifice噴嘴,設定為0.125),將化合物I以100加侖/英畝的水量施用,兩個試驗皆然。
在試驗中評估三或四次葉子發病率百分比(計算自整片土地中每棵樹上的每30(Winters)或50(Carmel)片葉子的目視患病葉子數)。使用記錄下來的嚴重度資料集,為每塊土地計算病害發展曲線下面積(AUDPC)。相對防治百分比係使用Abbotts法自AUDPC以未處理的控制組百分比計算得出。結果給於表17中。
一含有化合物I之殺真菌性治療物,用於一SC製劑(內置MSO)中,且在藥桶中與一佐劑(Adsee C80W 80%)混合,在生長階段BBCH67到69 以及BBCH69到72作2個施用,噴灑在扁桃樹上(PRNDU,Butte變種),施用率為60、120、150及180g ai/ha。實驗的土地是以自然感染的方式運作。這些處理為實驗性試驗之一部分,其為隨機完全區集(RCB)設計,有三重複及一約16 x 22英尺大小的土地。使用一機動化的後背式噴灑器,將化合物I以100加侖/英畝的水量施用。
在施用A後的105天(105 DAAA)評估且記錄葉子發病率百分比(計算自每一棵樹上每50片葉子的目視患病葉子數)。結果給於表18中。
一含有化合物I之殺真菌性治療物,用於一SC製劑(內置MSO)中,在開花期、花瓣脫落期及約在花瓣脫落期後的3週和5週,噴灑在扁桃樹(梅屬(Prunus)種)上,施用率為60、120、150及180g ai/ha。實驗的土地進行葡萄孢菌屬(Botrytis)菌的自然感染。這些處理為實驗性試驗之一部分,其為隨機完全區集(RCB)設計,有三重複及一約18 x 18英尺大小的土地。使用一Airblast噴灑器,將化合物I以100加侖/英畝的水量施用。
在施用4後17天(17 DAA4)評估並記錄果仁感染率(整片土地中的每棵樹上每個被計入的果仁總數之目視患病果仁數)。相對防治百分比係使用Abbotts法以未處理的控制組百分比計算得出。結果給於表19中。
Claims (3)
- 一種防治在果園、葡萄藤園及農園中具患病風險之選自於核果與梨果、葡萄、草莓及香蕉的作物之真菌疾病的方法,包含以下步驟:將化合物I或包括化合物I的一組成物接觸植物的至少一部分及/或一與植物相鄰的區域,
其中所述化合物在對抗一植物病原上係有效的且其中若所述作物係梨果或葡萄,所述真菌病原係選自於由以下致病原所組成的群組:蘋果白粉病(powdery mildew of apples)(白叉絲單囊殼(Podosphaera leucotricha))、蘋果葉斑病(leaf spot of apples)(蘋果鏈隔孢菌(Alternaria mali))、梨瘡痂病(scab of pear)(梨黑星病菌(Venturia pyrina))、梨煤病菌(sooty mold of pear)(煤炱屬(Capnodium)種)及葡萄藤灰黴病(gray mold of grapevine)(灰色葡萄孢菌(Botrytis cinerea))。 - 如請求項1所述之方法,其中該組成物進一步包括至少一選自於由一殺蟲劑、一除草劑及一殺真菌劑所組成之群組的一額外農業活性成份。
- 如請求項1所述之方法,其中所述真菌病原係選自於由以下致病原所組成的群組:花及核果類水果中的褐腐病(brown rot)(核果鏈核盤菌(Monilinia laxa)及果生鏈核盤菌(Monilinia fructicola))、核果中的水果腐病(fruit rot)(匍枝根黴(Rhizopus stolonifera))、草莓灰黴病(gray mold of strawberry)(灰色葡萄孢菌(Botrytis cinerea))、香蕉葉斑病(black sigatoka of bananas)(斐濟球腔菌(Mycosphaerella fijiensis))、櫻桃白粉病(powdery mildew of cherry)(隱蔽叉絲單囊殼(Podosphaera clandestina),PODOCL)、胡桃瘡痂病(pecan scab)(卡利金冷枝孢菌(Cladosporium caryigenum),CLADCA)、扁桃瘡痂病(almond scab)(嗜果枝孢菌(Cladosporium carpopilum),CLADSP)、扁桃中的穿孔病(shot hole in almond)(小點黴屬病菌(Stigmina carpophila),STIGCA)、銹病(rust)(異色疣雙胞銹菌(Tranzschelia discolor),TRANDI)、及扁桃中的套腐病(jacket rot)(葡萄孢菌屬(Botrytis)、根黴屬(Rhizopus)及鏈核盤菌屬(Monolinia))。
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| KR102640770B1 (ko) | 2024-02-27 |
| AR111662A1 (es) | 2019-08-07 |
| JP7618631B2 (ja) | 2025-01-21 |
| MX2025000896A (es) | 2025-03-07 |
| CN110933931B (zh) | 2021-10-26 |
| UY37715A (es) | 2018-11-30 |
| RU2769166C2 (ru) | 2022-03-28 |
| ZA201907339B (en) | 2021-04-28 |
| EP3618627A1 (en) | 2020-03-11 |
| EP3618627A4 (en) | 2020-12-02 |
| CO2019013355A2 (es) | 2020-01-17 |
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