TW201718566A - 具有殺蟲效用之分子以及與其相關之中間物、組成物及方法(五) - Google Patents
具有殺蟲效用之分子以及與其相關之中間物、組成物及方法(五) Download PDFInfo
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- TW201718566A TW201718566A TW105128401A TW105128401A TW201718566A TW 201718566 A TW201718566 A TW 201718566A TW 105128401 A TW105128401 A TW 105128401A TW 105128401 A TW105128401 A TW 105128401A TW 201718566 A TW201718566 A TW 201718566A
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- Prior art keywords
- alkyl
- haloalkyl
- group
- cycloalkyl
- alkenyl
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- 238000000034 method Methods 0.000 title claims abstract description 19
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- 230000008569 process Effects 0.000 title abstract description 5
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Abstract
此揭示係有關於下列領域:具有對抗節肢動物門、軟體動物門,及圓形動物門之害蟲之殺蟲效用的分子,生產此類分子之方法、使用於此類方法中之中間物、含有此等分子之殺蟲組成物,以及使用此等殺蟲分子對抗此種害蟲之方法。這些殺蟲組成物可使用作為舉例而言,殺蜱蟎劑、殺昆蟲劑、殺蟎劑、殺軟體動物劑,及殺線蟲劑。本文件揭示具有下式(“式1”)之分子。□
Description
發明領域 此揭示係有關於下列領域:具有對抗節肢動物門、軟體動物門,及圓形動物門之害蟲之殺蟲效用的分子,生產此類分子之方法、使用於此類方法中之中間物、含有此等分子之殺蟲組成物,以及使用此等殺蟲分子對抗此種害蟲之方法。這些殺蟲組成物可使用作為舉例而言,殺蜱蟎劑、殺昆蟲劑、殺蟎劑、殺軟體動物劑,及殺線蟲劑。
發明背景 “有許多最危險的人類疾病是由昆蟲媒介傳播的”(Rivero等人)。由歷史上來看,瘧疾、登革熱、黃熱病、鼠疫、絲蟲病、蝨傳斑疹傷寒、錐蟲病(trypanomiasis)、萊什曼病(leishmaniasis)和其他病媒感染疾病,較其他原因引起更多的人類疾病與死亡,自17至20世紀初期(Gubler)。病媒感染疾病佔全球寄生蟲病與傳染病約17%。僅僅瘧疾每年便造成超過800,000人死亡,這些死亡者有85%為五歲以下之孩童。每年約有五千萬至一億件案例之登革熱出血。每年發生另外的250,000至500,000件案例之登革熱出血(Matthews)。病媒防治在預防與控制感染性疾病方面扮演相當重要的角色。然而,殺蟲劑抗性包括多重殺蟲劑抗性,在人類疾病主要病媒之所有昆蟲物種上愈來愈嚴重(Rivero等人)。近來,超過550個節肢動物物種業已發展出對至少一種害蟲之抗性(Whalon等人)。再者,昆蟲抗性的個案顯然不斷地超越除草劑及殺真菌劑抗性個案的數目(Sparks等人)。
每年昆蟲、植物病原體與雜草破壞了所有潛在食物生產量之40%。儘管施用殺蟲劑及使用一系列廣泛的非化學控制,諸如輪作及生物控制,但此損失仍存在。若僅可保存此食物中的一些,便可用於供養世界上超過三十億營養不良的人口(Pimental)。
植物寄生線蟲為分佈最廣的害蟲之一,且常常為最隱伏及代價高的害蟲之一。據估計,由於線蟲造成之損失,在已開發國家為約9%,在未開發國家為約15%。然而,在美國,根據35個州對於各種作物之調查顯示,線蟲衍生之損失高達25%(Nicol等人)。
值得注意的是,腹足類(蛞蝓和蝸牛為經濟重要性低於其他的節肢動物或線蟲少的害蟲,但在某些地方,腹足類可能會實質上大量降低產率,嚴重影響收穫產品的品質,以及會傳播人類、動物及植物疾病。雖然只有幾十種腹足類是嚴重地區性害蟲,但有少數品種是世界範圍內的重要害蟲。特別是,腹足類影響廣泛多種農業和園藝作物,如耕地、牧場、和纖維作物;蔬菜;灌木和喬木果實;草本植物;以及觀賞植物(Speiser)。
白蟻會造成各種私人和公共建築,以及農業和林業資源損害。據估計,在2005年,白蟻造成每年全世界損失超過500億美元(Korb)。
因此,就許多理由,包括上述之該等理由,持續需要昂貴的(估計於2010年每害蟲為大約2億5千6百萬美元)、耗時的(每害蟲平均為大約10年),以及困難開發的新穎殺蟲劑(CropLife America)。此揭示引用的某些參考文獻
CropLife America, The Cost of New Agrochemical Product Discovery, Development & Registration, and Research & Development predictions for the Future, 2010. Drewes, M., Tietjen, K., Sparks, T.C., High–Throughput Screening in Agrochemical Research,Modern Methods in Crop Protection Research
, Part I,Methods for the Design and Optimization of New Active Ingredients
, Edited by Jeschke, P., Kramer, W., Schirmer, U., and Matthias W., p. 1–20, 2012. Gubler, D., Resurgent Vector–Borne Diseases as a Global Health Problem, Emerging Infectious Diseases, Vol. 4, No. 3, p. 442–450, 1998. Korb, J., Termites, Current Biology, Vol. 17, No. 23, 2007. Matthews, G., Integrated Vector Management: Controlling Vectors of Malaria and Other Insect Vector Borne Diseases, Ch. 1, p. 1, 2011. Nicol, J., Turner S., Coyne, L., den Nijs, L., Hocksland, L., Tahna–Maafi, Z., Current Nematode Threats to World Agriculture,Genomic and Molecular Genetics of Plant – Nematode Interactions
, p. 21–43, 2011. Pimental, D., Pest Control in World Agriculture,Agricultural Sciences
– Vol. II, 2009. Rivero, A., Vezilier, J., Weill, M., Read, A., Gandon, S., Insect Control of Vector–Borne Diseases: When is Insect Resistance a Problem?Public Library of Science Pathogens,
Vol. 6, No. 8, p. 1–9, 2010. Sparks T.C., Nauen R., IRAC: Mode of action classification and insecticide resistance management,Pesticide Biochemistry and Physiology
(2014) available online 4 December 2014. Speiser, B., Molluscicides,Encyclopedia of Pest Management
, Ch. 219, p. 506–508, 2002. Whalon, M., Mota–Sanchez, D., Hollingworth, R., Analysis of Global Pesticide Resistance in Arthropods,Global Pesticide Resistance in Arthropods
, Ch. 1, p. 5–33, 2008.
發明概要 依據本發明之一實施例,係特地提出一種具下式之分子 式1
其中:(A) Ar1
係選自於下列所構成的群組:呋喃基、苯基、嗒基、吡啶基、嘧啶基,或是噻吩基, 其中每個呋喃基、苯基、嗒基、吡啶基、嘧啶基,及噻吩基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基;(B) Het
為5或6員、飽和或不飽和之雜環,含有獨立地選自於氮、硫或氧之一或多個雜原子,以及其中Ar1
與L1
互相不為鄰位,但可為間位或對位,例如就五員環而言,其等為1,3,且就六員環而言,其等為1,3或1,4, 其中每個雜環可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、側氧、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基;(C) L1
係選自於下列所構成的群組:N(Rx
)-(C1
-C4
)烷基、N(Rx
)-(C3
-C8
)環烷基、N(Rx
)-(C2
-C6
)烯基、N(Rx
)-(C2
-C6
)炔基、N(Rx
)-S(O)n
-(C1
-C4
)烷基、(C1
-C4
)烷基-N(Rx
)-(C1
-C4
)烷基、(C1
-C4
)烷基-N(Rx
)-(C1
-C4
)烷基、(C1
-C4
)烷基-N(Rx
)、(C3
-C8
)環烷基-N(Rx
)、(C2
-C6
)炔基-N(Rx
)、(C1
-C4
)烷基-S(O)n
-N(Rx
)、C(O)-N(Rx
)、C(S)-N(Rx
)、N(Rx
)-C(O)、N(Rx
)-C(S)、C(O)-N(Rx
)-(C1
-C4
)烷基、C(S)-N(Rx
)-(C1
-C4
)烷基、(C1
-C4
)烷基-N(Rx
)-C(O),以及(C1
-C4
)烷基-N(Rx
)-C(S), 其中每個烷基、環烷基、烯基及炔基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基,以及(C2
-C6
)炔基;(D) Ar2
係選自於下列所構成的群組:呋喃基、苯基、嗒基、吡啶基、嘧啶基,或是噻吩基, 其中每個呋喃基、苯基、嗒基、吡啶基、嘧啶基,及噻吩基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(=O)O-(C1
-C4
)烷基、苯基,以及苯氧基;(E) R15
係選自於下列所構成的群組:H、(C1
-C4
)烷基、(C3
-C8
)環烷基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、C(O)-NRx
Ry
、C(O)-苯基、(C1
-C4
)烷基-NRx
Ry
、C(O)O-(C1
-C4
)烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基,(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基, 其中每個烷基、環烷基、烯基、炔基,及苯基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、側氧、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基;(F) Q1
係選自於O及S所構成的群組;(G)Q2
係選自於O及S所構成的群組;(H) R16
係選自於下列所構成的群組:(K)
、H、(C1
-C4
)烷基、(C3
-C8
)環烷基、(C2
-C6
)烯基、(C2
-C6
)炔基、C(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、(C1
-C4
)烷基苯基、(C1
-C4
)烷基-O-苯基、C(O)-(Het-1)、(Het-1)、(C1
-C4
)烷基-(Het-1)、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-NRx
Ry
、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-(Het-1)、(C1
-C4
)烷基-C(O)-(Het-1)、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基(NRx
Ry
)-C(O)OH、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-NRx
Ry
、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-N(Rx
)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基(N(Rx
)-C(O)O-(C1
-C4
)烷基)-C(O)OH、(C1
-C4
)烷基-C(O)-(Het-1)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C3
-C8
)環烷基、(C1
-C4
)烷基-OC(O)-(Het-1)、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基-N(Rx
)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-NRx
Ry
、(C1
-C4
)烷基-S(O)n
-(Het-1),以及(C1
-C4
)烷基-O-(Het-1), 其中每個烷基、環烷基、烯基、炔基、苯基,及(Het-1)可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)OH、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基)、苯基、苯氧基、Si((C1
-C4
)烷基)3
、S(O)n
-NRx
Ry
,以及(Het-1);(I) R17
係選自於下列所構成的群組:(K)
、H、(C1
-C4
)烷基、(C3
-C8
)環烷基、(C2
-C6
)烯基、(C2
-C6
)炔基、C(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、(C1
-C4
)烷基苯基、(C1
-C4
)烷基-O-苯基、C(O)-(Het-1)、(Het-1)、(C1
-C4
)烷基-(Het-1)、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-NRx
Ry
、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-(Het-1)、(C1
-C4
)烷基-C(O)-(Het-1)、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基(NRx
Ry
)-C(O)OH、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-NRx
Ry
、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-N(Rx
)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基(N(Rx
)-C(O)O-(C1
-C4
)烷基)-C(O)OH、(C1
-C4
)烷基-C(O)-(Het-1)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C3
-C8
)環烷基、(C1
-C4
)烷基-OC(O)-(Het-1)、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基-N(Rx
)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-NRx
Ry
、(C1
-C4
)烷基-S(O)n
-(Het-1),以及(C1
-C4
)烷基-O-(Het-1), 其中每個烷基、環烷基、烯基、炔基、苯基,及(Het-1)可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)OH、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基、苯氧基、Si((C1
-C4
)烷基)3
、S(O)n
-NRx
Ry
,以及(Het-1);(J) L2
係選自於下列所構成的群組:(C3
-C8
)環烷基、苯基、(C1
-C4
)烷基苯基、(C1
-C4
)烷基-O-苯基、(C2
-C6
)烯基-O-苯基、(Het-1)、(C1
-C4
)烷基-(Het-1),以及(C1
-C4
)烷基-O-(Het-1), 其中每個烷基、環烷基、烯基、苯基,及(Het-1)可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C1
-C4
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、O-(C1
-C4
)烷基、S-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基、苯氧基,以及(Het-1), 其中每個烷基、環烷基、烯基、苯基,及(Het-1)取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C1
-C4
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、O-(C1
-C4
)烷基、S-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基、苯氧基,以及(Het-1);(K) R16
及R17
與Cx
(Q2
)(Nx
)
一起形成一個4-至7-員飽和或不飽和之雜環,其可以進一步含有選自於氮、硫或氧所構成的群組之一個或更多個雜原子, 其中每個雜環可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:側氧、R18
及R19
, 其中R18
及R19
係各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2
、側氧、硫酮基、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及(Het-1);(L) Rx
及Ry
係各自獨立地選自於下列所構成的群組:H、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基,以及苯基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基,及苯基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及(Het-1);(M) (Het-1)
為5或6員、飽和或不飽和之雜環,含有獨立地選自於氮、硫或氧所構成的群組之一或多個雜原子, 其中每個雜環可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、側氧、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基;(N) n
每一者係獨立地為0、1或2;以及式1的分子之N-氧化物、農業上可接受的酸加成鹽類、鹽類衍生物、溶劑合物、酯類衍生物、結晶性多形體、同位素、解析的立體異構物,以及互變異構物。
本揭示之定義
在此等定義中所提供之範例一般而言並非非窮舉性的,且不得解釋為限制本揭示。應理解,取代基應依從與其所連接的特定分子相關之化學鍵結規則及立體相容性的限制。此等定義僅用於本揭示的目的。
用語「活性成分
」係意指一種材料,其具有控制害蟲有用的活性,及/或其有用於協助其他材料有更好的控制害蟲之活性,此等材料的實例包括但不限於:殺蜱蟎劑、除藻劑、拒食劑、殺鳥劑(avicide)、殺菌劑、驅鳥劑、化學絕育劑、殺真菌劑、除草劑安全劑、除草劑、誘蟲劑、驅蟲劑、殺昆蟲劑、驅哺乳動物劑、交配干擾劑、殺蟎劑、殺線蟲劑、植物活化劑、植物生長調節劑、滅鼠劑、協力劑,以及殺病毒劑(見alanwood.net)。此等材料的特定實例包括但不限於活性成分群組α之中列出的材料。
用語「活性成分 群 組α
」(此後稱為“AIGA
”)」係集體意指下列材料:(1)
(3-乙氧基丙基)溴化汞、1,2-二溴乙烷、1,2-二氯乙烷、1,2-二氯丙烷、1,3-二氯丙烯、1-MCP、1-甲基環丙烯、1-萘酚、2-(辛基硫基)乙醇、2,3,3-TPA、2,3,5-三碘苯甲酸、2,3,6-TBA、2,4,5-T、2,4,5-TB、2,4,5-TP、2,4-D、2,4-DB、2,4-DEB、2,4-DEP、2,4-DES、2,4-DP、2,4-MCPA、2,4-MCPB、2iP、2-甲氧基乙基氯化汞、2-苯基酚、3,4-DA、3,4-DB、3,4-DP、3,6-二氯2-吡啶甲酸、4-胺基吡啶、4-CPA、4-CPB、4-CPP、4-羥基苯乙基醇、8-羥基喹啉硫酸鹽、8-苯基汞氧基喹啉、阿巴美丁(abamectin)、阿巴美丁胺甲基(abamectin-aminomethyl)、脫落酸(abscisic acid)、ACC、毆殺松(acephate)、亞醌蟎(acequinocyl)、亞滅培(acetamiprid)、家蠅磷(acethion)、乙草胺(acetochlor)、三氯殺蟲酯(acetofenate)、乙酯磷(acetophos)、乙醯蟲腈(acetoprole)、阿拉酸式苯(acibenzolar)、亞喜芬(acifluorfen)、苯草醚(aclonifen)、CAN、內醯吖庚胺(acrep)、阿納寧(acrinathrin)、丙烯醛(acrolein)、丙烯腈、阿西佩它克斯(acypetacs)、阿斐多匹朋(afidopyropen)、阿福藍(afoxolaner)、拉草(alachlor)、鈉得爛(alanap)、棉鈴威(alanycarb)、阿苯達唑(albendazole)、得滅克(aldicarb)、得滅克碸、十二嗎啉(aldimorph)、涕滅碸威(aldoxycarb)、阿特靈(aldrin)、亞列寧(allethrin)、蒜素(allicin)、草毒死(allidochlor)、阿洛胺菌素(allosamidin)、亞汰草(alloxydim)、烯丙醇、除害威(allyxycarb)、亞羅列克(alorac)、α-賽滅寧(alpha
-cypermethrin)、α-安殺番(alpha
-endosulfan)、亞滅寧(alphamethrin)、六甲嘧胺(altretamine)、磷化鋁(aluminium phosphide)、磷化鋁(aluminum phosphide)、辛唑嘧菌胺(ametoctradin)、特津酮(ametridione)、草殺淨(ametryn)、草殺淨(ametryne)、特草嗪酮(amibuzin)、胺唑草酮(amicarbazone)、拌種靈(amicarthiazol)、賽硫磷(amidithion)、磺胺蟎酯(amidoflumet)、醯嘧磺隆(amidosulfuron)、滅害威(aminocarb)、環丙嘧啶酸(aminocyclopyrachlor)、氯胺吡啶酸(aminopyralid)、胺三唑、甲基胺草磷(amiprofos-methyl)、胺草磷(amiprofos)、甲基胺草磷(amiprofos-methyl)、安美速(amisulbrom)、阿米通(amiton)、三亞蟎(amitraz)、殺草強(amitrole)、胺磺酸銨鹽、代森銨(amobam)、非晶形矽膠、非晶形二氧化矽、1-胺基丙基磷酸(ampropylfos)、AMS、毒藜鹼(anabasine)、嘧啶醇(ancymidol)、敵菌靈(anilazine)、莎稗磷(anilofos)、疏草隆(anisuron)、蒽醌(anthraquinone)、安妥(antu)、唑磷嗪(apholate)、殺蟎特(aramite)、殘殺威(arprocarb)、三氧化二砷、福美砷(asomate)、阿司匹靈(aspirin)、磺草靈(asulam)、乙基殺撲磷(athidathion)、阿特拉通(atraton)、草脫淨(atrazine)、金色制黴素(aureofungin)、、阿維菌素B1(avermectin B1)、AVG、四烯雌酮(aviglycine)、氧環唑(azaconazole)、印苦楝子素(azadirachtin)、草芬定(azafenidin)、亞滅松(azamethiphos)、滅蚜松(azidithion)、四唑嘧磺隆(azimsulfuron)、乙基谷速松(azinphosethyl)、乙基谷速松(azinphos-ethyl)、谷速松(azinphosmethyl)、谷速松(azinphos-methyl)、疊氮津(aziprotryn)、滅蘇民(aziprotryne)、塞侖(azithiram)、偶氮苯(azobenzene)、亞環錫(azocyclotin)、偶氮磷(azothoate)、亞托敏(azoxystrobin)、菊乙胺酯(bachmedesh)、燕麥靈(barban)、燕麥靈(barbanate)、六氟矽酸鋇、多硫化鋇、矽氟化鋇(barium silicofluoride)、椒菊酯(barthrin)、鹼式碳酸銅(basic copper carbonate)、鹼式氯化銅(II)(basic copper chloride)、鹼式硫酸銅(basic copper sulfate)、BCPC、氟丁醯草胺(beflubutamid)、本達樂(benalaxyl)、本達樂-M、草除靈(benazolin)、醯苯草酮(bencarbazone)、異噻蟲唑(benclothiaz)、苯達魁丙治(bendaqingbingzhi)、免敵克(bendiocarb)、苯達松(bendioxide)、倍尼芬(benefin)、氟草胺(benfluralin)、免扶克(benfuracarb)、呋草黃(benfuresate)、苯嘧磺草胺(benmihuangcaoan)、麥鏽靈(benodanil)、免賴得(benomyl)、解草酮(benoxacor)、苯磷(benoxafos)、醌肟腙(benquinox)、免速隆(bensulfuron)、地散磷(bensulide)、免速達(bensultap)、苯他隆(bentaluron)、本達隆(bentazon)、本達隆(bentazone)、苯噻菌胺(benthiavalicarb)、苯噻硫氰(benthiazole)、(benthiocarb)、草噁嗪(bentranil)、苯甲醯胺氧乙酸(benzadox)、氯化烷基二甲基苄基銨、苯瑪松(benzamacril)、異噁草胺(benzamizole)、抑菌啉(benzamorf)、六氯化苯、雙苯嘧草酮(benzfendizone)、苄亞胺(benzimine)、苄草胺(benzipram)、苯并雙環酮(benzobicyclon)、硫丹(benzoepin)、吡草酮(benzofenap)、氟草黃(benzofluor)、苯基異羥肟酸(benzohydroxamic acid)、苯蟎特(benzomate)、苯并磷酸酯(benzophosphate)、苯并噻二唑(benzothiadiazole)、苯并烯氟菌唑(benzovindiflupyr)、西脫蟎(benzoximate)、新燕靈(benzoylprop)、苯噻隆(benzthiazuron)、苯唑草酮(benzuocaotong)、苯甲酸苄酯、苯甲基腺嘌呤(benzyladenine)、黃連素(berberine)、β-賽扶寧(beta
-cyfluthrin)、β-賽滅寧(beta
-cypermethrin)、比托沙(bethoxazin)、BHC、雙丙氨磷(bialaphos)、雙環哌喃酮(bicyclopyrone)、必芬蟎(bifenazate)、治草醚(bifenox)、畢芬寧(bifenthrin)、吡氟菌酯(bifujunzhi)、畢拉草(bilanafos)、百蟎克(binapacryl)、病氰硝(bingqingxiao)、百亞列寧(bioallethrin)、苄呋烯菊酯(bioethanomethrin)、生物氯菊酯(biopermethrin)、生物苄呋菊酯(bioresmethrin)、聯苯、吡殺茲(bisazir)、噻枯唑(bismerthiazol)、噻枯唑-銅(bismerthiazol-copper)、雙苯基汞亞甲基二(x-萘-y-磺酸) (bisphenylmercury methylenedi(x-naphthalene-y-sulphonate))、雙草醚(bispyribac)、雙三氟蟲脲(bistrifluron)、殺蟲雙(bisultap)、比多農(bitertanol)、硫雙二氯酚(bithionol)、聯苯吡菌胺(bixafen)、保米黴素(blasticidin-S)、硼砂、波爾多(Bordeaux)混合液、硼酸、白克列(boscalid)、BPPS、芸苔素內酯(brassinolide)、芸苔素內酯-乙基、小蠹集合信息素(brevicomin)、溴鼠隆(brodifacoum)、苄蟎醚(brofenprox)、溴滅菊酯(brofenvalerate)、溴氟苯胺(broflanilide)、溴氟菊酯(brofluthrinate)、克草(bromacil)、溴敵隆(bromadiolone)、二溴磷(bromchlophos)、溴鼠胺(bromethalin)、溴苄呋菊酯(bromethrin)、溴苯烯磷(bromfenvinfos)、溴乙醯胺(bromoacetamide)、除草溴(bromobonil)、溴丁醯草胺(bromobutide)、保滿丹(bromociclen)、保滿丹(bromocyclen)、溴-滴滴涕(DDT)、溴酚肟(bromofenoxim)、溴磷松(bromophos)、(bromomethane)、溴磷松(bromophos)、乙基-溴磷松、新殺蟎(bromopropylate)、溴菌腈(bromothalonil)、溴苯腈(bromoxynil)、殺莠敏(brompyrazon)、溴克座(bromuconazole)、溴硝醇(bronopol)、BRP、BTH、增效特(bucarpolate)、必克蝨(bufencarb)、佈敏納弗(buminafos)、布瑞莫(bupirimate)、布芬淨(buprofezin)、勃根第(Burgundy)混合液、白消安(busulfan)、白消安(busulphan)、畜蟲威(butacarb)、丁基拉草(butachlor)、布芬草(butafenacil)、牧草胺(butam)、抑草磷(butamifos)、丁烷-芬普尼(butane-fipronil)、佈伏斯(butathiofos)、丁烯草胺(butenachlor)、丁烷-芬普尼(butane-fipronil)、苄烯菊酯(butethrin)、丁硫咪唑酮(buthidazole)、丁硫啶(buthiobate)、丁噻隆(buthiuron)、脱葉磷(butifos)、佈嘉信(butocarboxim)、布托酯(butonate)、避蚊酮(butopyronoxyl)、丁酮碸威(butoxycarboxim)、比達寧(butralin)、丁苯草酮(butroxydim)、炔草隆(buturon)、丁基胺、丁酸鹽(butylate)、丁酯膦(butylchlorophos)、伸丁基-芬普尼(butylene-fipronil)、二甲胂酸(cacodylic acid)、硫線磷(cadusafos)、唑草胺(cafenstrole)、成骨醇(calciferol)、砷酸鈣、氯酸鈣、氰胺化鈣(calcium cyanamide)、氰化鈣、多硫化鈣、鈣殺畏(calvinphos)、卡本二氯(cambendichlor)、毒殺芬(camphechlor)、樟腦(camphor)、四氯丹(captafol)、蓋普丹(captan)、(carbam)、嗎菌威(carbamorph)、氯滅殺威(carbanolate)、胺甲萘(carbaril)、胺甲(carbaryl)、除草隆(carbasulam)、卡巴松(carbathion)、貝芬替(carbendazim)、多菌靈(carbendazol)、雙醯草胺(carbetamide)、卡波硫磷(carbofenotion)、加保扶(carbofuran)、二硫化碳、四氯化碳、硫化羰(carbonyl sulfide)、加芬松(carbophenothion)、馬拉硫磷(carbophos)、丁基加保扶(carbosulfan)、羧酸唑(carboxazole)、環二混劑(carboxide)、萎鏽靈(carboxin)、克繁草(carfentrazone)、加普胺(carpropamid)、培丹(cartap)、香芹酚(carvacrol)、香芹酮(carvone)、CAVP、CDAA、CDEA、CDEC、滅胞素(cellocidin)、CEPC、西拉洛(ceralure)、敵菌腙(cerenox)、沙巴達(cevadilla)、切欣特混合液(Cheshunt mixture)、愛卡士(chinalphos)、愛卡士-甲基(chinalphos-méthyl)、蟎離丹(chinomethionat)、滅蟎猛(chinomethionate)、愛卡士(chiralaxyl)、殼聚糖(chitosan)、克氯綜(chlobenthiazone)、甲氧基護谷(chlomethoxyfen)、氯醛糖(chloralose)、克爛本(chloramben)、氯胺磷(chloramine phosphorus)、氯黴素(chloramphenicol)、雙胺靈(chloraniformethan)、克氯尼(chloranil)、丁醯草胺(chloranocryl)、剋安勃(chlorantraniliprole)、炔禾靈(chlorazifop)、可樂津(chlorazine)、氯殺蟎(chlorbenside)、滅幼脲(chlorbenzuron)、冰片丹(chlorbicyclen)、滅落寧(chlorbromuron)、氯草靈(chlorbufam)、可氯丹(chlordane)、氯癸酮(chlordecone)、氯苯甲脒(chlordimeform)、氯烯炔菊酯(chlorempenthrin)、玉雄殺(chloretazate)、乙烯利(chlorethephon)、氯氧磷(chlorethoxyfos)、氯特龍(chloreturon)、伐草克(chlorfenac)、克凡派(chlorfenapyr)、2-(2-氯苯基)-1H-苯并咪唑(chlorfenazole)、殺蟎醇(chlorfenethol)、滅草隆(chlorfenidim)、燕麥酯(chlorfenprop)、殺蟎酯(chlorfenson)、敵蟎丹(chlorfensulphide)、氯芬松(chlorfenvinphos)、氯芬松-甲基(chlorfenvinphos-methyl)、克福隆(chlorfluazuron)、氟咪殺(chlorflurazole)、氯甲丹(chlorflurecol)、氯芴酸(chlorfluren)、整形醇(chlorflurenol)、氯草敏(chloridazon)、氯嘧磺隆(chlorimuron)、氯化物(chlorinate)、氯苯胺靈(chlor-IPC)、氯甲磷(chlormephos)、矮壯素陽離子(chlormequat)、磺草酮(chlormesulone)、甲氧基護谷(chlormethoxynil)、氯乙靈(chlornidine)、全滅草(chlornitrofen)、氯醋酸(chloroacetic acid)、克氯苯(chlorobenzilate)、氯二硝萘(chlorodinitronaphthalene)、殺蟎酯(chlorofénizon)、氯仿、滅蟎脒(chloromebuform)、滅蟲脲(chloromethiuron)、二氯甲氧苯(chloroneb)、氯鼠酮(chlorophacinone)、敵百蟲(chlorophos)、氯化苦(chloropicrin)、三氯丙酸(chloropon)、右旋反式氯丙炔菊酯(chloroprallethrin)、克氯蟎(chloropropylate)、四氯異苯腈(chlorothalonil)、氯麥隆(chlorotoluron)、(chloroxifenidim)、枯草隆(chloroxuron)、羥敵草腈(chloroxynil)、矮形磷(chlorphonium)、氯辛硫磷(chlorphoxim)、滅蟲吡啶(chlorprazophos)、氯普卡(chlorprocarb)、氯普芬(chlorpropham)、陶斯松(chlorpyrifos)、甲基陶斯松(chlorpyrifos-methyl)、四氯喹啉(chlorquinox)、氯磺隆(chlorsulfuron)、大克草(chlorthal)、草克樂(chlorthiamid)、克硫松(chlorthiophos)、(chlortoluron)、克氯得(chlozolinate)、乙菌利(chltosan)、膽鈣化醇(cholecalciferol)、氯化膽鹼、可芬諾(chromafenozide)、環己米特(cicloheximide)、抗倒酯(cimectacarb)、抗倒酯(cimetacarb)、瓜菊酯(cinerin)I、瓜菊酯II、瓜菊酯類(cinerins)、乙基環醯草酯(cinidon-ethyl)、環庚草醚(cinmethylin)、西速隆(cinosulfuron)、津奥啉(cintofen)、苯氰丁醯胺(ciobutide)、落草胺(cisanilide)、順式苄呋菊酯(cismethrin)、氯酰草膦(clacyfos)、環苯草酮(clefoxydim)、克崙吡林(clenpirin)、克崙吡林(clenpyrin)、剋草同(clethodim)、甘寶素(climbazole)、氯碘吡啶酯(cliodinate)、炔草酯(clodinafop)、除線威(cloethocarb)、苯噠嗪鉀(clofencet)、滴滴涕(clofenotane)、克芬蟎(clofentezine)、氯芬磷(clofenvinfos)、氯貝酸(clofibric acid)、氯丁草(clofop)、可滅蹤(clomazone)、克普草(clomeprop)、氯硝柳胺(clonitralid)、調果酸(cloprop)、環丁烯草酮(cloproxydim)、畢克草(clopyralid)、解毒喹(cloquintocet)、氯酯磺草胺(cloransulam)、氯氰碘柳胺(closantel)、可尼丁(clothianidin)、克黴唑(clotrimazole)、座果酸(cloxyfonac)、抑霉胺(cloxylacon)、抑霉胺(clozylacon)、CMA、CMMP、CMP、CMU、十二碳二烯醇(codlelure)、膽骨化醇(colecalciferol)、噻唑硫磷(colophonate)、8-羥基喹啉銅(copper 8-quinolinolate)、乙酸銅、乙醯亞砷酸銅、砷酸銅、碳酸銅、鹼式、氫氧化銅、萘酸銅、油酸銅、氯氧化銅、矽酸銅、硫酸銅、硫酸銅、鹼式、鉻酸銅鋅、氯殺鼠靈(coumachlor)、殺鼠靈(coumafène)、庫馬磷(coumafos)、克滅鼠(coumafuryl)、蠅毒磷(coumaphos)、殺鼠迷(coumatetralyl)、甲香菌酯(coumethoxystrobin)、畜蟲磷(coumithoate)、丁香菌酯(coumoxystrobin)、CPMC、CPMF、CPPC、必滅草(credazine)、甲酚(cresol)、甲苯酚(cresylic acid)、甲基鼠滅定(crimidine)、克羅米通(crotamiton)、丁烯磷(crotoxyfos)、丁烯磷(crotoxyphos)、育畜磷(crufomate)、冰晶石(cryolite)、誘蠅酮(cue-lure)、銅合浦單劑(cufraneb)、二苯隆(cumyleron)、草隆(cumyluron)、福美銅氯(cuprobam)、氧化亞銅、莪術醇(curcumenol)、CVMP、氰胺、氰草淨(cyanatryn)、氰乃淨(cyanazine)、施力松(cyanofenphos)、氰、氰乃松(cyanophos)、果蟲磷(cyanthoate)、氰蟲醯胺(cyantraniliprole)、三聚氰酸、賽座滅(cyazofamid)、賽百摧(cybutryne)、環菌胺(cyclafuramid)、環丙醯胺酸(cyclanilide)、環胺普羅(cyclaniliprole)、環戊烯菊酯(cyclethrin)、環草敵(cycloate)、環己醯亞胺(cycloheximide)、環蟎酯(cycloprate)、乙氰菊酯(cycloprothrin)、環比瑞摩(cyclopyrimorate)、環磺隆(cyclosulfamuron)、環殺草(cycloxydim)、環莠隆(cycluron)、唑蟎氰(cyenopyrafen)、賽芬胺(cyflufenamid)、賽芬蟎(cyflumetofen)、賽扶寧(cyfluthrin)、氯氟氰虫醯胺(cyhalodiamide)、賽伏草(cyhalofop)、賽洛寧(cyhalothrin)、錫蟎丹(cyhexatin)、蟎蜱胺(cymiazole)、克絕(cymoxanil)、解草胺腈(cyometrinil)、伏賜丁(cypendazole)、賽滅寧(cypermethrin)、牧草快(cyperquat)、賽芬寧(cyphenothrin)、環丙津(cyprazine)、三環噻草胺(cyprazole)、環克座(cyproconazole)、賽普洛(cyprodinil)、酯菌胺(cyprofuram)、環草胺(cypromid)、環丙磺醯胺(cyprosulfamide)、賽滅淨(cyromazine)、賽滅磷(cythioate)、賽翠斯(cytrex)、汰草龍(daimuron)、得拉本(dalapon)、丁醯肼(daminozide)、噠幼酮(dayoutong)、邁隆(dazomet)、DBCP、d
-樟腦(d
-camphor)、DCB、DCIP、DCPA(日本)、DCPA(美國)、DCPTA、DCU、DDD、DDPP、DDT、DDVP、咪菌威(debacarb)、癸磷錫(decafentin)、溴氰菊酯(decamethrin)、去甲基克百威(decarbofuran)、避蚊胺(deet)、去氫乙酸、敵草快(deiquat)、異丁草胺(delachlor)、大克松(delnav)、第滅寧(deltamethrin)、甲基滅賜松(demephion)、甲基滅賜松-O、甲基滅賜松-S、内吸磷(demeton)、甲基内吸磷、内吸磷-O、甲基内吸磷-O、内吸磷-S、甲基内吸磷-S、碸吸磷(demeton-S-methyl sulphon)、碸吸磷(demeton-S-methylsulphon)、DEP、生物丙烯菊酯(depalléthrine)、毒利死(derris)、甜菜安(desmedipham)、敵草淨(desmetryn)、敵草淨(desmetryne)、d
-反式氯炔丙菊酯(d
-fanshiluquebingjuzhi)、汰芬隆(diafenthiuron)、氯亞磷(dialifor)、得拉松(dialifos)、燕麥敵(diallate)、燕麥敵(di-allate)、除線特(diamidafos)、麥草畏(dianat)、矽藻土(diatomaceous earth)、矽藻土(diatomite)、大利松(diazinon)、二溴磷(dibrom)、酞酸二丁酯、丁二酸二丁酯、汰克草(dicamba)、異氯磷(dicapthon)、二氯苯腈(dichlobenil)、除線磷(dichlofenthion)、益發靈(dichlofluanid)、二氯萘醌(dichlone)、氯全隆(dichloralurea)、滅幼脲(dichlorbenzuron)、敵草隆(dichlorfenidim)、羧酸芴(dichlorflurecol)、二氯甲丹(dichlorflurenol)、苄胺靈(dichlormate)、二氯丙烯胺(dichlormid)、二氯甲烷、二氯酚(dichlorophen)、2,4-滴丙酸(dichlorprop)、2,4-滴丙酸-P、二氯松(dichlorvos)、賜克滅(dichlozolin)、賜克滅(dichlozoline)、苄氯三唑醇(diclobutrazol)、雙氯氰菌胺(diclocymet)、禾草靈(diclofop)、達滅淨(diclomezine)、大克爛(dicloran)、二氯滅座替(dicloromezotiaz)、雙氯磺草胺(diclosulam)、大克蟎(dicofol)、二氯二苯三氯乙烷(dicophane)、雙香豆素(dicoumarol)、大跨希(dicresyl)、雙特松(dicrotophos)、地快樂(dicryl)、雙羥香豆素(dicumarol)、環蟲腈(dicyclanil)、二環隆(dicyclonon)、地特靈(dieldrin)、得氯蟎(dienochlor)、二依馬(diethamquat)、乙醯甲草胺(diethatyl)、乙硫磷(diethion)、乙硫磷(diéthion)、乙黴威(diethofencarb)、迪艾索諾(dietholate)、(diéthon)、焦碳酸二乙酯(diethyl pyrocarbonate)、二乙甲苯醯胺(diethyltoluamide)、鼠得克(difenacoum)、待克利(difenoconazole)、戊味禾草靈(difenopenten)、枯莠隆(difenoxuron)、野燕枯(difenzoquat)、噻鼠靈(difethialone)、氟蟎(diflovidazin)、二福隆(diflubenzuron)、吡氟草胺(diflufenican)、吡氟草胺(diflufenicanil)、氟吡草腙(diflufenzopyr)、二氟林(diflumetorim)、敵草克(dikegulac)、二羥丙茶鹼(dilor)、滴馬提夫(dimatif)、四氟甲醚菊酯(dimefluthrin)、甲氟磷(dimefox)、唑隆(dimefuron)、殺蟲雙(dimehypo)、哌草丹(dimepiperate)、菌核淨(dimetachlone)、地麥威(dimetan)、混滅威(dimethacarb)、菌核淨(dimethachlone)、二甲草胺(dimethachlor)、異戊乙淨(dimethametryn)、汰草滅(dimethenamid)、汰草滅-P、噻節因(dimethipin)、二甲嘧酚(dimethirimol)、大滅松(dimethoate)、達滅芬(dimethomorph)、苄菊酯(dimethrin)、卡百酸二甲酯(dimethyl carbate)、二硫二甲烷、酞酸二甲酯、二甲基亞硝胺(dimethylvinphos)、敵蠅威(dimetilan)、草滅散(dimexano)、草噠酮(dimidazon)、醚菌胺(dimoxystrobin)、敵匹硫磷(dimpylate)、殺草隆(dimuron)、消蟎酚(dinex)、啶菌噁唑(dingjunezuo)、達克利(diniconazole)、達克利-M、撻乃安(dinitramine)、二硝基酚、大脫蟎(dinobuton)、白粉克(dinocap)、白粉克-4、白粉克-6、敵蟎消(dinocton)、地樂特(dinofenate)、硝戊酯(dinopenton)、硝丙酚(dinoprop)、戊硝酚(dinosam)、達諾殺(dinoseb)、硝辛酯殺蟎劑(dinosulfon)、達特南(dinotefuran)、特樂酚(dinoterb)、硝丁酯(dinoterbon)、苯蟲醚(diofenolan)、殺力松(dioxabenzofos)、二氧威(dioxacarb)、敵殺磷(dioxathion)、敵殺磷(dioxation)、敵鼠(diphacin)、得伐鼠(diphacinone)、得伐鼠(diphenadione)、大芬滅(diphenamid)、大芬滅(diphenamide)、二苯碸、二苯胺、硫化二苯基(diphenylsulphide)、調呋酸(diprogulic acid)、胺樂靈(dipropalin)、殺草淨(dipropetryn)、三氯松(dipterex)、大芬滅替松(dipymetitrone)、雙硫氧吡啶(dipyrithione)、大刈特(diquat)、四硼酸二鈉、殺蟲雙(disosultap)、環氧十九烷(disparlure)、麥草畏甲酯(disugran)、賽松(disul)、二硫龍(disulfiram)、二硫松(disulfoton)、普得松(ditalimfos)、腈硫醌(dithianon)、大賽伏(dithicrofos)、二硫醚、甲基乙拌磷(dithiométon)、汰硫草(dithiopyr)、達有龍(diuron)、二黄原酸(dixanthogen)、d-檸檬油精(d-limonene)、DMDS、DMPA、DNOC、十二環
啉(dodemorph)、多地辛(dodicin)、多寧(dodine)、朵芬娜賓(dofenapyn)、多果定(doguadine)、多明尼卡路(dominicalure)、多滅蟲(doramectin)、DPC、肼菌酮(drazoxolon)、DSMA、右旋反式氯丙炔菊酯(d-trans-allethrin)、右旋反式苄呋菊酯(d-trans-resmethrin)、毒氟磷(dufulin)、殺草隆(dymron)、EBEP、EBP、克線丹(ebufos)、蛻皮甾酮(ecdysterone)、氯唑靈(echlomezol)、EDB、EDC、EDDP、護粒松(edifenphos)、甘草津(eglinazine)、因滅汀(emamectin)、EMPC、益避寧(empenthrin)、烯腺嘌呤(enadenine)、安殺番(endosulfan)、草多索(endothal)、草多索(endothall)、因毒磷(endothion)、安特靈(endrin)、烯肟菌酯(enestroburin)、恩康唑(enilconazole)、烯肟菌酯(enoxastrobin)、除蟎酯(ephirsulfonate)、EPN、丙醯芸苔素內酯(epocholeone)、保幼醚(epofenonane)、依普座(epoxiconazole)、乙醯胺基阿維菌素(eprinomectin)、磺唑草(epronaz)、ε-美特寧(epsilon-metofluthrin)、ε-氧苄氟菊酯(epsilon-momfluorothrin)、EPTC、抑草蓬(erbon)、鈣化醇(ergocalciferol)、二氯醯草胺(erlujixiancaoan)、富右旋反式丙烯菊酯(esdépalléthrine)、益化利(esfenvalerate)、ESP、禾草畏(esprocarb)、乙烯矽(etacelasil)、乙環唑(etaconazole)、抑他風(etaphos)、益地安(etem)、噻唑菌胺(ethaboxam)、克草胺(ethachlor)、乙丁烯氟靈(ethalfluralin)、胺苯磺隆(ethametsulfuron)、殺草胺(ethaprochlor)、乙烯利(ethephon)、磺噻隆(ethidimuron)、愛芬克(ethiofencarb)、硫草敵(ethiolate)、愛殺松(ethion)、乙嗪草酮(ethiozin)、乙蟲腈(ethiprole)、依瑞莫(ethirimol)、益硫磷(ethoate-methyl)、乙氧苯草胺(ethobenzanid)、益覆滅(ethofumesate)、乙基己二醇(ethohexadiol)、滅克磷(ethoprop)、普伏松(ethoprophos)、氯氟草醚(ethoxyfen)、乙氧基喹啉(ethoxyquin)、亞速隆(ethoxysulfuron)、吲唑酯(ethychlozate)、甲酸乙酯(ethyl formate)、焦磷酸乙酯(ethyl pyrophosphate)、乙滴涕(ethylan)、乙基-DDD、乙烯、二溴化乙烯、二氯化乙烯、環氧乙烷、乙蒜素(ethylicin)、乙基汞2,3二羥基丙基硫醇酯(ethylmercury 2,3-dihydroxypropyl mercaptide)、乙基乙酸汞(ethylmercury acetate)、乙基溴化汞(ethylmercury bromide)、乙基氯化汞、乙基磷酸汞、硝草酚(etinofen)、ETM、乙胺草醚(etnipromid)、乙氧苯草胺(etobenzanid)、依芬寧(etofenprox)、依殺蟎(etoxazole)、依得利(etridiazole)、益多松(etrimfos)、益多松(étrimphos)、丁香酚(eugenol)、EXD、凡殺同(famoxadone)、胺磺磷(famphur)、伐草克(fenac)、咪唑菌酮(fenamidone)、敵磺鈉(fenaminosulf)、烯肟菌胺(fenaminstrobin)、芬滅松(fenamiphos)、咪菌腈(fenapanil)、芬瑞莫(fenarimol)、醯苯磺威(fenasulam)、抗蟎唑(fenazaflor)、芬殺蟎(fenazaquin)、芬克座(fenbuconazole)、芬佈賜(fenbutatin oxide)、解草唑(fenchlorazole)、樂乃松(fenchlorphos)、樂乃松(fenchlorfos)、解草啶(fenclorim)、芬硫克(fenethacarb)、五氟苯菊酯(fenfluthrin)、甲呋醯胺(fenfuram)、環醯菌胺(fenhexamid)、非草隆(fenidin)、種衣酯(fenitropan)、撲滅松(fenitrothion)、芬蟎酯(fénizon)、酚菌酮(fenjuntong)、丁基滅必蝨(fenobucarb)、毒菌錫(fenolovo)、2,4,5-涕丙酸(fenoprop)、芬硫克(fenothiocarb)、芬噁寧(fenoxacrim)、芬諾尼(fenoxanil)、芬殺草(fenoxaprop)、芬殺草-P、異噁苯碸(fenoxasulfone)、芬諾克(fenoxycarb)、拌種咯(fenpiclonil)、吡氯氰菊酯(fenpirithrin)、芬普寧(fenpropathrin)、苯鏽啶(fenpropidin)、芬普福(fenpropimorph)、胺苯吡菌酮(fenpyrazamine)、芬普蟎(fenpyroximate)、芬昆諾三酮(fenquinotrione)、殺雄嗪(fenridazon)、芬蟎酯(fenson)、繁福松(fensulfothion)、氯苯氧乙醇(fenteracol)、噻唑禾草靈(fenthiaprop)、芬殺松(fenthion)、乙基芬殺松(fenthion-ethyl)、噻唑禾草靈(fentiaprop)、三苯錫(fentin)、四唑醯草胺(fentrazamide)、芳氟胺(fentrifanil)、非草隆(fenuron)、非草隆TCA、芬化利(fenvalerate)、富爾邦(ferbam)、富米綜(ferimzone)、硫酸亞鐵、芬普尼(fipronil)、麥草氟酯(flamprop)、麥草氟酯-M、伏速隆(flazasulfuron)、伏滅鼠(flocoumafen)、弗美托奎(flometoquin)、氟尼胺(flonicamid)、雙氟磺草胺(florasulam)、嘧蟎酯(fluacrypyrim)、右旋反式氯丙炔菊酯(fluazaindolizine)、伏寄普(fluazifop)、伏寄普-P (fluazifop-P)、扶吉胺(fluazinam)、異丙吡草酯(fluazolate)、氟啶蜱脲(fluazuron)、氟大滅(flubendiamide)、氟苯并胺噻唑(flubenzimine)、溴氟菊酯(flubrocythrinate)、氟酮磺隆(flucarbazone)、氟吡磺隆(flucetosulfuron)、氟消草(fluchloralin)、伏克隆(flucofuron)、氟蟎脲(flucycloxuron)、護賽寧(flucythrinate)、護汰寧(fludioxonil)、聯氟蟎(fluénéthyl)、聯苯氟(fluenetil)、氟噻蟲碸(fluensulfone)、氟噻草胺(flufenacet)、嘧蟲胺(flufenerim)、弗芬肯(flufenican)、氟芬隆(flufenoxuron)、氟菌蟎酯(flufenoxystrobin)、三氟醚菊酯(flufenprox)、氟噠草酯(flufenpyr)、氟蟎嗪(flufenzine)、丁蟲腈(flufiprole)、氟菲殺碸(fluhexafon)、氟氯苯菊酯(flumethrin)、氟醯菌胺(flumetover)、氟節胺(flumetralin)、唑嘧磺草胺(flumetsulam)、氟每淨(flumezin)、氟烯草酸(flumiclorac)、丙炔氟草胺(flumioxazin)、炔草胺(flumipropyn)、氟
啉(flumorph)、可奪草(fluometuron)、氟比來(fluopicolide)、氟吡菌醯胺(fluopyram)、氟殺蟎(fluorbenside)、增糖胺(fluoridamid)、氟乙醯胺(fluoroacetamide)、氟乙酸(fluoroacetic acid)、氟咯草酮(fluorochloridone)、三氟硝草醚(fluorodifen)、乙羧氟草醚(fluoroglycofen)、氟醯亞胺(fluoroimide)、氟氯菌核利(fluoromide)、唑啶草(fluoromidine)、氟除草醚(fluoronitrofen)、氯氟吡氧乙酸(fluoroxypyr)、殺克丹(fluothiuron)、三氟苯唑(fluotrimazole)、氟嘧菌酯(fluoxastrobin)、氟胺草唑(flupoxam)、氟異丙嘧草酯(flupropacil)、氟鼠啶(flupropadine)、氟丙酸(flupropanate)、弗比南載夫隆(flupyradifurone)、氟啶嘧磺隆(flupyrsulfuron)、氟喹唑(fluquinconazole)、氟拉藍(fluralaner)、解草安(flurazole)、抑草丁(flurecol)、抑草丁(flurenol)、氟啶草酮(fluridone)、氟咯草酮(flurochloridone)、氟氯嘧定(fluromidine)、氟氯比(fluroxypyr)、呋嘧醇(flurprimidol)、硫氟磺醯胺(flursulamid)、呋草酮(flurtamone)、護矽得(flusilazole)、氟硫滅(flusulfamide)、氟蟎嗪(flutenzine)、氟噻草酯(fluthiacet)、氟噻草胺(fluthiamide)、氟停安(flutianil)、福多寧(flutolanil)、護汰芬(flutriafol)、福化利(fluvalinate)、氟唑滅特胺(fluxametamide)、氟唑菌醯胺(fluxapyroxad)、肟草安(fluxofenim)、滅菌丹(folpel)、福爾培(folpet)、氟磺胺草醚(fomesafen)、大福松(fonofos)、甲醯胺磺隆(foramsulfuron)、氟吡脲(forchlorfenuron)、甲醛、覆滅蟎(formetanate)、福木松(formothion)、藻蟎威(formparanate)、調節膦(fosamine)、福賽得(fosetyl)、丁苯硫磷(fosmethilan)、甲基氯吡磷(fospirate)、福賽絕(fosthiazate)、丁硫環磷(fosthietan)、弗羅塔林(frontalin)、四氯苯酞(fthalide)、麥穗靈(fuberidazole)、氟草淨(fucaojing)、氟草醚(fucaomi)、氟菌蟎酯(fujunmanzhi)、氟乳醚(fulumi)、薰草呋(fumarin)、氟奈西草林(funaihecaoling)、呋苯硫脲(fuphenthiourea)、乙二醇縮糠醛(furalane)、呋霜靈(furalaxyl)、炔呋菊酯(furamethrin)、福拉比(furametpyr)、呋喃蟲醯肼(furan tebufenozide)、呋線威(furathiocarb)、二甲呋醯胺(furcarbanil)、呋菌唑(furconazole)、呋菌唑(furconazole)-順式、糠醛菊酯(furethrin)、糠醛(furfural)、呋喃解草唑(furilazole)、伴種胺(furmecyclox)、呋甲硫菌靈(furophanate)、呋氧草醚(furyloxyfen)、γ-BHC、γ-賽洛寧(gamma
-cyhalothrin)、γ-HCH、格蟎酯(genit)、赤黴酸(gibberellic acid)、赤黴素A3 (gibberellin A3)、赤黴素(gibberellins)、甘氟(gliftor)、鼠甘伏(glitor)、氯醛葡糖(glucochloralose)、草銨膦(glufosinate)、草銨膦-P、固毆寧(glyodin)、乙二肟(glyoxime)、嘉磷塞(glyphosate)、草甘二膦(glyphosine)、誘蟲十六酯(gossyplure)、誘殺烯混劑(grandlure)、灰黃黴素(griseofulvin)、胍諾克丁(guanoctine)、雙胍辛(guazatine)、丙烯酸喹啉酯(halacrinate)、哈洛昔芬(halauxifen)、合芬寧(halfenprox)、合芬隆(halofenozide)、鹵殺芬(halosafen)、合速隆(halosulfuron)、氟啶草(haloxydine)、合氯氟(haloxyfop)、合氯氟-P、合氯氟-R、HCA、HCB、HCH、六甲蜜胺(hemel)、海母帕(hempa)、HEOD、飛佈達(heptachlor)、烯肟菌(heptafluthrin)、飛達松(heptenophos)、增產肟(heptopargil)、除莠菌素(herbimycin)、除莠菌素A(herbimycin A)、速殺硫磷(heterophos)、六六六(hexachlor)、六六六(hexachloran)、六氯丙酮(hexachloroacetone)、六氯苯、六氯丁二烯、六氯酚(hexachlorophene)、菲克利(hexaconazole)、六伏隆(hexaflumuron)、六伏胺(hexafluoramin)、六氟鹽(hexaflurate)、紅鈴誘烯(hexalure)、己醯胺(hexamide)、菲殺淨(hexazinone)、己硫松(hexylthiofos)、合賽多(hexythiazox)、HHDN、赫洛塞呋(holosulf)、高油菜素内酯(homobrassinolide)、磺硝肟(huancaiwo)、磺蟲淨(huanchongjing)、磺草靈(huangcaoling)、環菌唑(huanjunzuo)、愛美隆(hydramethylnon)、汞加芬(hydrargaphen)、熟石灰(hydrated lime)、氫氰胺(hydrogen cyanamide)、氰化氫(hydrogen cyanide)、烯蟲乙酯(hydroprene)、土菌消(hydroxyisoxazole)、殺紋寧(hymexazol)、水奎威(hyquincarb)、IAA、IBA、IBP、埃卡瑞丁(icaridin)、依滅列(imazalil)、咪草酸(imazamethabenz)、甲氧咪草煙(imazamox)、甲咪唑烟酸(imazapic)、依滅草(imazapyr)、滅草喹(imazaquin)、咪唑乙煙酸(imazethapyr)、依速隆(imazosulfuron)、易胺座(imibenconazole)、新煙鹼類(imicyafos)、益達胺(imidacloprid)、氯噻啉(imidaclothiz)、克熱淨(iminoctadine)、依普寧(imiprothrin)、依納素(inabenfide)、茚草酮(indanofan)、三嗪茚草胺(indaziflam)、因得克(indoxacarb)、枯瘟淨(inezin)、矽藻土(infusorial earth)、碘普尼(iodobonil)、碘卡佈(iodocarb)、丙胺磷(iodofenphos)、碘甲烷(iodomethane)、碘磺隆(iodosulfuron)、碘芬磺隆(iofensulfuron)、碘苯腈(ioxynil)、抑草津(ipazine)、IPC、種菌唑(ipconazole)、鹵苯胺唑(ipfencarbazone)、丙基喜樂松(iprobenfos)、依普同(iprodione)、丙森辛(iprovalicarb)、丙草定(iprymidam)、小蟲二醇烯(ipsdienol)、小蟲醇烯(ipsenol)、IPSP、IPX、依殺米朵孚斯(isamidofos)、依殺松(isazofos)、碳氯靈(isobenzan)、丁咪醯胺(isocarbamid)、丁咪醯胺(isocarbamide)、水胺硫磷(isocarbophos)、異草定(isocil)、異氯甲橋(isodrin)、亞芬松(isofenphos)、甲基亞芬松、艾索非他米(isofetamid)、異索威(isolan)、丁草酮(isomethiozin)、異草完隆(isonoruron)、異潘松(isopamphos)、氮蕈草(isopolinate)、滅必蝨(isoprocarb)、異草定(isoprocil)、異丙樂靈(isopropalin)、異丙吡草酯(isopropazol)、亞賜圃(isoprothiolane)、異丙隆(isoproturon)、萘吡菌胺(isopyrazam)、異皮莫(isopyrimol)、獲賜松(isothioate)、異噻菌胺(isotianil)、愛速隆(isouron)、異凡二酮(isovaledione)、異草胺(isoxaben)、異氯草酮(isoxachlortole)、雙苯噁唑酸(isoxadifen)、異唑草酮(isoxaflutole)、異草醚(isoxapyrifop)、加褔松(isoxathion)、異噁隆(isuron)、依維菌素(ivermectin)、異草胺(ixoxaben)、淨種磷(izopamfos)、淨種磷(izopamphos)、茉莉油(japonilure)、喃烯菊酯(japothrins)、茉酮菊酯素(jasmolin)I、茉酮菊酯素II、茉莉酸(jasmonic acid)、甲磺蒽腙(jiahuangchongzong)、甲基硝啉(jiajizengxiaolin)、甲香菊酯(jiaxiangjunzhi)、解草完(jiecaowan)、解草稀(jiecaoxi)、井崗黴素A(Jinganmycin A)、護粒松(jodfenphos)、青春激素I(juvenile hormone I)、青春激素II、青春激素III、噻嗯菊酯(kadethrin)、κ-畢芬寧(kappa
-bifenthrin)、κ-汰福寧(kappa
-tefluthrin)、特胺靈(karbutilate)、卡列他南(karetazan)、嘉賜黴素(kasugamycin)、柯均林(kejunlin)、氯戊環(kelevan)、酮螺氧(ketospiradox)、矽藻土(kieselguhr)、細胞分裂素(kinetin)、烯蟲炔酯(kinoprene)、精苯霜靈(kiralaxyl)、克收欣(kresoxim-methyl)、庫卡辛(kuicaoxi)、乳氟禾草靈(lactofen)、λ-賽洛寧(lambda-cyhalothrin)、拉提路(latilure)、砷酸鉛(lead arsenate)、環草定(lenacil)、里琵菌素(lepimectin)、福賜松(leptophos)、聯苯肼酯(lianbenjingzhi)、石灰硫磺(lime sulfur)、靈丹(lindane)、雷尼汀(lineatin)、理有龍(linuron)、力輪松(lirimfos)、利露(litlure)、誘池蛾酯(looplure)、祿芬隆(lufenuron)、氯氟氰虫醯胺(lüfuqingchongxianan)、氯醯草膦(lüxiancaolin)、氯啶菌酯(lvdingjunzhi)、氯氟醚菊酯(lvfumijvzhi)、氯醯草膦(lvxiancaolin)、噻唑磷(lythidathion)、M-74、M-81、MAA、磷化鎂、馬拉松(malathion)、麥迪遜(maldison)、順丁烯二醯肼(maleic hydrazide)、特蟎腈(malonoben)、麥芽糊精(maltodextrin)、MAMA、代森錳銅(mancopper)、鋅錳乃浦(mancozeb)、曼戴克敏(mandestrobin)、曼普胺(mandipropamid)、錳乃浦(maneb)、苦參鹼(matrine)、疊氮磷(mazidox)、MCC、MCP、MCPA、硫乙基MCPA、MCPB、MCPP、巴斯丹(mebenil)、滅加松(mecarbam)、苯并威(mecarbinzid)、四甲磷(mecarphon)、2-甲-4-氯丙酸(mecoprop)、2-甲-4-氯丙酸-P、殺蟎脒(medimeform)、地樂施(medinoterb)、誘殺酯(medlure)、滅芬草(mefenacet)、右滅達樂(mefenoxam)、吡唑二酸(mefenpyr)、氟磺醯草胺(mefluidide)、十四碳二烯酸(megatomoic acid)、蜜蠟醇、雙薰草素醇(melitoxin)、MEMC、美納松(menazon)、MEP、滅派林(mepanipyrim)、氯氟醚菊酯(meperfluthrin)、甲苯諾(mephenate)、美福松(mephosfolan)、甲哌啶(mepiquat)、滅普寧(mepronil)、敵蟎普(meptyldinocap)、滅蟲威(mercaptodimethur)、倍硫磷(mercaptophos)、內吸磷(mercaptophos thiol)、馬拉硫磷(mercaptothion)、氯化汞、氧化汞、氯化亞汞、脫葉亞磷(merphos)、脫葉亞磷氧化物(merphos oxide)、滅莠津(mesoprazine)、磺胺磺隆(mesosulfuron)、硝磺草酮(mesotrione)、甲硫酚(mesulfen)、倍硫磷亞碸(mesulfenfos)、每蘇芬(mesulphen)、間甲酚(metacresol)、美氟綜(metaflumizone)、滅達樂(metalaxyl)、右滅達樂(metalaxyl-M)、聚乙醛(metaldehyde)、斯美地(metam)、唑醯草胺(metamifop)、苯草酮(metamitron)、偏磷酸鈣(metaphos)、興豐寶(metaxon)、滅草胺(metazachlor)、雙醚氯吡嘧磺隆(metazosulfuron)、間氯敵菌酮(metazoxolon)、滅特座(metconazole)、甲基涕巴(metepa)、二甲噠草伏(metflurazon)、甲基苯噻隆(methabenzthiazuron)、滅克松(methacrifos)、甲基丙樂靈(methalpropalin)、威百畝(metham)、達馬松(methamidophos)、滅速克(methasulfocarb)、滅草唑(methazole)、呋菌胺(methfuroxam)、甲基苯噻隆(methibenzuron)、滅大松(methidathion)、甲硫苯威(methiobencarb)、滅賜克(methiocarb)、甲硫嘧磺隆(methiopyrisulfuron)、甲硫涕巴(methiotepa)、美西除靈(methiozolin)、滅草恆(methiuron)、殺蟲乙烯磷(methocrotophos)、速滅威(métholcarb)、醚草通(methometon)、納乃得(methomyl)、美賜平(methoprene)、蓋草津(methoprotryn)、格草淨(methoprotryne)、喹啉羧酸-丁基(methoquin-butyl)、甲醚菊酯(methothrin)、甲氧滴滴涕(methoxychlor)、滅芬諾(methoxyfenozide)、去草酮(methoxyphenone)、甲基唑磷嗪(methyl apholate)、溴甲烷、甲基丁香粉(methyl eugenol)、碘甲烷(methyl iodide)、異硫氰酸甲酯(methyl isothiocyanate)、甲基巴拉松(methyl parathion)、甲基乙酯磷(methylacetophos)、甲氯仿、甲基二硫胺甲酸(methyldithiocarbamic acid)、甲基殺草隆(methyldymron)、二氯甲烷、甲基亞芬松(methyl-isofenphos)、甲基倍硫磷(methylmercaptophos)、甲基倍硫磷氧化物(methylmercaptophos oxide)、甲基內吸磷(methylmercaptophos thiol)、甲基苯甲酸汞(methylmercury benzoate)、甲基汞二氰二胺(methylmercury dicyandiamide)、甲基五氯苯氧化汞(methylmercury pentachlorophenoxide)、亞甲癸醯胺(methylneodecanamide)、殺螟硫磷(methylnitrophos)、保棉磷(methyltriazothion)、唑嘧磺草胺(metiozolin)、免得爛(metiram)、免得爛鋅(metiram-zinc)、吡喃隆(metobenzuron)、撲奪草(metobromuron)、美特寧(metofluthrin)、莫多草(metolachlor)、治滅蝨(metolcarb)、苯磺隆(metometuron)、苯氧菌胺(metominostrobin)、磺草唑胺(metosulam)、蟲酮(metoxadiazone)、甲氧隆(metoxuron)、滅芬農(metrafenone)、代森聯(metriam)、滅必淨(metribuzin)、敵百蟲(metrifonate)、敵百蟲(metriphonate)、噻菌胺(metsulfovax)、磺隆(metsulfuron)、美文松(mevinphos)、治克威(mexacarbate)、滅除威(miechuwei)、邁森(mieshuan)、滅蚊菊酯(miewenjuzhi)、密滅汀(milbemectin)、倍脈心(milbemycin oxime)、代森環(milneb)、嘧蟎胺(mimanan)、丙胺氟磷(mipafox)、MIPC、滅蟻樂(mirex)、MNAF、蘑菇醇(moguchun)、稻得壯(molinate)、殺蟲單(molosultap)、氧苄氟菊酯(momfluorothrin)、庚醯草胺(monalide)、莫尼速隆(monisuron)、單甲脒(monoamitraz)、一氯乙酸、亞素靈(monocrotophos)、綠谷龍(monolinuron)、殺蟲單(monomehypo)、舒非侖(monosulfiram)、單嘧磺隆(monosulfuron)、殺蟲單(monosultap)、滅草隆(monuron)、滅草隆TCA、伐草快(morfamquat)、嗎啉胍(moroxydine)、茂硫磷(morphothion)、墨茲(morzid)、莫西菌素(moxidectin)、MPMC、MSMA、MTMC、誘蟲烯(muscalure)、邁克尼(myclobutanil)、滅克寧(myclozolin)、三十醇(myricyl alcohol)、N-(乙基汞)-對-甲苯磺醯胺苯、NAA、NAAm、代森鈉(nabam)、萘肽磷(naftalofos)、乃力松(naled)、萘、萘乙醯胺、萘二甲酸酐(naphthalic anhydride)、萘酞磷(naphthalophos)、萘氧乙酸、萘乙酸、萘啉烷-1,3- 二酮(naphthylindane-1,3-diones)、萘氧基乙酸(naphthyloxyacetic acids)、萘丙胺(naproanilide)、滅落脫(napropamide)、滅落脫-M(napropamide-M)、納得爛(naptalam)、納他黴素(natamycin)、NBPOS、草不隆(neburea)、草不龍(neburon)、安特靈(nendrin)、新菸鹼、尼克羅福(nichlorfos)、除草醚(niclofen)、氯硝柳胺(niclosamide)、啶醯菌胺(nicobifen)、煙嘧磺隆(nicosulfuron)、尼古丁、硫酸菸鹼(nicotine sulfate)、伏蟻靈(nifluridide)、尼克黴素(nikkomycins)、NIP、吡氯草胺(nipyraclofen)、氟氯草胺(nipyralofen)、烯啶蟲胺(nitenpyram)、硝乙脲噻唑(nithiazine)、滅殺草(nitralin)、氯啶(nitrapyrin)、戊氰威(nitrilacarb)、護谷(nitrofen)、三氟甲草醚(nitrofluorfen)、硝苯乙烯(nitrostyrene)、酞菌酯(nitrothal-isopropyl)、鼠特靈(nobormide)、壬醇、鼠特靈(norbormide)、草完隆(norea)、氟草敏(norflurazon)、降菸鹼(nornicotine)、草完隆(noruron)、諾伐隆(novaluron)、多氟脲(noviflumuron)、NPA、尼瑞莫(nuarimol)、諾瑞隆(nuranone)、OCH、八氯二丙基醚、辛噻酮(octhilinone)、鄰二氯苯(o-dichlorobenzene)、呋醯胺(ofurace)、歐滅松(omethoate)、鄰苯基苯酚、坪草丹(orbencarb)、歐弗拉洛(orfralure)、坪草丹(orthobencarb)、鄰二氯苯(ortho-dichlorobenzene)、嘧苯胺磺隆(orthosulfamuron)、歐塔路(oryctalure)、肟醚菌胺(orysastrobin)、歐拉靈(oryzalin)、王草腦(osthol)、王草腦(osthole)、歐斯措莫(ostramone)、除蟎酯(ovatron)、蟎淨(ovex)、解草腈(oxabetrinil)、丙炔草酮(oxadiargyl)、樂滅草(oxadiazon)、毆殺斯(oxadixyl)、草氨酸酯(oxamate)、歐殺滅(oxamyl)、草噠松(oxapyrazon)、草噠松(oxapyrazone)、環氧嘧磺隆(oxasulfuron)、奧賽普林(oxathiapiprolin)、 草酮(oxaziclomefone)、快得寧(oxine-copper)、快得寧(oxine-Cu)、歐索林酸(oxolinic acid)、咪唑(oxpoconazole)、嘉保信(oxycarboxin)、滅多松(oxydemeton-methyl)、異亞碸磷(oxydeprofos)、碸拌磷(oxydisulfoton)、羥烯腺嘌呤(oxyenadenine)、復祿芬(oxyfluorfen)、氧化苦參鹼(oxymatrine)、土黴素(oxytetracycline)、滅蟎猛(oxythioquinox)、PAC、巴克素(paclobutrazol)、哌蟲啶(paichongding)、亞烈寧(palléthrine)、PAP、對-二氯苯(para-dichlorobenzene)、對氟隆(parafluron)、巴拉刈(paraquat)、巴拉松(parathion)、甲基巴拉松、苯吡醇(parinol)、巴黎綠(Paris green)、PCNB、PCP、PCP-Na、對-二氯苯(p-dichlorobenzene)、PDJ、克草猛(pebulate)、消蟎酚(pédinex)、披扶座(pefurazoate)、壬酸(pelargonic acid)、平克座(penconazole)、賓克隆(pencycuron)、施得圃(pendimethalin)、半滴乙酯(penfenate)、戊苯吡菌胺(penflufen)、氟幼脲(penfluron)、二甲戊靈(penoxalin)、平速爛(penoxsulam)、五氯酚(pentachlorophenol)、月桂酸五氯苯酯(pentachlorophenyl laurat)、甲氯醯草胺(pentanochlor)、噻菌胺(penthiopyrad)、百滅寧(pentmethrin)、環戊草酮(pentoxazone)、滅蟻靈(perchlordecone)、苯氟磺安(perfluidone)、百滅寧(permethrin)、烯草胺(pethoxamid)、PHC、氰烯菌胺(phenamacril)、乙基氰烯菌胺(phenamacril-ethyl)、敵磺鈉(phénaminosulf)、葉枯淨(phenazine oxide)、酚那卡貝(phénétacarbe)、棉胺寧(phenisopham)、芬硫磷(phenkapton)、甜菜寧(phenmedipham)、乙基甜菜寧、醯草隆(phenobenzuron)、酚硫殺(phenothiol)、酚丁滅寧(phenothrin)、苯蟎醚(phenproxide)、賽達松(phenthoate)、苯基汞脲(phenylmercuriurea)、苯基乙酸汞(phenylmercury acetate)、苯基汞氯化物(phenylmercury chloride)、焦兒茶酚之苯基汞衍生物(phenylmercury derivative of pyrocatechol)、硝酸苯汞(phenylmercury nitrate)、苯基汞水楊酸鹽(phenylmercury salicylate)、福瑞松(phorate)、毒鼠磷(phosacetim)、裕必松(phosalone)、特丁淨(phosametine)、毒鼠磷(phosazetim)、毒鼠磷(phosazetin)、三磷錫(phoscyclotin)、氯瘟磷(phosdiphen)、乙磷(phosethyl)、硫環磷(phosfolan)、硫環磷-甲基(phosfolan-methyl)、甘胺硫磷(phosglycin)、益滅松(phosmet)、對氯硫磷(phosnichlor)、磷醯胺(phosphamide)、福賜米松(phosphamidon)、膦、草丁膦(phosphinothricin)、磷克(phosphocarb)、磷、三磷錫(phostin)、巴賽松(phoxim)、甲基巴賽松、熱必斯(phthalide)、亞胺硫磷(phthalophos)、胺菊酯(phthalthrin)、皮卡布西(picarbutrazox)、避卡蚋叮(picaridin)、畢克爛(picloram)、氟吡醯草胺(picolinafen)、啶氧菌酯(picoxystrobin)、鏈黴菌素(pimaricin)、殺鼠酮(pindone)、唑啉草酯(pinoxaden)、哌丙靈(piperalin)、哌(piperazine)、胡椒基丁氧化物、胡椒基環己烯酮(piperonyl cyclonene)、哌草磷(piperophos)、哌壯素(piproctanly)、哌壯素(piproctanyl)、增效醛(piprotal)、必美松(pirimetaphos)、比加普(pirimicarb)、滅鼠優(piriminil)、嘧啶氧磷(pirimioxyphos)、必滅松(pirimiphos-ethyl)、亞特松(pirimiphos-methyl)、殺鼠酮(pival)、殺鼠酮(pivaldione)、三氯殺三氯酯(plifenate)、PMA、PMP、聚丁烯(polybutenes)、聚胺甲酸酯(polycarbamate)、多氯化莰烯(polychlorcamphene)、聚乙氧基喹啉(polyethoxyquinoline)、保粒黴素D (polyoxin D)、保粒黴素(polyoxins)、保粒黴素丁(polyoxorim)、多噻烷(polythialan)、亞砷酸鉀(potassium arsenite)、疊氮化鉀(potassium azide)、氰酸鉀、乙基黃原酸鉀(potassium ethylxanthate)、環烷酸鉀(potassium naphthenate)、多硫化鉀(potassium polysulfide)、硫氰酸鉀(potassium thiocyanate)、4,4-滴滴涕(pp’
-DDT)、普亞烈寧(prallethrin)、早熟素I(precocene I)、早熟素II、早熟素III、普拉草(pretilachlor)、嘧啶松(primidophos)、氟嘧磺隆(primisulfuron)、撲殺熱(probenazole)、撲克拉(prochloraz)、丙氯醇(proclonol)、丙腈津(procyazine)、撲滅寧(procymidone)、氨氟樂靈(prodiamine)、佈飛松(profenofos)、氟唑草胺(profluazol)、環丙氟靈(profluralin)、丙氟菊酯(profluthrin)、氯苯噻草酮(profoxydim)、(profurite-aminium)、丙草止津(proglinazine)、調環酸(prohexadione)、茉莉酮(prohydrojasmon)、蜱虱威(promacyl)、普滅克(promecarb)、撲滅通(prometon)、佈滅淨(prometryn)、佈滅淨(prometryne)、捕滅鼠(promurit)、拿草特(pronamide)、雷蒙得(propachlor)、丙蟲磷(propafos)、普羅帕脒(propamidine)、普拔克(propamocarb)、除草寧(propanil)、加護松(propaphos)、普拔草(propaquizafop)、毆蟎多(propargite)、撲蟲菊(proparthrin)、普拔根(propazine)、撲達松(propetamphos)、苯胺靈(propham)、普克利(propiconazole)、羥哌酯(propidine)、甲基鋅乃浦(propineb)、異丙草胺(propisochlor)、安丹(propoxur)、丙苯磺隆(propoxycarbazone)、丙基增效劑(propyl isome)、咪唑嘧磺隆(propyrisulfuron)、戊炔草胺(propyzamide)、丙氧喹啉(proquinazid)、骨酯素(prosuler)、甲硫磺樂靈(prosulfalin)、苄草丹(prosulfocarb)、三氟丙磺隆(prosulfuron)、乙噻唑磷(prothidathion)、胺丙威(prothiocarb)、丙硫菌唑(prothioconazole)、普硫松(prothiofos)、飛克松(prothoate)、丙苯烴菊酯(protrifenbute)、撲滅生(proxan)、吡嘧丹磷(prymidophos)、丙炔草胺(prynachlor)、補骨脂素(psoralen)、補骨脂素(psoralene)、吡達農(pydanon)、氟唑菌醯羥胺(pydiflumetofen)、派福布敏(pyflubumide)、派滅淨(pymetrozine)、賜加落(pyracarbolid)、白克松(pyraclofos)、雙唑草腈(pyraclonil)、百克敏(pyraclostrobin)、派芬草(pyraflufen)、必伏清(pyrafluprole)、嘧啶威(pyramat)、唑胺菌酯(pyrametostrobin)、唑菌酯(pyraoxystrobin)、磺醯草吡唑(pyrasulfotole)、必記福敏(pyraziflumid)、(pyrazolate)、苄草唑(pyrazolynate)、殺草敏(pyrazon)、白粉松(pyrazophos)、百速隆(pyrazosulfuron)、彼硫磷(pyrazothion)、普芬草(pyrazoxyfen)、吡菊酯(pyresmethrin)、除蟲菊精I、除蟲菊精II、除蟲菊精類、草醚-異丙基(pyribambenz-isopropyl)、草醚-丙基(pyribambenz-propyl)、吡菌苯威(pyribencarb)、嘧啶肟草醚(pyribenzoxim)、稗草丹(pyributicarb)、氯草定(pyriclor)、畢達本(pyridaben)、噠草福(pyridafol)、啶蟲丙醚(pyridalyl)、必芬松(pyridaphenthion)、噠嗪硫磷(pyridaphenthione)、必汰草(pyridate)、雙滴保(pyridinitril)、比芬諾(pyrifenox)、氟蟲吡喹(pyrifluquinazon)、環酯草醚(pyriftalid)、吡嘧他磷(pyrimétaphos)、派美尼(pyrimethanil)、抗蚜威(pyrimicarbe)、畢汰芬(pyrimidifen)、嘧草醚(pyriminobac)、嘧蟎胺(pyriminostrobin)、乙基嘧啶磷(pyrimiphos-éthyl)、甲基嘧啶磷(pyrimiphos-méthyl)、吡嘧蘇芬(pyrimisulfan)、嘧硫磷(pyrimitate)、滅鼠優(pyrinuron)、甲氧苯啶菌(pyriofenone)、必清(pyriprole)、吡啶醇(pyripropanol)、百利普芬(pyriproxyfen)、啶菌噁唑(pyrisoxazole)、嘧硫草醚(pyrithiobac)、吡唑威(pyrolan)、百快隆(pyroquilon)、吡唑碸(pyroxasulfone)、甲氧磺草胺(pyroxsulam)、氯甲氧吡啶(pyroxychlor)、氯吡根呋醚(pyroxyfur)、嗪草酸(qincaosuan)、青枯靈(qingkuling)、苦木(quassia)、喹烯酮(quinacetol)、拜裕松(quinalphos)、甲基拜裕松、醌菌腙(quinazamid)、快克草(quinclorac)、喹克座(quinconazole)、氯甲喹啉酸(quinmerac)、滅藻醌(quinoclamine)、滅蟎猛(quinomethionate)、氯藻胺(quinonamid)、畜寧磷(quinothion)、快諾芬(quinoxyfen)、喹硫磷(quintiofos)、五氯硝苯(quintozene)、快伏草(quizalofop)、快伏草-P、驅蚊酯(quwenzhi)、驅蠅啶(quyingding)、吡咪唑(rabenzazole)、碘醚柳胺(rafoxanide)、(R-diniconazole)、二乙基苯甲醯胺(rebemide)、敵草快(reglone)、瑞毒隆(renriduron)、列卡路(rescalure)、列滅寧(resmethrin)、硫氰苯胺(rhodethanil)、鬧羊花毒素-III(rhodojaponin-III)、病毒唑(ribavirin)、碸嘧磺隆(rimsulfuron)、丁蟲腈(rizazole)、R-滅達樂(R-metalaxyl)、硫氰苯胺(rodéthanil)、皮蠅磷(ronnel)、魚藤酮(rotenone)、蘭尼汀(ryania)、沙巴藜蘆(sabadilla)、嘧啶肟草醚(saflufenacil)、噻菌茂(saijunmao)、噻森銅(saisentong)、柳醯胺苯、氟矽菊酯(salifluofen)、血根鹼(sanguinarine)、山道年(santonin)、右亞列寧(S-bioallethrin)、八甲焦磷醯胺(schradan)、海蔥糖苷(scilliroside)、另丁津(sebuthylazine)、仲丁通(secbumeton)、環丙吡菌胺(sedaxane)、色拉菌素(selamectin)、單甲咪(semiamitraz)、增效菊(sesamex)、芝麻啉(sesamolin)、西松(sesone)、西殺草(sethoxydim)、西維因(sevin)、雙甲胺草磷(shuangjiaancaolin)、雙甲胺草磷(shuangjianancaolin)、S-烯蟲乙酯(S-hydroprene)、環草隆(siduron)、西福明津治(sifumijvzhi)、誘蟲環(siglure)、矽護芬(silafluofen)、雜氮矽三環(silatrane)、矽氣凝膠(silica aerogel)、矽膠、矽噻菌胺(silthiofam)、矽噻菌胺(silthiopham)、矽噻菌胺(silthiophan)、2,4,5-涕丙酸(silvex)、草滅淨(simazine)、矽氟唑(simeconazole)、西瑪通(simeton)、西草淨(simetryn)、西草淨(simetryne)、殺雄啉(sintofen)、S-烯蟲炔酯(S-kinoprene)、熟石灰(slaked lime)、SMA、S-美賜平(S-methoprene)、左旋莫多草(S-metolachlor)、亞砷酸鈉、疊氮化鈉、氯酸鈉、氰化鈉、氟化鈉、氟乙酸鈉、六氟矽酸鈉、環烷酸鈉(sodium naphthenate)、鄰苯基苯酚化鈉(sodium o-phenylphenoxide)、鄰苯基苯酚化鈉(sodium orthophenylphenoxide)、五氯酚鈉(sodium pentachlorophenate)、五氯酚鈉(sodium pentachlorophenoxide)、多硫化鈉(sodium polysulfide)、氟矽酸鈉(sodium silicofluoride)、四硫代硫酸鈉(sodium tetrathiocarbonate)、硫氰酸鈉、斯隆(solan)、蘇硫磷(sophamide)、賜諾特(spinetoram)、賜諾殺(spinosad)、賜派芬(spirodiclofen)、螺甲蟎酯(spiromesifen)、螺蟲乙酯(spirotetramat)、螺環菌胺(spiroxamine)、司替羅磷(stirofos)、鏈黴素(streptomycin)、番木鼈鹼(strychnine)、食菌甲誘醇(sulcatol)、殺克隆(sulcofuron)、磺草酮(sulcotrione)、草克死(sulfallate)、氟磺唑草胺(sulfentrazone)、舒非侖(sulfiram)、氟蟲胺(sulfluramid)、磺噻隆(sulfodiazole)、嘧磺隆(sulfometuron)、草硫磷(sulfosate)、磺醯磺隆(sulfosulfuron)、治螟磷(sulfotep)、治螟磷(sulfotepp)、氟啶蟲胺腈(sulfoxaflor)、亞碸(sulfoxide)、硫肟磷(sulfoxime)、硫、硫酸、磺醯氟、蘇葡卡賓(sulglycapin)、草硫磷(sulphosate)、硫丙磷(sulprofos)、戊苯碸(sultropen)、滅草靈(swep)、τ-福化利(tau
-fluvalinate)、稗草烯(tavron)、噻蟎威(tazimcarb)、TBTO、TBZ、TCA、TCBA、TCMTB、TCNB、TDE、得克利(tebuconazole)、得芬諾(tebufenozide)、得芬瑞(tebufenpyrad)、異丁乙氧喹啉(tebufloquin)、丁基嘧啶磷(tebupirimfos)、牧草胺(tebutam)、得匍隆(tebuthiuron)、克枯爛(tecloftalam)、四氯硝基苯(tecnazene)、福美雙聯(tecoram)、三氯殺蟎碸(tedion)、得福隆(teflubenzuron)、汰福寧(tefluthrin)、特呋三酮(tefuryltrione)、環磺酮(tembotrione)、替美磷(temefos)、亞培松(temephos)、替哌(tepa)、TEPP、得殺草(tepraloxydim)、吡喃草酮(teproloxydim)、環戊烯丙菊酯(terallethrin)、特草定(terbacil)、特草靈(terbucarb)、特丁草胺(terbuchlor)、托福松(terbufos)、特丁通(terbumeton)、特丁津(terbuthylazine)、芽根靈(terbutol)、特丁淨(terbutryn)、特丁淨(terbutryne)、五氯硝基苯(terraclor)、土黴素(terramicin)、土黴素(terramycin)、四環唑(tetcyclacis)、四氯乙烷(tetrachloroethane)、樂本松(tetrachlorvinphos)、四克利(tetraconazole)、得脫蟎(tetradifon)、殺蟎好(tetradisul)、四氟隆(tetrafluron)、治滅寧(tetramethrin)、四氟醚菊酯(tetramethylfluthrin)、四胺、殺蟎黴素(tetranactin)、四普羅(tetraniliprole)、四氟丙酸鈉(tetrapion)、殺蟎硫醚(tetrasul)、硫酸鉈(thallium sulfate)、硫酸鉈(thallous sulfate)、欣克草(thenylchlor)、θ-賽滅寧(cypermethrin)、腐絕(thiabendazole)、賽果培(thiacloprid)、噻二(thiadiazine)、噻噠氟(thiadifluor)、賽速安(thiamethoxam)、噻磺隆(thiameturon)、蟲腈(thiapronil)、噻氟隆(thiazafluron)、噻氟隆(thiazfluron)、噻唑(thiazone)、噻草啶(thiazopyr)、賽伏(thicrofos)、噻菌腈(thicyofen)、噻二唑草胺(thidiazimin)、噻苯隆(thidiazuron)、酮脲磺草吩酯(thiencarbazone)、噻吩磺隆(thifensulfuron)、賽氟滅(thifluzamide)、乙汞硫柳酸鈉(thimerosal)、甲拌磷(thimet)、殺丹(thiobencarb)、抗蟲威(thiocarboxime)、硫氯苯亞胺(thiochlorfenphim)、硫氯苯亞胺(thiochlorphenphime)、氰硫二硝基苯(thiocyanatodinitrobenzenes)、硫賜安(thiocyclam)、硫丹(thiodan)、噻菌-銅(thiodiazole-copper)、硫敵克(thiodicarb)、久效威(thiofanocarb)、硫伐隆(thiofanox)、硫氟肟(thiofluoximate)、不育硫磷(thiohempa)、硫柳汞(thiomersal)、硫滅松(thiometon)、治線磷(thionazin)、多保淨(thiophanate)、乙基多保淨(thiophanate-ethyl)、甲基多保淨(thiophanate-methyl)、對硫磷(thiophos)、克殺蟎(thioquinox)、胺基硫脲(thiosemicarbazide)、殺蟲雙(thiosultap)、噻替派(thiotepa)、殺線威(thioxamyl)、得恩地(thiram)、秋蘭姆(thiuram)、蘇力菌素(thuringiensin)、噻苯達唑(tiabendazole)、噻醯菌胺(tiadinil)、氟丙嘧草酯(tiafenacil)、調劑胺(tiaojiean)、TIBA、噻蟎胺(tifatol)、仲草丹(tiocarbazil)、啼草胺(tioclorim)、替奧沙芬(tioxazafen)、替係米(tioxymid)、威線肟(tirpate)、TMTD、脫克松(tolclofos-methyl)、脫芬瑞(tolfenpyrad)、托普洛卡(tolprocarb)、托普瑞蕾特(tolpyralate)、對甲抑菌靈(tolyfluanid)、甲基益發靈(tolylfluanid)、甲苯基乙酸汞、托馬蘭(tomarin)、吡草磺(topramezone)、德克沙芬(toxaphene)、TPN、三甲苯草酮(tralkoxydim)、溴氯氰菊酯(tralocythrin)、泰滅寧(tralomethrin)、曲洛比利(tralopyril)、拜富寧(transfluthrin)、反式百滅寧(transpermethrin)、曲他胺(tretamine)、三十烷醇(triacontanol)、三泰芬(triadimefon)、三泰隆(triadimenol)、氟酮磺草胺(triafamone)、野麥畏(triallate)、野麥畏(tri-allate)、三唑磷胺(triamiphos)、抑芽唑(triapenthenol)、三苯噻蟎吩(triarathene)、嘧菌醇(triarimol)、醚苯磺隆(triasulfuron)、唑蚜威(triazamate)、丁三唑(triazbutil)、三氟草胺(triaziflam)、三落松(triazophos)、乙基谷硫磷(triazothion)、唑菌(triazoxide)、鹼式氯化銅(tribasic copper chloride)、三元硫酸銅(tribasic copper sulfate)、苯磺隆(tribenuron)、脫葉磷(tribufos)、氧化三丁基錫、殺草畏(tricamba)、水楊菌胺(trichlamide)、三氯吡氧乙酸(trichlopyr)、三氯松(trichlorfon)、樂乃松(trichlormetaphos)-3、毒壤膦(trichloronat)、壤蟲磷(trichloronate)、三氯三硝基苯(trichlorotrinitrobenzenes)、敵百蟲(trichlorphon)、三氯比(triclopyr)、三環吡菌威(triclopyricarb)、三甲酚(tricresol)、三賽唑(tricyclazole)、三環己基氫氧化錫(tricyclohexyltin hydroxide)、三得芬(tridemorph)、滅草環(tridiphane)、草達津(trietazine)、蝸螺殺(trifenmorph)、三氯丙氧磷(trifenofos)、三氟敏(trifloxystrobin)、三氟啶磺隆(trifloxysulfuron)、三福戴嗎沙(trifludimoxazin)、三福滅作派林(triflumezopyrim)、賽福座(triflumizole)、三福隆(triflumuron)、三福林(trifluralin)、氟胺磺隆(triflusulfuron)、三氟苯氧丙酸(trifop)、三氟禾草肟(trifopsime)、賽福寧(triforine)、三羥基三、誘蠅羧酯(trimedlure)、混滅威(trimethacarb)、三甲隆(trimeturon)、抗倒酯(trinexapac)、三苯錫(triphenyltin)、烯蟲硫酯(triprene)、三丙丹(tripropindan)、雷公藤甲素(triptolide)、草達克(tritac)、殺蟲釘(trithialan)、滅菌唑(triticonazole)、三氟甲磺隆(tritosulfuron)、特朗扣(trunc-call)、脱葉磷(tuoyelin)、單克素(uniconazole)、單克素(uniconazole)-P、福美甲胂(urbacide)、烏瑞替派(uredepa)、戊酸酯(valerate)、維利黴素(validamycin)、維利黴素A(validamycin A)、伐利芬奈蕾特(valifenalate)、異殺鼠酮(valone)、繁米松(vamidothion)、泛佳(vangard)、凡力(vaniliprole)、萬隆(vernolate)、免克寧(vinclozolin)、維生素D3 (vitamin D3)、華法林(warfarin)、硝蟲硫磷(xiaochongliulin)、辛菌胺(xinjunan)、烯肟菌胺(xiwojunan)、烯肟菌酯(xiwojunzhi)、XMC、二甲苯草胺(xylachlor)、二甲苯酚(xylenols)、滅爾蝨(xylylcarb)、噻蟎胺(xymiazole)、依希淨(yishijing)、氰菌胺(zarilamid)、玉米素(zeatin)、增效胺(zengxiaoan)、增效林(zengxiaolin)、ζ-賽滅寧(zeta-cypermethrin)、萘酸鋅、磷化鋅(zinc phosphide)、噻唑鋅(zinc thiazole)、噻唑鋅(zinc thiozole)、三氯酚鋅(zinc trichlorophenate)、三氯酚鋅(zinc trichlorophenoxide)、鋅乃浦(zineb)、福美鋅(ziram)、左拉伏(zolaprofos)、華法林鈉(zoocoumarin)、座賽胺(zoxamide)、唑胺菌酯(zuoanjunzhi)、唑草胺(zuocaoan)、唑菌酯(zuojunzhi)、唑嘧磺隆(zuomihuanglong)、α-氯醇(α-chlorohydrin)、α-蛻皮激素(α-ecdysone)、α-多紋素(α-multistriatin)、α-萘乙酸(α-naphthaleneacetic acid),及β-蛻皮激素(β-ecdysone);(2)
下列分子(a)
N-(3-氯-1-(吡啶-3-基)-1H-吡唑-4-基)-N-乙基-3-((3,3,3-三
氟丙基)硫)丙醯胺(此後稱為“AI–1
”) (b)
(3S,6S,7R,8R)-8-苯甲基-3-(3-((異丁醯氧基)甲氧基)-4-甲氧基吡啶甲醯胺基)-6-甲基-4,9-二氧-1,5-二氧雜環壬-7-基 異丁酸酯((3S,6S,7R,8R)–8–benzyl–3–(3–((isobutyryloxy)methoxy)–4–methoxypicolinamido)–6–methyl–4,9–dioxo–1,5–dioxonan–7–yl isobutyrate) (此後稱為“AI–2
”) (3)
一種被稱為羅提蘭(Lotilaner)的分子,其具有下列結構;以及(4)
表A中的下列分子表A- M#- 活性成分 的結構
如在本揭示中使用,上文各者為一種活性成分。關於更多資訊,請查閱位於Alanwood.net
之“Compendium of Pesticide Common Names
”,及位於bcpcdata.com.
之“The Pesticide Manual
”之各種版本,包括在線版。
特別佳的活性成分之選擇是1,3-二氯丙烯、陶斯松(chlorpyrifos)、六伏隆(hexaflumuron)、滅芬諾(methoxyfenozide)、多氟脲(noviflumuron)、賜諾特(spinetoram)、賜諾殺(spinosad)、氟啶蟲胺腈(sulfoxaflor),以及磺醯氟(此後稱為“AIGA–2
”)。
此外,另一特別佳的活性成分之選擇是亞醌蟎(acequinocyl)、亞滅培(acetamiprid)、乙醯蟲腈(acetoprole)、阿維菌素(avermectin)、谷速松(azinphos-methyl)、必芬蟎(bifenazate)、畢芬寧(bifenthrin)、胺甲(carbaryl)、加保扶(carbofuran)、克凡派(chlorfenapyr)、克福隆(chlorfluazuron)、可芬諾(chromafenozide)、可尼丁(clothianidin)、賽扶寧(cyfluthrin)、賽滅寧(cypermethrin)、第滅寧(deltamethrin)、汰芬隆(diafenthiuron)、因滅汀苯甲酸鹽(emamectin benzoate)、安殺番(endosulfan)、益化利(esfenvalerate)、乙蟲腈(ethiprole)、依殺蟎(etoxazole)、芬普尼(fipronil)、氟尼胺(flonicamid)、嘧蟎酯(fluacrypyrim)、γ-賽洛寧(gamma
-cyhalothrin)、合芬隆(halofenozide)、因得克(indoxacarb)、λ-賽洛寧(lambda
-cyhalothrin)、祿芬隆(lufenuron)、馬拉松(malathion)、納乃得(methomyl)、諾伐隆(novaluron)、百滅寧(permethrin)、啶蟲丙醚(pyridalyl)、畢汰芬(pyrimidifen)、賜派芬(spirodiclofen)、得芬諾(tebufenozide)、賽果培(thiacloprid)、賽速安(thiamethoxam)、硫敵克(thiodicarb)、脫芬瑞(tolfenpyrad),以及ζ-賽滅寧(zeta
-cypermethrin) (此後稱為“AIGA–3
”)。
術語「烯基
」意指由碳及氫組成之非環狀、不飽和(至少一個碳-碳雙鍵)、分支鏈或未分支的取代基,例如乙烯基、烯丙基、丁烯基、戊烯基及己烯基。
術語「烯氧基
」係指進一步由碳-氧單鍵組成之烯基,如烯丙基氧基、丁烯氧基、戊烯氧基、己烯氧基。
術語「烷氧基
」係指進一步由碳-氧單鍵組成之烷基,如甲氧基、乙氧基、丙氧基、異丙氧基、丁氧基,以及三級丁氧基。
術語「烷基
」係指由碳及氫組成之非環狀、飽和、分支鏈或未分支的取代基,例如甲基、乙基、丙基、異丙基、丁基及三級丁基。
術語「炔基
」意指由碳及氫組成之非環狀、不飽和(至少一個碳-碳參鍵)、分支鏈或未分支的取代基,例如乙炔基、炔丙基、丁炔基及戊炔基。
術語「炔氧基
」意指進一步由碳-氧單鍵組成之炔基,例如戊炔氧基、己炔氧基、庚炔氧基及辛炔氧基。
術語「芳基
」意指由氫及碳組成之環狀、芳香族取代基,例如苯基、萘基及聯苯。
術語「生物性殺蟲劑
」意指一種微生物型生物性害蟲防治劑,一般而言,係以與化學性殺蟲劑類似的方式來施用。通常其等為細菌型,但亦有真菌控制劑之實例,包括木黴屬(Trichoderma spp
.)及白粉寄生孢(Ampelomyces quisqualis
)。一種眾所周知的生物性殺蟲劑實例為芽孢桿菌屬(Bacillus
)物種,其係一種鱗翅目(Lepidoptera)、鞘翅目(Coleoptera)及雙翅目(Diptera)之細菌性疾病。生物性殺昆蟲劑包括以下列為基礎之產物:昆蟲致病性真菌(如黑殭菌(Metarhizium anisopliae
)),昆蟲致病性線蟲(如蕪菁夜蛾斯氏線蟲(Steinernema feltiae
)),以及昆蟲致病性病毒(如蘋果蠹蛾(Cydia pomonella
)顆粒體病毒)。昆蟲致病性生物體的其他實例包括但不限於桿狀病毒、原生動物及微孢子目(Microsporidia)。為了避免疑問,生物性殺蟲劑為活性成分。
術語「環烯基
」意指由碳與氫組成之單環或多環、不飽和(至少一碳-碳雙鍵)取代基,例如環丁烯基、環戊烯基、環己烯基、降莰烯、雙環[2.2.2]辛烯基、四氫萘基、六氫萘基,以及八氫萘基。
術語「環烯氧基
」係指更進一步由碳-氧單鍵組成之環烯基,例如環丁烯氧基、環戊烯氧基、降莰烯氧基,以及雙環[2.2.2]辛烯氧基。
術語「環烷基
」係指由碳與氫組成之單環或多環、飽和取代基,例如環丙基、環丁基、環戊基、降莰烯、雙環[2.2.2]辛基與十氫萘。
術語「環烷氧基
」係指更進一步由碳-氧單鍵組成之環烷基,如環丙氧基、環丁氧基、環戊氧基、降莰烯氧基與雙環[2.2.2]辛基氧基。
術語「鹵基
」係指氟、氯、溴與碘。
術語「鹵烷氧基
」係指一烷氧基,其進一步由一至最大可能數目之相同或相異之鹵素組成,如氟甲氧基、三氟甲氧基、2,2-二氟丙氧基、氯甲氧基、三氯甲氧基、1,1,2,2-四氟乙氧基與五氟乙氧基。
術語「鹵烷基
」係指進一步由一至最大可能數目、相同或相異之鹵素組成之烷基,如氟甲基、三氟甲基、2,2-二氟丙基、氯甲基、三氯甲基與1,1,2,2-三氟乙基。
術語「雜環基
」意指可能為芳香族、完全飽和,或部分或完全不飽和的環狀取代基,其中該環狀結構含有至少一個碳及至少一個雜原子,其中該雜原子為氮、硫或氧。實例為:(1) 芳香性雜環 基 取代基
包括,但不限於苯并呋喃基、苯并異噻唑基、苯并異唑基、苯并噻吩基、苯并噻唑基、苯并唑基、啉基(cinnolinyl)、呋喃基、咪唑基、吲唑基、吲哚基、異吲哚基、異喹啉基、異噻唑基、異唑基、二唑基、唑啉基、唑基、呔基、吡基、吡唑啉基、吡唑基、嗒基、吡啶基、嘧啶基、吡咯基、喹唑啉基、喹啉基、喹喏啉基、四唑基、噻唑啉基、噻唑基、噻吩基、三基及三唑基;(2) 完全飽和之雜環基取代基
包括,但不限於:六氫吡基、哌啶基、嗎啉基、吡咯啶基、四氫呋喃基,及四氫哌喃基;(3) 部分 或完全 不飽和的雜環基取代基
包括,但不限於4,5-二氫-異唑基、、4,5-二氫-唑基、4,5-二氫-1H
-吡唑基、2,3-二氫-[1,3,4]-二唑基,以及1,2,3,4-四氫喹啉基;以及(4)
額外的雜環基實例包括以下各者: 硫化三亞甲基 硫化三亞甲基-氧化物 硫化三亞甲基-二氧化物。
術語「所在地
」意指一棲息地、養育場、植物、種子、土壤、材料,或害蟲將生長或能走過之環境。舉例而言,所在地可為:生長中之農作物、樹木、水果、穀物、飼料種類、葡萄、草皮,及/或觀賞植物之處;圈養動物居住之處;建築之內部或外部表面(如儲存穀物之處);建築內所使用之建構材料(如浸漬木材);以及建築附近之土壤。
用語「MoA 材料
」意指一種活性成分,其具有如同位於 irac-online.org.,IRAC MoA Classification v. 7.4中所示的作用模式(「MoA
」),描述以下幾組。(1) 乙醯膽鹼酯酶(AChE) 抑制劑
,包括下列活性成分:毆殺松(acephate)、棉鈴威(alanycarb)、得滅克(aldicarb)、亞滅松(azamethiphos)、乙基谷速松(azinphos-ethyl)、谷速松(azinphos-methyl)、免敵克(bendiocarb)、免扶克(benfuracarb)、佈嘉信(butocarboxim)、丁酮碸威(butoxycarboxim)、硫線磷(cadusafos)、胺甲(carbaryl)、加保扶(carbofuran)、丁基加保扶(carbosulfan)、氯氧磷(chlorethoxyfos)、氯芬松(chlorfenvinphos)、氯甲磷(chlormephos)、陶斯松(chlorpyrifos)、甲基陶斯松(chlorpyrifos-methyl)、蠅毒磷(coumaphos)、氰乃松(cyanophos)、甲基内吸磷-S、大利松(diazinon)、二氯松(dichlorvos)/DDVP、雙特松(dicrotophos)、大滅松(dimethoate)、二甲基亞硝胺(dimethylvinphos)、二硫松(disulfoton)、EPN、愛芬克(ethiofencarb)、愛殺松(ethion)、普伏松(ethoprophos)、胺磺磷(famphur)、芬滅松(fenamiphos)、撲滅松(fenitrothion)、丁基滅必蝨(fenobucarb)、芬殺松(fenthion)、覆滅蟎(formetanate)、福賽絕(fosthiazate)、呋線威(furathiocarb)、飛達松(heptenophos)、新煙鹼類(imicyafos)、亞芬松(isofenphos)、滅必蝨(isoprocarb)、異丙基 O-(甲氧基胺基硫基-磷醯基)水楊酸酯、加褔松(isoxathion)、馬拉松(malathion)、滅加松(mecarbam)、達馬松(methamidophos)、滅大松(methidathion)、滅賜克(methiocarb)、納乃得(methomyl)、治滅蝨(metolcarb)、美文松(mevinphos)、亞素靈(monocrotophos)、乃力松(Naled)、歐滅松(omethoate)、歐殺滅(oxamyl)、滅多松(oxydemeton-methyl)、巴拉松(parathion)、甲基巴拉松、賽達松(phenthoate)、福瑞松(phorate)、裕必松(phosalone)、益滅松(phosmet)、福賜米松(phosphamidon)、巴賽松(phoxim)、比加普(pirimicarb)、亞特松(pirimiphos-methyl)、佈飛松(profenofos)、撲達松(propetamphos)、安丹(propoxur)、普硫松(prothiofos)、白克松(pyraclofos)、必芬松(pyridaphenthion)、拜裕松(quinalphos)、治螟磷(sulfotep)、丁基嘧啶磷(tebupirimfos)、亞培松(temephos)、托福松(terbufos)、樂本松(tetrachlorvinphos)、硫敵克(thiodicarb)、硫伐隆(thiofanox)、硫滅松(thiometon)、唑蚜威(triazamate)、三落松(triazophos)、三氯松(trichlorfon)、混滅威(trimethacarb)、繁米松(vamidothion)、XMC,以及滅爾蝨(xylylcarb)。(2) GABA- 閘控型氯離子通道拮抗劑
,包括下列活性成分:可氯丹(chlordane)、安殺番(endosulfan)、乙蟲腈(ethiprole),以及芬普尼(fipronil)。(3) 鈉離子通道調節劑
,包括下列活性成分:阿納寧(acrinathrin)、亞列寧(allethrin)、右旋 - 順式- 反式
氯丙炔菊酯(d–cis–trans
allethrin)、右旋反式
氯丙炔菊酯(d-trans
-allethrin)、畢芬寧(bifenthrin)、百亞列寧(bioallethrin)、S–環戊烯基百亞列寧 (bioallethrin S–cyclopentenyl)、生物苄呋菊酯(bioresmethrin)、乙氰菊酯(cycloprothrin)、賽扶寧(cyfluthrin)、β-賽扶寧、賽洛寧(cyhalothrin)、λ-賽洛寧(lambda-
cyhalothrin)、γ-賽洛寧、賽滅寧(cypermethrin)、α-賽滅寧、β-賽滅寧、θ-賽滅寧、ζ-賽滅寧、賽酚寧[(1R)– 反式
–異構物] (cyphenothrin [(1R)–trans
–isomers])、第滅寧(deltamethrin)、益避寧[(EZ
)–(1R
)–異構物] (empenthrin[(EZ
)–(1R
)–isomers])、益化利(esfenvalerate)、依芬寧(etofenprox)、芬普寧(fenpropathrin)、芬化利(fenvalerate)、護賽寧(flucythrinate)、氟氯苯菊酯(flumethrin)、τ-福化利(tau
-fluvalinate)、合芬寧(halfenprox)、依普寧(imiprothrin)、噻嗯菊酯(kadethrin)、百滅寧(permethrin)、酚丁滅寧[(1R)– 反式
–異構物] (phenothrin [(1R)–trans
–isomer])、普亞烈寧(prallethrin)、除蟲菊精(除蟲菊酯(pyrethrum))、吡菊酯(pyresmethrin)、矽護芬(silafluofen)、汰福寧(tefluthrin)、治滅寧(tetramethrin)、治滅寧[(1R
)–異構物]、泰滅寧(tralomethrin),以及甲氧滴滴涕(methoxychlor)。(4) 菸 鹼型乙醯膽鹼(nAChR) 協同劑
,包括下列活性成分:(4A)
亞滅培(acetamiprid)、可尼丁(clothianidin)、達特南(dinotefuran)、益達胺(imidacloprid)、烯啶蟲胺(nitenpyram)、賽果培(thiacloprid)、賽速安(thiamethoxam),(4B)
尼古丁,(4C)
氟啶蟲胺腈(sulfoxaflor),(4D)
弗比南載夫隆(flupyradifurone),(4E)
三福滅作派林(triflumezopyrim)及二氯滅座替(dicloromezotiaz)。(5) 菸 鹼型乙醯膽鹼受器(nAChR) 別構活化物
,包括下列活性成分:賜諾特(spinetoram)及賜諾殺(spinosad)。(6) 氯離子通道活化劑
,包括下列活性成分:阿巴美丁(abamectin)、因滅汀苯甲酸鹽(emamectin benzoate)、里琵菌素(lepimectin),以及密滅汀(milbemectin)。(7) 保幼激素模擬物
,包括下列活性成分:烯蟲乙酯(hydroprene)、烯蟲炔酯(kinoprene)、美賜平(methoprene)、芬諾克(fenoxycarb),以及百利普芬(pyriproxyfen)。(8) 雜類非特異性( 多重位置) 抑制劑
,包括下列活性成分:溴甲烷、氯化苦(chloropicrin)、磺醯氟、硼砂、硼酸、八硼酸二鈉、硼酸鈉、偏硼酸鈉、吐酒石、重氮甲(diazomet),以及斯美地(metam)。(9) 弦音器官 (Chordotonal Organs ) 調節劑
,包括下列活性成分:派滅淨(pymetrozine)及氟尼胺(flonicamid)。(10) 蟎生長抑制劑
,包括下列活性成分:克芬蟎(clofentezine)、合賽多(hexythiazox)、氟蟎(diflovidazin),以及依殺蟎(etoxazole)。(11) 破壞昆蟲中腸膜之微生物
,包括下列活性成分:蘇力菌以色列亞種(Bacillus thuringiensis subsp. israelensis
)、蘇力菌鮎澤亞種(Bacillus thuringiensis subsp. aizawai
)、蘇力菌庫斯克亞種(Bacillus thuringiensis subsp. kurstaki
)、蘇力菌擬步行甲亞種(Bacillus thuringiensis subsp. tenebrionenis
)、Bt作物蛋白(Bt crop proteins) (Cry1Ab、Cry1Ac、Cry1Fa、Cry1A.105、Cry2Ab、Vip3A、mCry3A、Cry3Ab、Cry3Bb、Cry34Ab1/Cry35Ab1),以及球形芽孢桿菌(Bacillus sphaericus
)。(12) 粒腺體ATP 合成酶抑制劑
,包括下列活性成分:得脫蟎(tetradifon)、毆蟎多(propargite)、亞環錫(azocyclotin)、錫蟎丹(cyhexatin)、芬佈賜(fenbutatin oxide),以及汰芬隆(diafenthiuron)。(13) 經由破壞質子梯度之氧化性磷酸化非耦聯劑
,包括下列活性成分:克凡派(chlorfenapyr)、DNOC,以及氟蟲胺(sulfluramid)。(14) 菸 鹼型乙醯膽鹼受器(nAChR) 通道阻斷劑
,包括下列活性成分:免速達(bensultap)、培丹鹽酸鹽(cartap hydrochloride)、硫賜安(thiocyclam),以及殺蟲雙鈉(thiosultap–sodium)。(15) 幾丁質生合成抑制劑,第0 型
,包括下列活性成分:雙三氟蟲脲(bistrifluron)、克福隆(chlorfluazuron)、二福隆(diflubenzuron)、氟蟎脲(flucycloxuron)、氟芬隆(flufenoxuron)、六伏隆(hexaflumuron)、祿芬隆(lufenuron)、諾伐隆(novaluron)、多氟脲(noviflumuron)、得福隆(teflubenzuron),以及三福隆(triflumuron)。(16) 幾丁質生合成抑制劑,第1 型
,包括下列活性成分:布芬淨(buprofezin)。(17) 雙翅目脫皮干擾劑
,包括下列活性成分:賽滅淨(cyromazine)。(18) 蛻皮激素受器協同劑
,包括下列活性成分:可芬諾(chromafenozide)、合芬隆(halofenozide)、滅芬諾(methoxyfenozide),以及得芬諾(tebufenozide)。(19) 章魚胺受器協同劑
,包括下列活性成分:三亞蟎(amitraz)。(20) 粒腺體複合物III 電子傳遞抑制劑
,包括下列活性成分:愛美隆(hydramethylnon)、亞醌蟎(acequinocyl),以及嘧蟎酯(fluacrypyrim)。(21) 粒腺體複合物I 電子傳遞抑制劑
,包括下列活性成分:芬殺蟎(fenazaquin)、芬普蟎(fenpyroximate)、畢汰芬(pyrimidifen)、畢達本(pyridaben)、得芬瑞(tebufenpyrad)、脫芬瑞(tolfenpyrad),以及魚藤酮(rotenone)。(22) 電壓- 依賴型鈉離子通道阻斷劑
,包括下列活性成分:因得克(indoxacarb)以及美氟綜(metaflumizone)。(23) 乙醯基輔酶A 羧化酶抑制劑
,包括下列活性成分:賜派芬(spirodiclofen)、螺甲蟎酯(spiromesifen),以及螺蟲乙酯(spirotetramat)。(24) 粒腺體複合物IV 電子傳遞抑制劑
,包括下列活性成分:磷化鋁、磷化鈣、膦、磷化鋅,以及氰化物。(25) 粒腺體複合物II 電子傳遞抑制劑
,包括下列活性成分:唑蟎氰(cyenopyrafen)、賽芬蟎(cyflumetofen),及派福布敏(pyflubumide),以及(28) 羅納丹受 器 (R yanodine receptor) 調節劑
,包括下列活性成分:剋安勃(chlorantraniliprole)、氰蟲醯胺(cyantraniliprole),以及氟大滅(flubendiamide)。
這個版本的分類系統未分配第26組及第27組。此外,有包含未知的或是不確定的作用模式之活性成分UN 組
。此組包括下列活性成分:印苦楝子素(azadirachtin)、西脫蟎(benzoximate)、必芬蟎(bifenazate)、新殺蟎(bromopropylate)、蟎離丹(chinomethionat)、冰晶石(cryolite)、大克蟎(dicofol)、啶蟲丙醚(pyridalyl),以及氟蟲吡喹(pyrifluquinazon)。
術語「害蟲
」係意指一種生物體,其對人類或是人類關心的事物(譬如,作物、食物、家畜等等)是有害的,該生物體係來自於節肢動物門、軟體動物門,或圓形動物門。特定的實例為螞蟻、蚜蟲、床虱(bed bug)、甲蟲、蠹蟲(bristletails)、毛蟲、蟑螂、蟋蟀、蠼螋(earwigs)、跳蚤、蒼蠅、蚱蜢、螬、大黃蜂、小葉蟬(jassids)、葉蟬、潛葉蟲、蝨、蝗蟲、蛆、水蠟蟲(mealybugs)、蟎、蛾、線蟲(nematode)、盲蝽(plant bug)、飛蝨(planthopper)、木蝨(psyllids)、鋸蜂(sawflies)、介殼蟲、蠹魚(silverfish)、蛞蝓、蝸牛、蜘蛛、彈尾蟲、臭蟲、綜合綱(symphylans)、白蟻、薊馬(thrips)、壁蝨、胡蜂、粉虱,以及線蟲(wireworm)。
額外的實例為下列之害蟲:(1) 螯肢動物亞門(Subphyla Chelicerata) 、多足亞門(Myriapoda) ,及六足亞門(Hexapoda)
。(2) 蛛形綱 (Arachnida) 、綜合綱 (Symphyla) , 及昆蟲綱 (Insecta) 。 (3) 虱目 (Order Anoplura)
。特定屬之非窮舉性清單包括,但不限於,血虱屬(Haematopinus
spp.)、甲脅虱屬(Hoplopleura
spp.)、顎虱屬(Linognathus
spp.)、虱屬(Pediculus
spp.)、鱗虱屬(Polyplax
spp.)、牛蝨屬(Solenopotes
spp.)及新血虱屬(Neohaematopinis
spp.)。特定物種之非窮舉性清單包括,但不限於,驢血虱(Haematopinus asini
)、豬血虱(Haematopinus suis
)、毛虱(Linognathus setosus
)、綿羊顎虱(Linognathus ovillus
)、人頭蝨(Pediculus humanus capitis
)、人體虱(Pediculus humanus humanus
)及陰虱(Pthirus pubis
)。(4) 鞘翅目 (Order Coleoptera)
。特定屬之非窮舉性清單包括但不限於,豆象屬(Acanthoscelides
spp.)、叩頭蟲屬(Agriotes
spp.)、花象屬(Anthonomus
spp.)、梨象屬(Apion
spp.)、金龜屬(Apogonia
spp.)、(Araecerus
spp.)、守瓜屬(Aulacophora
spp.)、豆象蟲屬(Bruchus
spp.)、天牛屬(Cerosterna
spp.)、豆葉甲蟲屬(Cerotoma
spp.)、龜象屬(Ceutorhynchus
spp.)、跳甲屬(Chaetocnema
spp.)、肖葉甲蟲屬(Colaspis
spp.)、金針蟲屬(Ctenicera
spp.)、象鼻蟲屬(Curculio
spp.)、圓頭犀金龜屬(Cyclocephala
spp.)、葉甲屬(Diabrotica
spp.)、竹長蠹屬(Dinoderus
spp.)、榖盜屬(Gnathocerus
spp.)、竊蠹屬(Hemicoelus
spp.)、異翅長蠹屬(Heterobostruchus
spp.)、葉象屬(Hypera
spp.)、齒小蠹屬(Ips
spp.)、粉蠹屬(Lyctus
spp.)、美洲葉甲屬(Megascelis
spp.)、露尾甲屬(Meligethes
spp.)、蜘蛛甲屬(Mezium
spp.)、黃蛛甲屬(Niptus
spp.)、耳象屬屬(Otiorhynchus
spp.)、短喙象屬(Pantomorus
spp.)、鰓角金龜屬(Phyllophaga
spp.)、菜葉蚤屬(Phyllotreta
spp.)、蛛甲屬(Ptinus
spp.)、根觸金龜屬(Rhizotrogus
spp.)、虎象屬(Rhynchites
spp.)、大象鼻蟲屬(Rhynchophorus
spp.)、小蠹屬(Scolytus
spp.)、禾象鼻蟲屬(Sphenophorus
spp.)、米象屬(Sitophilus
spp.)、擬步行蟲屬(Tenebrio
spp.),以及擬穀盜屬(Tribolium
spp.)。特定物種之非窮舉性清單包括但不限於,菜豆象(Acanthoscelides obtectus
)、白蠟窄吉丁(Agrilus planipennis
)、背圓粉扁蟲(Ahasverus advena
)、外米擬步行蟲(Alphitobius diaperinus
)、光肩星天牛(Anoplophora glabripennis
)、棉鈴象蟲(Anthonomus grandis
)、小園皮蠹(Anthrenus verbasci
)、麗黃圓皮蠹(Anthrenus falvipes
)、黑絨金龜(Ataenius spretulus
)、甜菜隱食甲蟲(Atomaria linearis
)、黑毛皮蠹(Attagenus unicolor
)、甜菜象(Bothynoderes punctiventris
)、豌豆象(Bruchus pisorum
)、四紋豆象(Callosobruchus maculatus
)、黃斑露尾甲(Carpophilus hemipterus
)、甜菜龜甲(Cassida vittata
)、方頸扁甲(Cathartus quadricollis
)、豆葉甲(Cerotoma trifurcata
)、白菜籽龜象(Ceutorhynchus assimilis
)、芫菁龜象(Ceutorhynchus napi
)、梯斑叩頭蟲(Conoderus scalaris
)、多斑叩頭蟲(Conoderus stigmosus
)、李象鼻蟲(Conotrachelus nenuphar
)、綠花金龜(Cotinis nitida
)、天門冬金花蟲(Crioceris asparagi
)、鏽赤扁穀盜(Cryptolestes ferrugineus
)、長角扁穀盜(Cryptolestes pusillus
)、土耳其扁穀盜(Cryptolestes turcicus
)、密點細枝象蟲(Cylindrocopturus adspersus
)、芒果切葉象甲(Deporaus marginatus
)、火腿皮蠹(Dermestes lardarius
)、白腹皮蠹(Dermestes maculatus
)、墨西哥豆瓢蟲(Epilachna varivestis
)、盾葉蟲(Euvrilletta peltata
)、蛀莖象甲(Faustinus cubae
)、蒼白根頸象(Hylobius pales
)、家天牛(Hylotrupes bajulus
)、紫苜蓿葉象(Hypera postica
)、咖啡果小蠹(Hypothenemus hampei
)、菸草甲(Lasioderma serricorne
)、馬鈴薯甲蟲(Leptinotarsa decemlineata
)、太平洋岸線蟲(Limonius canus
)、麗金龜(Liogenys fuscus
)、條紋水象甲(Liogenys suturalis
)、水稻水象鼻蟲(Lissorhoptrus oryzophilus
)、暹羅榖盜(Lophocateres pusillus
)、平頸粉蠹(Lyctus planicollis)、Maecolaspis joliveti
、玉米叩甲(Melanotus communis
)、油菜露尾甲(Meligethes aeneus
)、大栗鰓角金龜子(Melolontha melolontha
)、赤足郭公蟲(Necrobia rufipes
)、梯頂天牛(Oberea brevis
)、線形筒天牛(Oberea linearis
)、椰子犀角金龜(Oryctes rhinoceros
)、貿易穀盜扁蟲(Oryzaephilus mercator
)、鋸穀盜(Oryzaephilus surinamensis
)、黑角負泥蟲(Oulema melanopus
)、水稻負泥蟲(Oulema oryzae
)、金龜子(Phyllophaga cuyabana
)、黑粉蠹蟲(Polycaon stoutti
)、日本麗金龜(Popillia japonica
)、大穀蠹(Prostephanus truncatus
)、穀蠹(Rhyzopertha dominica
)、條紋根瘤象甲(Sitona lineatus
)、穀象(Sitophilus granarius
)、米象(Sitophilus oryzae
)、玉米象(Sitophilus zeamais
)、藥材甲(Stegobium paniceum
)、大榖盜(Tenebroides mauritanicus
)、擬穀盜(Tribolium castaneum
)、雜擬穀盜(Tribolium confusum
)、小紅鰹節蟲(Trogoderma granarium
)、花斑皮蠹(Trogoderma variabile
)、紅毛竊蠹(Xestobium rufovillosum
),及玉米距步甲蟲(Zabrus tenebrioides
)。(5) 革翅目 (Order Dermaptera)
。特定屬之非窮舉性清單包括但不限於,普通蠼螋(Forficula auricularia
)。(6) 蜚蠊目 (Order Blattaria)
。特定物種之非窮舉性清單包括但不限於,德國姬蠊(Blattella germanica
)、亞洲姬蠊(Blattella asahina
)、東方蜚蠊(Blatta orientalis
)、櫻桃紅蟑螂(Blatta lateralis
)、賓西法尼亞木蠊(Parcoblatta pennsylvanica
)、美洲家蠊(Periplaneta americana
)、澳洲家蠊(Periplaneta australasiae
)、棕色家蠊(Periplaneta brunnea
)、黑褐家蠊(Periplaneta fuliginosa
)、蔗綠蜚蠊(Pycnoscelus surinamensis
)及長鬚帶蠊(Supella longipalpa
)。(7) 雙翅目 (Order Diptera)
。特定屬之非窮舉性清單包括但不限於,斑蚊屬(Aedes
spp.)、潛蠅屬(Agromyza
spp.)、按實蠅屬(Anastrepha
spp.)、瘧蚊屬(Anopheles
spp.)、果實蠅屬(Bactrocera
spp.)、地中海實蠅屬(Ceratitis
spp.)、斑虻屬(Chrysops
spp.)、錐蠅屬(Cochliomyia
spp.)、癭蚊屬(Contarinia
spp.)、家蚊屬(Culex
spp.)、庫蠓屬(Culicoides
spp.)、葉癭蚊屬(Dasineura
spp.)、艷粉蝶屬(Delia
spp.)、果蠅屬(Drosophila
spp.)、廁蠅屬(Fannia
spp.)、黑蠅屬(Hylemya
spp.)、斑潛蠅屬(Liriomyza
spp.)、家蠅屬(Musca
spp.)、草種蠅屬(Phorbia
spp.)、粉蠅屬(Pollenia
spp.)、蛾蚋屬(Psychoda
spp.)、蚋屬(Simulium
spp.)、虻屬(Tabanus
spp.)及大蚊屬(Tipula
spp.)。特定物種之非窮舉性清單包括但不限於,紫苜蓿潛蠅(Agromyza frontella
)、加勒比按實蠅(Anastrepha suspensa
)、墨西哥果實蠅(Anastrepha ludens
)、西印度果實蠅(Anastrepha
obliqua)、瓜實蠅(Bactrocera cucurbitae
)、東方果實蠅(Bactrocera dorsalis
)、入侵實蠅(Bactrocera invadens
)、桃實蠅(Bactrocera zonata
)、地中海實蠅(Ceratitis capitata
)、油菜葉癭蚊(Dasineura brassicae
)、灰地種蠅(Delia platura
)、黃腹廁蠅(Fannia canicularis
)、灰腹廁蠅(Fannia scalaris
)、腸胃蠅(Gasterophilus intestinalis
)、Gracillia perseae
、東方臂蠅(Haematobia irritans
)、紋皮蠅(Hypoderma lineatum
)、菜斑潛蠅(Liriomyza brassicae
)、蔬菜斑潛蠅(Liriomyza sativa
)、綿羊虱蠅(Melophagus ovinus
)、秋家蠅(Musca autumnalis
)、普通家蠅(Musca domestica
)、羊狂蠅(Oestrus ovis
)、黑麥稈蠅(Oscinella frit
)、甜菜泉蠅(Pegomya betae
)、鎧氏酪蠅(Piophila casei
)、胡蘿蔔蠅(Psila rosae
)、櫻桃果實蠅(Rhagoletis cerasi
)、蘋果果實蠅(Rhagoletis pomonella
)、藍橘繞實蠅(Rhagoletis mendax
)、麥紅吸漿蟲(Sitodiplosis mosellana
)及廄螫蠅(Stomoxys calcitrans
)。(8) 半翅目 (Order Hemiptera)
。特定屬之非窮舉性清單包括但不限於,球蚜屬(Adelges
spp.)、輪盾介殼蟲屬(Aulacaspis
spp.)、沫蟬屬(Aphrophora
spp.)、蚜蟲屬(Aphis
spp.)、粉虱屬(Bemisia
spp.)、蠟蚧屬(Ceroplastes
spp.)、雪盾介殼蟲屬(Chionaspis
spp.)、褐圓盾介殼蟲屬(Chrysomphalus
spp.)、介殼蟲屬(Coccus
spp.)、小綠葉蟬屬(Empoasca
spp.)、美洲蝽屬(Euschistus
spp.)、蠣盾介殼蟲屬(Lepidosaphes
spp.)、稻椿象屬(Lagynotomus
spp.)、草盲蝽屬(Lygus
spp.)、長管蚜屬(Macrosiphum
spp.)、黑尾葉蟬屬(Nephotettix
spp.)、稻綠蝽屬(Nezara
spp.)、褐飛蝨屬(Nilaparvata
spp.)、沫蟬屬(Philaenus
spp.)、植盲蝽屬(Phytocoris
spp.)、壁蝽屬(Piezodorus
spp.)、臀紋粉介殼蟲屬(Planococcus
spp.)、粉介殼蟲屬(Pseudococcus
spp.)、縊管蚜屬(Rhopalosiphum
spp.)、黑盔蚧屬(Saissetia
spp.)、彩斑蚜屬(Therioaphis
spp.)、蠟蚧蟲屬(Toumeyella
spp.)、桔蚜屬(Toxoptera
spp.)、粉虱屬(Trialeurodes
spp.)、錐蝽屬(Triatoma
spp.)及矢盾介殼蟲屬(Unaspis
spp.)。特定物種之非窮舉性清單包括但不限於,擬綠蝽(Acrosternum hilare
)、豌豆蚜(Acyrthosiphon pisum
)、甘藍粉虱(Aleyrodes proletella
)、螺旋粉虱(Aleurodicus dispersus
)、絲絨粉虱(Aleurothrixus floccosus
)、二點小綠葉蟬(Amrasca biguttula biguttula
)、紅圓蚧(Aonidiella aurantii
)、蠶豆蚜(Aphis fabae
)、棉蚜(Aphis gossypii
)、大豆蚜(Aphis glycines
)、蘋果蚜(Aphis pomi
)、馬鈴薯蚜(Aulacorthum solani
)、馬鈴薯/番茄木虱(Bactericera cockerelli
)、菘蝽荷疇(Bagrada hilaris
)、銀葉粉虱(Bemisia argentifolii
)、煙草粉虱(Bemisia tabaci
)、麥長蝽(Blissus leucopterus
)、梣葉槭蝽(Boisea trivittata
)、天門冬小管蚜(Brachycorynella asparagi
)、稻粉介殼蟲(Brevennia rehi
)、甘藍蚜(Brevicoryne brassicae
)、梨木蝨(Cacopsylla pyri
)、梨黃木蝨(Cacopsylla pyricola
)、馬鈴薯俊盲蝽(Calocoris norvegicus
)、紅蠟介殼蟲(Ceroplastes rubens
)、熱帶臭蟲(Cimex hemipterus
)、溫帶臭蟲(Cimex lectularius
)、桔軟蠟介殼蟲(Coccus pseudomagnoliarum
)、Dagbertus fasciatus
、Dichelops furcatus
、麥雙尾蚜(Diuraphis noxia
)、柑橘木虱(Diaphorina citri
)、車前圓尾蚜(Dysaphis plantaginea
)、棉黑翅紅蝽(Dysdercus suturellus
)、Edessa meditabunda
、假眼小綠葉蟬(Empoasca vitis
)、蘋果綿蚜(Eriosoma lanigerum
)、西方葡萄葉蟬(Erythroneura elegantula
)、歐扁盾蝽(Eurygaster maura
)、美洲蝽(Euschistus conspersus
)、英雄美洲蝽(Euschistus heros
)、褐美洲蝽(Euschistus servus
)、褐翅蝽(Halyomorpha halys
)、安氏角盲蝽(Helopeltis antonii
)、桃粉蚜(Hyalopterus pruni
)、安氏角盲蝽(Helopeltis antonii
)、茶角盲蝽(Helopeltis theivora
)、吹棉介殼蟲(Icerya purchasi
)、檬果褐葉蟬(Idioscopus nitidulus
)、小綠葉蟬(Jacobiasca formosana
)、斑飛虱(Laodelphax striatellus
)、東方球蠟蚧(Lecanium corni
)、大稻緣蝽(Leptocorisa oratorius
)、稻緣椿象(Leptocorisa varicornis
)、豆莢草盲蝽(Lygus hesperus
)、桑粉介殼蟲(Maconellicoccus hirsutus
)、大戟長管蚜(Macrosiphum euphorbiae
)、麥長管蚜(Macrosiphum granarium
)、薔薇長管蚜(Macrosiphum rosae
)、翠菊葉蟬(Macrosteles quadrilineatus
)、沫蟬(Mahanarva frimbiolata
)、豆龜蝽(Megacopta cribraria
)、麥無網蚜(Metopolophium dirhodum
)、長角蝽象(Mictis longicornis
)、桃蚜(Myzus persicae
)、萵苣蚜蟲(Nasonovia ribisnigri
)、偽黑尾葉蟬(Nephotettix cincticeps
)、Neurocolpus longirostris
、稻綠蝽(Nezara viridula
)、褐飛蝨(Nilaparvata lugens
)、木瓜秀粉介殼蟲(Paracoccus marginatus
)、馬鈴薯/番茄木虱(Paratrioza cockerelli
)、糠片盾蚧(Parlatoria pergandii
)、黑片盾介殼蟲(Parlatoria ziziphi
)、玉米花翅飛虱(Peregrinus maidis
)、葡萄根瘤蚜(Phylloxera vitifoliae
)、去杉球蚧(Physokermes piceae
)、加州盲蝽(Phytocoris californicus
)、植盲蝽(Phytocoris relativus
)、蓋德擬壁蝽(Piezodorus guildinii
)、桔臀紋粉介殼蟲(Planococcus citri
)、無花果臀紋粉介殼蟲(Planococcus ficus
)、四線盲蝽(Poecilocapsus lineatus
)、盲蝽(Psallus vaccinicola
)、酪梨椿象(Pseudacysta perseae
)、菠蘿潔粉介殼蟲(Pseudococcus brevipes
)、梨園盾蚧(Quadraspidiotus perniciosus
)、玉米蚜(Rhopalosiphum maidis
)、稻麥蚜(Rhopalosiphum padi
)、欖珠蠟蚧(Saissetia oleae
)、栗花椿象(Scaptocoris castanea
)、麥二叉蚜(Schizaphis graminum
)、麥長管蚜(Sitobion avenae
)、白背飛虱(Sogatella furcifera
)、溫室粉虱(Trialeurodes vaporariorum
)、結翅粉蝨(Trialeurodes abutiloneus
)、箭頭介殼蟲(Unaspis yanonensis
)以及Zulia entrerriana
。(9) 膜翅目 (Order Hymenoptera)
。特定屬之非窮舉性清單包括但不限於,切葉蟻屬(Acromyrmex
spp.)、葉蟻屬(Atta
spp.)、巨山蟻屬(Camponotus
spp.)、松葉蜂屬(Diprion
spp.)、黃胡蜂屬(Dolichovespula
spp.)、蟻屬(Formica
spp.)、單家蟻屬(Monomorium
spp.)、新松葉蜂屬(Neodiprion
spp.)、黃山蟻屬(Paratrechina
spp.)、大頭家蟻屬(Pheidole
spp.)、收穫蟻屬(Pogonomyrmex
spp.)、馬蜂屬(Polistes
spp.)、紅火蟻屬(Solenopsis
spp.)、扁琉璃蟻屬(Technomyrmex
, spp.)、皺家蟻屬(Tetramorium
spp.)、黃胡蜂屬(Vespula
spp.)、胡蜂屬(Vespa
spp.),及絨木蜂屬(Xylocopa
spp.)。特定物種之非窮舉性清單包括但不限於,紅角菜葉蜂(Athalia rosae
)、德克塞斯切葉蟻(Atta texana
)、櫻桃粘葉蜂(Caliroa cerasi
)、美洲榆錘角葉蜂(Cimbex americana
)、阿根廷虹琉璃蟻(Iridomyrmex humilis
)、阿根廷蟻(Linepithema humile
)、歐洲黑蜂(Mellifera Scutellata
)、小黑蟻(Monomorium minimum
)、小黃單家蟻(Monomorium pharaonis
)、松黃葉蜂(Neodiprion sertifer
)、入侵紅火蟻(Solenopsis invicta
)、熱帶火蟻(Solenopsis geminata
)、偷竊蟻(Solenopsis molesta
)、黑火蟻(Solenopsis richtery
)、南方火蟻(Solenopsis xyloni
)、酸臭家蟻(Tapinoma sessile
),及小火蟻(Wasmannia auropunctata
)。(10) 等翅目 (Order Isoptera)
。特定屬之非窮舉性清單包括但不限於,乳白蟻屬(Coptotermes
spp.)、角象白蟻屬(Cornitermes
spp.)、堆砂白蟻屬(Cryptotermes
spp.)、異白蟻屬(Heterotermes
spp.)、木白蟻屬(Kalotermes
spp.)、楹白蟻屬(Incisitermes
spp.)、大白蟻屬(Macrotermes
spp.)、緣木白蟻屬(Marginitermes
spp.)、鋸白蟻屬(Microcerotermes
spp.)、原角白蟻屬(Procornitermes
spp.)、散白蟻屬(Reticulitermes
spp.)、長鼻白蟻屬(Schedorhinotermes
spp.)及古白蟻屬(Zootermopsis
spp.)。特定物種之非窮舉性清單包括但不限於,(Coptotermes acinaciformis
)、曲顎乳白蟻(Coptotermes curvignathus
)、法國乳白蟻(Coptotermes frenchii
)、臺灣乳白蟻(Coptotermes formosanus
)、格斯特乳白蟻(Coptotermes gestroi
)、麻頭堆砂白蟻(Cryptotermes brevis
)、金黃異白蟻(Heterotermes aureus
)、南美異白蟻(Heterotermes tenuis
)、小楹白蟻(Incisitermes minor
)、斯氏楹白蟻(Incisitermes snyderi
)、稻麥小白蟻(Microtermes obesi
)、角象白蟻(Nasutitermes corniger
)、臺灣土白蟻(Odontotermes formosanus
)、土白蟻(Odontotermes obesus
)、班努斯散白蟻(Reticulitermes banyulensis
)、草地散白蟻(Reticulitermes grassei
)、黃肢散白蟻(Reticulitermes flavipes
)、哈氏散白蟻(Reticulitermes hageni
)、西方散白蟻(Reticulitermes hesperus
)、桑特散白蟻(Reticulitermes santonensis
)、黃胸散白蟻(Reticulitermes speratus
)、美黑脛散白蟻(Reticulitermes tibialis
)及美小黑散白蟻(Reticulitermes virginicus
)。(11) 鱗翅目 (Order Lepidoptera)
。特定屬之非窮舉性清單包括但不限於,捲葉蛾屬(Adoxophyes
spp.)、地老虎屬(Agrotis
spp.)、帶卷蛾屬(Argyrotaenia
spp.)、卷葉蛾屬(Cacoecia
spp.)、麗細蛾屬(Caloptilia
spp.)、水稻螟蟲屬(Chilo
spp.)、錁紋夜蛾屬(Chrysodeixis
spp.)、豆粉蝶屬(Colias
spp.)、草螟屬(Crambus
spp.)、絹野螟屬(Diaphania
spp.)、螟屬(Diatraea
spp.)、鑽夜蛾屬(Earias
spp.)、粉斑螟屬(Ephestia
spp.)、尺蠖蛾屬(Epimecis
spp.)、斑點夜蛾屬(Feltia
spp.)、角劍夜蛾屬(Gortyna
spp.)、鈴夜蛾屬(Helicoverpa
spp.)、實夜蛾屬(Heliothis
spp.)、根蠹屬(Indarbela spp.
)、潛夜細蛾屬(Lithocolletis
spp.)、切根蟲屬(Loxagrotis
spp.)、天幕毛蟲屬(Malacosoma
spp.)、谷蛾屬(Nemapogon
spp.)、疆夜蛾屬(Peridroma
spp.)、小潛細蛾屬(Phyllonorycter
spp.)、黏夜蛾屬(Pseudaletia
spp.)、菜蛾屬(Plutella
spp.)、蛀莖夜蛾屬(Sesamia
spp.)、夜盗蛾屬(Spodoptera
spp.)、透翅蛾屬(Synanthedon
spp.)及巢蛾屬(Yponomeuta
spp.)。特定物種之非窮舉性清單包括但不限於,飛揚阿夜蛾(Achaea janata
)、棉褐帶卷蛾(Adoxophyes orana
)、小地老虎(Agrotis ipsilon
)、棉葉波紋夜蛾(Alabama argillacea
)、鱷梨卷葉蟲(Amorbia cuneana
)、臍橙螟(Amyelois transitella
)、棕灰蛾(Anacamptodes defectaria
)、桃枒蛾(Anarsia lineatella
)、黃麻夜蛾(Anomis sabulifera
)、梨豆夜蛾(Anticarsia gemmatalis
)、果樹黃捲蛾(Archips argyrospila
)、玫瑰黃捲蛾(Archips rosana
)、桔帶卷蛾(Argyrotaenia citrana
)、伽馬紋夜蛾(Autographa gamma
)、捲葉蛾(Bonagota cranaodes
)、禾弄蝶(Borbo cinnara
)、棉潛蛾(Bucculatrix thurberiella
)、菸卷蛾(Capua reticulana
)、桃蛀果蛾(Carposina niponensis
)、芒果螟蛾(Chlumetia transversa
)、玫瑰色卷蛾(Choristoneura rosaceana
)、稻縱卷葉螟(Cnaphalocrocis medinalis
)、可可細蛾(Conopomorpha cramerella
)、外米綴蛾(Corcyra cephalonica
)、芳香木蠹蛾(Cossus cossus
)、石核桃卷蛾(Cydia caryana
)、李小食心蟲(Cydia funebrana
)、梨小食心蟲(Cydia molesta
)、豌豆小卷蛾(Cydia nigricana
)、蘋果蠹蛾(Cydia pomonella
)、茶刺蛾(Darna diducta
)、黄瓜絹野螟(Diaphania nitidalis
)、小蔗桿草螟(Diatraea saccharalis
)、西南玉米桿草螟(Diatraea graniosella
)、埃及鑽夜蛾(Earias insulata
)、翠紋鑽夜蛾(Earias vitella
)、對小卷蛾(Ecdytolopha aurantianum
)、南美玉米苗斑螟(Elasmopalpus lignosellus
)、粉斑螟(Ephestia cautella
)、菸草粉斑螟(Ephestia elutella
)、地中海粉螟(Ephestia kuehniella
)、大豆捲葉蛾(Epinotia aporema
)、淡棕蘋果蛾(Epiphyas postvittana
)、香蕉弄蝶(Erionota thrax
)、鹽澤燈蛾(Estigmene acrea
)、女貞細卷蛾(Eupoecilia ambiguella
)、原切根蟲(Euxoa auxiliaris
)、蠟螟(Galleria mellonella
)、桃折心蟲(Grapholita molesta
)、三紋螟蛾(Hedylepta indicata
)、棉鈴蟲(Helicoverpa armigera
)、玉米穗蟲(Helicoverpa zea
)、菸芽夜蛾(Heliothis virescens
)、菜心野螟(Hellula undalis
)、番茄蠹蛾(Keiferia lycopersicella
)、茄螟蛾(Leucinodes orbonalis
)、咖啡潛葉蛾(Leucoptera coffeella
)、旋紋潛蛾(Leucoptera malifoliella
)、葡萄花翅小卷蛾(Lobesia botrana
)、豆白緣切根蟲(Loxagrotis albicosta
)、舞毒蛾(Lymantria dispar
)、桃潛葉蛾(Lyonetia clerkella
)、蓑蛾(Mahasena corbetti
)、甘藍夜蛾(Mamestra brassicae
)、烟草天蛾(Manduca sexta
)、豆莢螟(Maruca testulalis
)、袋蛾(Metisa plana
)、栗夜盜蟲(Mythimna unipuncta
)、番茄蛀蟲(Neoleucinodes elegantalis
)、白水螟蛾(Nymphula depunctalis
)、冬尺蠖蛾(Operophtera brumata
)、歐洲玉米螟(Ostrinia nubilalis
)、大戟草尺蠖蛾(Oxydia vesulia)
、疆褐卷蛾(Pandemis cerasana
)、蘋褐卷蛾(Pandemis heparana
)、非洲達摩鳳蝶(Papilio demodocus
)、白咖啡潛夜蟲(Pectinophora gossypiella
)、雜色夜蛾(Peridroma saucia
)、咖啡潛葉蛾(Perileucoptera coffeella
)、馬鈴薯蠹蛾(Phthorimaea operculella
)、柑橘潛夜蛾(Phyllocnisitis citrella
)、斑幕潛葉蛾(Phyllonorycter blancardella
)、紋白蝶(Pieris rapae
)、苜蓿綠夜蛾(Plathypena scabra
)、蘋果芽小卷蛾(Platynota idaeusalis
)、印度穀螟蛾(Plodia interpunctella
)、小菜蛾(Plutella xylostella
)、葡萄捲葉蛾(Polychrosis viteana
)、桔果巢蛾(Prays endocarpa
)、油橄欖巢蛾(Prays oleae
)、一星黏蟲(Pseudaletia unipuncta
)、大豆夜蛾(Pseudoplusia includens
)、向日葵尺蠖(Rachiplusia nu
)、三化螟(Scirpophaga incertulas
)、稻蛀莖夜蛾(Sesamia inferens
)、西非蛀莖夜蛾(Sesamia nonagrioides
)、蕁麻毛蟲(Setora nitens
)、麥蛾(Sitotroga cerealella
)、葡萄長鬚卷葉蛾(Sparganothis pilleriana
)、甜菜夜蛾(Spodoptera exigua
)、草地貪夜蛾(Spodoptera fugiperda
)、南部灰翅夜蛾(Spodoptera eridania
)、菠蘿褐灰蝶(Thecla basilides
)、衣蛾(Tinea pellionella
)、袋衣蛾(Tineola bisselliella
)、粉斑夜蛾(Trichoplusia ni
)、番茄斑潛蠅(Tuta absoluta
)、咖啡豹蠹蛾(Zeuzera coffeae
)以及梨豹蠹蛾(Zeuzera pyrina
)。(12) 食毛目 (Order Mallophaga)
。特定屬之非窮舉性清單包括但不限於,細鵝虱屬(Anaticola
spp.)、牛毛虱屬(Bovicola
spp.)、大火雞虱屬(Chelopistes
spp.)、雞角羽虱(Goniodes
spp.)、雞虱屬(Menacanthus
spp.)及犬毛虱屬(Trichodectes
spp.)。特定物種之非窮舉性清單包括但不限於,牛羽虱(Bovicola bovis
)、山羊住牛虱(Bovicola caprae
)、綿羊虱(Bovicola ovis
)、大火雞虱(Chelopistes meleagridis
)、雞角羽虱(Goniodes dissimilis
)、大角羽虱(Goniodes gigas
)、雛雞羽蝨(Menacanthus stramineus
)、雞羽虱(Menopon gallinea
)以及犬嚙毛虱(Trichodectes canis
)。(13) 直翅目 (Order Orthoptera)
。特定屬之非窮舉性清單包括但不限於,黑蝗屬(Melanoplus
spp.)及側羽葉屬(Pterophylla
spp.)。特定物種之非窮舉性清單包括但不限於,家蟋蟀(Acheta domesticus
)、摩門螽斯(Anabrus simplex
)、非洲螻蛄(Gryllotalpa africana
)、南方螻蛄(Gryllotalpa australis
)、黑短螻蛄(Gryllotalpa brachyptera
)、歐洲痣蟋蟀(Gryllotalpa hexadactyla
)、東亞飛蝗(Locusta migratoria
)、角翅螽斯(Microcentrum retinerve
)、沙漠蝗(Schistocerca gregaria
),以及叉尾灌叢樹螽(Scudderia furcata
)。(14) 囓蟲目 ( Order Psocoptera )
。特定物種之非窮舉性清單包括但不限於,無色書蝨(Liposcelis decolor
)、囓蟲書蝨(Liposcelis entomophila
)、姬嚙蟲(Lachesilla quercus
),以及粉茶蛀蟲(Trogium pulsatorium
)。(15) 蚤目 (Order Siphonaptera)
。特定物種之非窮舉性清單包括但不限於,雞角葉蚤(Ceratophyllus gallinae
)、黑角葉蚤(Ceratophyllus niger
)、犬櫛頭蚤(Ctenocephalides canis
)、貓櫛頭蚤(Ctenocephalides felis
),以及人蚤(Pulex irritans
)。(16) 纓翅目 (Order Thysanoptera)
。特定屬之非窮舉性清單包括但不限於,巢針薊馬屬(Caliothrips
spp.)、花薊馬屬(Frankliniella
spp.)、跳薊馬屬(Scirtothrips
spp.)及薊馬屬(Thrips
spp.)。特定物種之非窮舉性清單包括但不限於,巢針薊馬(Caliothrips phaseoli
)、菱花薊馬(Frankliniella bispinosa
)、菸褐花薊馬(Frankliniella fusca
)、西方花薊馬(Frankliniella occidentalis
)、梳缺花薊馬(Frankliniella schultzei
)、檬果花薊馬(Frankliniella tritici
)、威廉斯花薊馬(Frankliniella williamsi
)、變葉木薊馬(Heliothrips haemorrhaidalis
)、腹鉤薊馬(Rhipiphorothrips cruentatus
)、桔硬薊馬(Scirtothrips citri
)、小黃薊馬(Scirtothrips dorsalis
)、帶薊馬(Taeniothrips rhopalantennalis
)、黃胸薊馬(Thrips hawaiiensis
)、豆黃薊馬(Thrips nigropilosus
)、東方薊馬(Thrips orientalis
)、南黃薊馬(Thrips palmi
),以及菸薊馬(Thrips tabaci
)。(17) 纓尾目 (Order Thysanura)
。特定屬之非窮舉性清單包括但不限於,衣魚屬(Lepisma
spp.)以及小灶衣魚屬(Thermobia
spp.)。(18) 蜱蟎目 (Order Acarina)
。特定屬之非窮舉性清單包括但不限於,粉蟎屬(Acarus
spp.)、刺皮節蜱屬(Aculops
spp.)、Argus
屬(Argus
spp.)、牛蜱蝨屬(Boophilus
spp.)、蠕形蟎屬(Demodex
spp.)、革蜱屬(Dermacentor
spp.)、上癭蟎屬(Epitimerus
spp.)、節蜱屬(Eriophyes
spp.)、硬蜱屬(Ixodes
spp.)、赤葉蟎屬(Oligonychus
spp.)、全爪蟎屬(Panonychus
spp.)、扇頭蜱屬(Rhizoglyphus
spp.)及葉蟎屬(Tetranychus
spp.)。特定物種之非窮舉性清單包括但不限於,伍德氏蟎(Acarapis woodi
)、粗腳粉蟎(Acarus siro
)、芒果瘤癭蟎(Aceria mangiferae
)、番茄刺皮癭蟎(Aculops lycopersici
)、皮氏刺皮癭蟎(Aculus pelekassi
)、斯氏刺癭蟎(Aculus schlechtendali
)、美洲鈍眼蜱(Amblyomma americanum
)、卵形短鬚蟎(Brevipalpus obovatus
)、紫紅短鬚蟎(Brevipalpus phoenicis
)、變異革蜱(Dermacentor variabilis
)、歐洲室塵蟎(Dermatophagoides pteronyssinus
)、鵝耳櫪始葉蟎(Eotetranychus carpini
)、異脂刺蟎(Liponyssoides sanguineus
)、貓節痂蟎(Notoedres cati
)、茶紅葉蟎(Oligonychus coffe a e
)、伊氏赤葉蟎(Oligonychus ilicis
)、柏氏禽刺蟎(Ornithonyssus bacoti
)、柑橘葉蟎(Panonychus citri
)、歐洲葉蟎(Panonychus ulmi
)、柑桔皺葉刺節蜱(Phyllocoptruta oleivora
)、側多食跗線蟎(Polyphagotarsonemun latus
)、血紅扇頭蜱(Rhipicephalus sanguineus
)、人疥蟎(Sarcoptes scabiei
)、鱷梨頂冠癭蟎(Tegolophus perseaflorae
)、二點葉蟎(Tetranychus urticae
)、長食酪蟎(Tyrophagus longior
),以及狄氏瓦蟎(Varroa destructor
)。(19) 真蜘蛛目 (Order Araneae )
。特定屬之非窮舉性清單包括但不限於,斜蛛屬(Loxosceles
spp.
)、寡婦蛛屬(Latrodectus
spp.
),以及漏斗蜘蛛屬(Atrax
spp.
)。特定物種之非窮舉性清單包括但不限於,棕色遁蛛(Loxosceles reclusa
)、黑寡婦蜘蛛(Latrodectus mactans
),以及雪梨漏斗網蜘蛛(Atrax robustus)
。(20) 結閥綱 (Class Symphyla ) 。
特定物種之非窮舉性清單包括但不限於,白松蟲(Scutigerella immaculata
)。(21) 粘管亞綱 (Subclass Collembola ) 。
特定物種之非窮舉性清單包括但不限於,黄星圓跳蟲(Bourletiella hortensis
)、棘跳蟲(Onychiurus armatus
)、跳蟲(Onychiurus fimetarius
),以及綠圓跳蟲(Sminthurus viridis
)。(22) 圓形動物門 (Phylum Nematoda)
。特定屬之非窮舉性清單包括但不限於,線蟲屬(Aphelenchoides
spp.)、刺線蟲屬(Belonolaimus
spp.)、小環線蟲屬(Criconemella
spp.)、莖線蟲屬(Ditylenchus
spp.)、黃金線蟲屬(Globodera
spp.)、孢囊線蟲屬(Heterodera
spp.)、潛根線蟲屬(Hirschmanniella
spp.)、紐帶線蟲屬(Hoplolaimus
spp.)、根瘤線蟲屬(Meloidogyne
spp.)、根腐線蟲屬(Pratylenchus
spp.)及穿孔線蟲屬(Radopholus
spp.)。特定物種之非窮舉性清單包括但不限於,犬惡絲蟲(Dirofilaria immitis
)、馬鈴薯孢囊線蟲(Globodera pallida
)、大豆孢囊線蟲(Heterodera glycines
)、玉米胞囊線蟲(Heterodera zeae
)、南方根結線蟲(Meloidogyne incognita
)、爪哇根瘤線蟲(Meloidogyne javanica
)、人蟠尾絲蟲(Onchocerca volvulus
)、穿刺短體根腐線蟲(Pratylenchus penetrans
)、相似穿孔線蟲(Radopholus similis
)以及腎狀線蟲(Rotylenchus reniformis
)。(23) 軟體動物門 ( Phylum Mollusca )
。特定物種之非窮舉性清單包括但不限於,西班牙蛞蝓(Arion vulgaris
)、螺旋蝸牛(Cornu aspersum
)、網紋野蛞蝓(Deroceras reticulatum
)、黄蛞蝓(Limax flavus
)、黑色小蛞蝓(Milax gagates
),以及福壽螺(Pomacea canaliculata
)。
特別佳要控制的害蟲群組是取食汁液之害蟲。取食汁液之害蟲
,一般說來,具有銳利及/或吸吮的口器,並且取食汁液與植物之內部植物組織。農業特別關注的取食汁液之害蟲的實例含括但不限於,蚜蟲、葉蟬、蛾、介殼蟲(scales)、薊馬(thrips)、木蝨(psyllids)、水蠟蟲(mealybugs)、臭蟲,以及粉虱。農業關注的取食汁液之害蟲的特定目實例含括但不限於,虱目(Order Anoplura)及半翅目(Order Hemiptera)。農業關注的半翅目特定實例含括但不限於,輪盾介殼蟲屬(Aulacaspis
spp.)、沫蟬屬(Aphrophora
spp.)、蚜蟲屬(Aphis
spp.)、粉虱屬(Bemisia
spp.)、介殼蟲屬(Coccus
spp.)、美洲蝽屬(Euschistus
spp.)、草盲蝽屬(Lygus
spp.)、長管蚜屬(Macrosiphum
spp.)、稻綠蝽屬(Nezara
spp.),以及縊管蚜屬(Rhopalosiphum
spp.)。
另一特別佳要控制的害蟲群組是嚼食性害蟲。嚼食性害蟲
,一般說來,具有銳利及/或吸吮的口器使其等能嚼食植物組織,含括根、莖、葉及生殖組織(含括但不限於,花、果實及種子)。農業關注的嚼食性害蟲的實例含括但不限於,毛蟲、甲蟲、蚱蜢及蝗蟲。農業關注的嚼食性害蟲的特定目實例含括但不限於,鞘翅目(Coleoptera)及鱗翅目(Lepidoptera)。農業關注的鞘翅目之特定實例含括但不限於,豆象屬(Acanthoscelides
spp.)、豆葉甲蟲屬(Cerotoma
spp.)、跳甲屬(Chaetocnema
spp.)、肖葉甲蟲屬(Colaspis
spp.)、圓頭犀金龜屬(Cyclocephala
spp.)、葉甲屬(Diabrotica
spp.)、葉象屬(Hypera
spp.)、鰓角金龜屬(Phyllophaga
spp.)、菜葉蚤屬(Phyllotreta
spp.)、禾象鼻蟲屬(Sphenophorus
spp.)、米象屬(Sitophilus
spp.)。
用語「殺蟲 有效量
」意指對害蟲達成可觀察到的效應所需要的殺蟲劑量,舉例而言壞死、死亡、遲緩、預防、移除、破壞的效應,不然就是能減少害蟲於一所在地的發生及/或害蟲的活性。於一所在地驅逐害蟲族群,害蟲於一所在地或附近無行為能力,以及/或是害蟲於一所在地或附近消滅的時候,可產生此效應。當然,可發生此等效應之組合。一般而言,害蟲族群、活性或是二者都希望降低超過百分之五十,較佳為超過百分之九十,且最佳為超過百分之九十九。通常,對於農業目的,殺蟲有效量為從大約每公頃0.0001公克至大約每公頃5000公克,較佳為從大約每公頃0.0001公克至大約每公頃500公克,以及還更佳為從大約每公頃0.0001公克至大約每公頃50 公克。
較佳實施例之詳細說明 本文件揭示式 1
分子 式1
其中:(A) Ar1
係選自於下列所構成的群組:呋喃基、苯基、嗒基、吡啶基、嘧啶基,或是噻吩基, 其中每個呋喃基、苯基、嗒基、吡啶基、嘧啶基,及噻吩基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基;(B) Het
為5或6員、飽和或不飽和之雜環,含有獨立地選自於氮、硫或氧之一或多個雜原子,以及其中Ar1
與L1
互相不為鄰位,但可為間位或對位,例如就五員環而言,其等為1,3,且就六員環而言,其等為1,3或1,4, 其中每個雜環可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、側氧、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基;(C) L1
係選自於下列所構成的群組:N(Rx
)-(C1
-C4
)烷基、N(Rx
)-(C3
-C8
)環烷基、N(Rx
)-(C2
-C6
)烯基、N(Rx
)-(C2
-C6
)炔基、N(Rx
)-S(O)n
-(C1
-C4
)烷基、(C1
-C4
)烷基-N(Rx
)-(C1
-C4
)烷基、(C1
-C4
)烷基-N(Rx
)-(C1
-C4
)烷基、(C1
-C4
)烷基-N(Rx
)、(C3
-C8
)環烷基-N(Rx
)、(C2
-C6
)炔基-N(Rx
)、(C1
-C4
)烷基-S(O)n
-N(Rx
)、C(O)-N(Rx
)、C(S)-N(Rx
)、N(Rx
)-C(O)、N(Rx
)-C(S)、C(O)-N(Rx
)-(C1
-C4
)烷基、C(S)-N(Rx
)-(C1
-C4
)烷基、(C1
-C4
)烷基-N(Rx
)-C(O),以及(C1
-C4
)烷基-N(Rx
)-C(S), 其中每個烷基、環烷基、烯基及炔基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基,以及(C2
-C6
)炔基;(D) Ar2
係選自於下列所構成的群組:呋喃基、苯基、嗒基、吡啶基、嘧啶基,或是噻吩基, 其中每個呋喃基、苯基、嗒基、吡啶基、嘧啶基,及噻吩基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(=O)O-(C1
-C4
)烷基、苯基,以及苯氧基;(E) R15
係選自於下列所構成的群組:H、(C1
-C4
)烷基、(C3
-C8
)環烷基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、C(O)-NRx
Ry
、C(O)-苯基、(C1
-C4
)烷基-NRx
Ry
、C(O)O-(C1
-C4
)烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基,(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基, 其中每個烷基、環烷基、烯基、炔基,及苯基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、側氧、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基;(F) Q1
係選自於O及S所構成的群組;(G)Q2
係選自於O及S所構成的群組;(H) R16
係選自於下列所構成的群組:(K)
、H、(C1
-C4
)烷基、(C3
-C8
)環烷基、(C2
-C6
)烯基、(C2
-C6
)炔基、C(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、(C1
-C4
)烷基苯基、(C1
-C4
)烷基-O-苯基、C(O)-(Het-1)、(Het-1)、(C1
-C4
)烷基-(Het-1)、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-NRx
Ry
、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-(Het-1)、(C1
-C4
)烷基-C(O)-(Het-1)、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基(NRx
Ry
)-C(O)OH、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-NRx
Ry
、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-N(Rx
)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基(N(Rx
)-C(O)O-(C1
-C4
)烷基)-C(O)OH、(C1
-C4
)烷基-C(O)-(Het-1)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C3
-C8
)環烷基、(C1
-C4
)烷基-OC(O)-(Het-1)、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基-N(Rx
)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-NRx
Ry
、(C1
-C4
)烷基-S(O)n
-(Het-1),以及(C1
-C4
)烷基-O-(Het-1), 其中每個烷基、環烷基、烯基、炔基、苯基,及(Het-1)可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)OH、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基)、苯基、苯氧基、Si((C1
-C4
)烷基)3
、S(O)n
-NRx
Ry
,以及(Het-1);(I) R17
係選自於下列所構成的群組:(K)
、H、(C1
-C4
)烷基、(C3
-C8
)環烷基、(C2
-C6
)烯基、(C2
-C6
)炔基、C(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、(C1
-C4
)烷基苯基、(C1
-C4
)烷基-O-苯基、C(O)-(Het-1)、(Het-1)、(C1
-C4
)烷基-(Het-1)、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-NRx
Ry
、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-(Het-1)、(C1
-C4
)烷基-C(O)-(Het-1)、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基(NRx
Ry
)-C(O)OH、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-NRx
Ry
、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-N(Rx
)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基(N(Rx
)-C(O)O-(C1
-C4
)烷基)-C(O)OH、(C1
-C4
)烷基-C(O)-(Het-1)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C3
-C8
)環烷基、(C1
-C4
)烷基-OC(O)-(Het-1)、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基-N(Rx
)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-NRx
Ry
、(C1
-C4
)烷基-S(O)n
-(Het-1),以及(C1
-C4
)烷基-O-(Het-1), 其中每個烷基、環烷基、烯基、炔基、苯基,及(Het-1)可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)OH、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基、苯氧基、Si((C1
-C4
)烷基)3
、S(O)n
-NRx
Ry
,以及(Het-1);(J) L2
係選自於下列所構成的群組:(C3
-C8
)環烷基、苯基、(C1
-C4
)烷基苯基、(C1
-C4
)烷基-O-苯基、(C2
-C6
)烯基-O-苯基、(Het-1)、(C1
-C4
)烷基-(Het-1),以及(C1
-C4
)烷基-O-(Het-1), 其中每個烷基、環烷基、烯基、苯基,及(Het-1)可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C1
-C4
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、O-(C1
-C4
)烷基、S-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基、苯氧基,以及(Het-1), 其中每個烷基、環烷基、烯基、苯基,及(Het-1)取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C1
-C4
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、O-(C1
-C4
)烷基、S-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基、苯氧基,以及(Het-1);(K) R16
及R17
與Cx
(Q2
)(Nx
)
一起形成一個4-至7-員飽和或不飽和之雜環,其可以進一步含有選自於氮、硫或氧所構成的群組之一個或更多個雜原子, 其中每個雜環可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:側氧、R18
及R19
, 其中R18
及R19
係各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2
、側氧、硫酮基、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及(Het-1);(L) Rx
及Ry
係各自獨立地選自於下列所構成的群組:H、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基,以及苯基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基,及苯基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及(Het-1);(M) (Het-1)
為5或6員、飽和或不飽和之雜環,含有獨立地選自於氮、硫或氧所構成的群組之一或多個雜原子, 其中每個雜環可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、側氧、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基;(N) n
每一者係獨立地為0、1或2;以及 式1的分子之N-氧化物、農業上可接受的酸加成鹽類、鹽類衍生物、溶劑合物、結晶性多形體、同位素、解析的立體異構物,以及互變異構物。
式1分子可以以不同的幾何或光學異構物或是不同的互變異構物形式存在。可以存在一個或更多個掌性中心,在這種情況下,式1分子可以存在為純的鏡相異構物、鏡相異構物混合物、純的非鏡相異構物或是非鏡相異構物混合物。熟習此項技術者將瞭解,一種立體異構物可比其他立體異構物更具活性。個別立體異構物可藉由已知的選擇性合成程序獲得、使用經解析之起始物質藉由習知合成程序獲得,或是藉由習知解析程序來獲得。該分子內可能存在雙鍵,在這種情況下,式1分子可以存在為單一的幾何異構物(順式或反式,E
或Z
),或是幾何異構物(順式及反式,E
及Z
)之混合物。可以存在互變異構中心。本揭示涵蓋所有此等異構物、互變異構物,以及其等所有比例之混合物。本揭示中繪出的結構僅用於清楚說明幾何形式,不應理解為代表該分子之所有幾何形式。
在另一個具體例中,Ar1
為(1a) (1a)
, 其中:(1) R1
、R2
、R4
及R5
各自獨立地為H;以及(2) R3
為(C1
-C4
)鹵烷氧基。
本具體例可與Het 、L1 、Ar2 、R15 、Q1 、Q2 、R16 、R17
,及L2
之其他具體例組合使用。
在另一個具體例中,Ar1
為(1a)
,其中R3
為OCF3
。本具體例可與R1 、R2 、R4 、R5 、Het 、L1 、Ar2 、R15 、Q1 、Q2 、R16 、R17
,及L2
之其他具體例組合使用。
在另一個具體例中,Het
為(1b) (1b)
, 其中R6
為H。本具體例可與Ar1 、L1 、Ar2 、R15 、Q1 、Q2 、R16 、R17
,及L2
之其他具體例組合使用。
在另一個具體例中,L1
為(1c) (1c)
, 其中R7 、R8
及R10
各自獨立地為H或(C1
-C4
)烷基。本具體例可與Ar1 、Het 、Ar2 、R15 、Q1 、Q2 、R16 、R17
,及L2
之其他具體例組合使用。
在另一個具體例中,L1
為(1c) ,
其中R7
及R10
各自獨立地為CH3
。本具體例可與Ar1 、Het 、R8 、Ar2 、R15 、Q1 、Q2 、R16 、R17
,及L2
之其他具體例組合使用。
在另一個具體例中,L1
為(1d) (1d)
, 其中R7
、R9
及R10
各自獨立地為H或(C1
-C4
)烷基。本具體例可與Ar1 、Het 、Ar2 、R15 、Q1 、Q2 、R16 、R17
,及L2
之其他具體例組合使用。
在另一個具體例中,L1
為(1d)
,其中R7
及R10
各自獨立地為CH3
。本具體例可與Ar1 、Het 、R9 、Ar2 、R15 、Q1 、Q2 、R16 、R17
,及L2
之其他具體例組合使用。
在另一個具體例中,L1
為(1e) (1e)
, 其中,(1) Qx
為O或S;以及(2) R10
為H或(C1
-C4
)烷基。本具體例可與Ar1 、Het 、Ar2 、R15 、Q1 、Q2 、R16 、R17
,及L2
之其他具體例組合使用。
在另一個具體例中,L1
為(1e)
,其中R10
為CH3
。本具體例可與Ar1 、Het 、Q3 、Ar2 、R15 、Q1 、Q2 、R16 、R17
,及L2
之其他具體例組合使用。
在另一個具體例中,L1
為(1f) (1f)
, 其中:(1) Qx
為O或S;以及(2) R7
為H或(C1
-C4
)烷基。本具體例可與Ar1 、Het 、Ar2 、R15 、Q1 、Q2 、R16 、R17
,及L2
之其他具體例組合使用。
在另一個具體例中,L1
為(1f)
,其中R7
為CH3
。本具體例可與Ar1 、Het 、Q3 、Ar2 、R15 、Q1 、Q2 、R16 、R17
,及L2
之其他具體例組合使用。
在另一個具體例中,Ar2
為(1g) (1g)
, 其中:(1) R11
及R12
各自獨立地為H;(2) X1
為N或 CR13
,其中R13
為H或F;以及(3) R14
為H或Cl。
本具體例可與Ar1 、Het 、L1 、R15 、Q1 、Q2 、R16 、R17
,及L2
之其他具體例組合使用。
在另一個具體例中,R15
為H。本具體例可與Ar1 、Het 、L1 、Ar2 、Q1 、Q2 、R16 、R17
,及L2
之其他具體例組合使用。
在另一個具體例中,Q1
為O。本具體例可與Ar1 、Het 、L1 、Ar2 、R15 、Q2 、R16 、R17
,及L2
之其他具體例組合使用。
在另一個具體例中,Q2
為S。本具體例可與Ar1 、Het 、L1 、Ar2 、R15 、Q1 、R16 、R17
,及L2
之其他具體例組合使用。
在另一個具體例中,L2
為(1h) (1h)
, 其中:(1) R20
為(C1
-C4
)烷基,或是(C1
-C4
)烷基-O-(C1
-C4
)烷基;(2) R21 、R22
及R24
各自獨立地為H;以及(3) R23
為(C1
-C4
)烷基。
本具體例可與Ar1 、Het 、L1 、Ar2 、R15 、Q1 、Q2 、R16
及R17
之其他具體例組合使用。
在另一個具體例中,L2
為(1h)
,其中R20
為CH2
CH2
CH3
、CH(CH3
)2
、CH2
OCH3
,或是CH(CH3
)OCH3
。本具體例可與Ar1 、Het 、L1 、Ar1 、Q1 、Q2 、R16 、R17 、R21 、R22 、R23
,及R24
之其他具體例組合使用。
在另一個具體例中,L2
為(1f)
,其中R23
為CH3
。本具體例可與Ar1 、Het 、L1 、Ar2 、Q1 、Q2 、R16 、R17 、R20 、R21 、R22
,及R24
之其他具體例組合使用。
在另一個具體例中,R16
及R17
與Cx
(Q2
)(Nx
)
一起,為(1i) (1i)
,其中R18
及R19
各自獨立地為H。本具體例可與Ar1 、Het 、L1 、Ar2 、R15 、Q1
,及L2
之其他具體例組合使用。
在另一個具體例中(A) Ar1
為(1a) (1a) ,
其中,R1
、R2 、R3 、R4
及R5
各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基;(B) Het
為(1b) (1b) ,
其中R6
可以選擇性地以選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、側氧、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基;(C) L1
係選自於下列所構成的群組 (1c) , (1d) , (1e) ,
以及 (1f)
, 其中:(1) Qx
係各自獨立地選自於O及S所構成的群組,以及(2) R7
、R8 、R9
及R10
係各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基,以及(C2
-C6
)炔基;(D) Ar2
為(1g) (1g) ,
其中:(1) X1
係選自於N及CR13
所構成的群組,以及(2)R11
、R12 、R13 、
及R14
各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(=O)O-(C1
-C4
)烷基、苯基,以及苯氧基;(E) R15
係選自於下列所構成的群組:H、(C1
-C4
)烷基、(C3
-C8
)環烷基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、C(O)-NRx
Ry
、C(O)-苯基、(C1
-C4
)烷基-NRx
Ry
、C(O)O-(C1
-C4
)烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基,(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基, 其中每個烷基、環烷基、烯基、炔基,及苯基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、側氧、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基;(F) Q1
係選自於O及S所構成的群組;(G)Q2
係選自於O及S所構成的群組;(H) R16
係選自於下列所構成的群組:(K)
、H、(C1
-C4
)烷基、(C3
-C8
)環烷基、(C2
-C6
)烯基、(C2
-C6
)炔基、C(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、(C1
-C4
)烷基苯基、(C1
-C4
)烷基-O-苯基、C(O)-(Het-1)、(Het-1)、(C1
-C4
)烷基-(Het-1)、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-NRx
Ry
、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-(Het-1)、(C1
-C4
)烷基-C(O)-(Het-1)、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基(NRx
Ry
)-C(O)OH、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-NRx
Ry
、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-N(Rx
)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基(N(Rx
)-C(O)O-(C1
-C4
)烷基)-C(O)OH、(C1
-C4
)烷基-C(O)-(Het-1)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C3
-C8
)環烷基、(C1
-C4
)烷基-OC(O)-(Het-1)、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基-N(Rx
)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-NRx
Ry
、(C1
-C4
)烷基-S(O)n
-(Het-1),以及(C1
-C4
)烷基-O-(Het-1), 其中每個烷基、環烷基、烯基、炔基、苯基,及(Het-1)可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)OH、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基)、苯基、苯氧基、Si((C1
-C4
)烷基)3
、S(O)n
-NRx
Ry
,以及(Het-1);(I) R17
係選自於下列所構成的群組:(K)
、H、(C1
-C4
)烷基、(C3
-C8
)環烷基、(C2
-C6
)烯基、(C2
-C6
)炔基、C(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、(C1
-C4
)烷基苯基、(C1
-C4
)烷基-O-苯基、C(O)-(Het-1)、(Het-1)、(C1
-C4
)烷基-(Het-1)、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-NRx
Ry
、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-(Het-1)、(C1
-C4
)烷基-C(O)-(Het-1)、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基(NRx
Ry
)-C(O)OH、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-NRx
Ry
、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-N(Rx
)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基(N(Rx
)-C(O)O-(C1
-C4
)烷基)-C(O)OH、(C1
-C4
)烷基-C(O)-(Het-1)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C3
-C8
)環烷基、(C1
-C4
)烷基-OC(O)-(Het-1)、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基-N(Rx
)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-NRx
Ry
、(C1
-C4
)烷基-S(O)n
-(Het-1),以及(C1
-C4
)烷基-O-(Het-1), 其中每個烷基、環烷基、烯基、炔基、苯基,及(Het-1)可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)OH、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基、苯氧基、Si((C1
-C4
)烷基)3
、S(O)n
-NRx
Ry
,以及(Het-1);(J) L2
係(1h) (1h) ,
其中R20
、R21 、R22 、R23
及R24
各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C1
-C4
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、O-(C1
-C4
)烷基、S-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基、苯氧基,以及(Het-1), 其中每個烷基、環烷基、烯基、苯基,及(Het-1)取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C1
-C4
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、O-(C1
-C4
)烷基、S-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基、苯氧基,以及(Het-1);(K) R16
及R17
與Cx
(Q2
)(Nx
)
一起,係(1i) (1i) ,
其中R18
及R19
係各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2
、側氧、硫酮基、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及(Het-1);(L) Rx
及Ry
係各自獨立地選自於下列所構成的群組:H、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基,以及苯基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基,及苯基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及(Het-1);(M) (Het-1)
為5或6員、飽和或不飽和之雜環,含有獨立地選自於氮、硫或氧所構成的群組之一或多個雜原子, 其中每個雜環可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、側氧、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,及苯氧基;以及(N) n
每一者係獨立地為0、1或2。
在另一個具體例中,(A) Ar1
為(1a) (1a) ,
其中,R1
、R2 、R3 、R4
及R5
各自獨立地選自於下列所構成的群組:H及(C1
-C4
)鹵烷氧基;(B) Het
為(1b) (1b) ,
其中,R6
為H;(C) L1
係選自於下列所構成的群組 (1c) , (1d) , (1e) ,
及 (1f)
, 其中:(1) Qx
為O,以及(2) R7
、R8 、R9
及R10
各自獨立地選自於H及(C1
-C4
)烷基所構成的群組;(D) Ar2
為(1g) (1g) ,
其中:(1) X1
係選自於N及CR13
所構成的群組,以及(2)R11
、R12 、R13
及R14
各自獨立地選自於下列所構成的群組:H、F以及Cl;(E)R15
為H;(F) Q1
為O;(G)Q2
為S;(H)R16
為(K)
;(I)R17
為(K)
;(J) L2
係(1h) (1h) ,
其中,R20
、R21 、R22 、R23
及R24
各自獨立地選自於下列所構成的群組:H、(C1
-C4
)烷基,以及(C1
-C4
)烷基-O-(C1
-C4
)烷基;以及(K) R16
及R17
與Cx
(Q2
)(Nx
)
一起,係(1i) (1i) ,
其中R18
及R19
各自獨立地為H。
在另一個具體例中,(A) Ar1
為(1a) (1a) ,
其中,R1
、R2 、R3 、R4
及R5
各自獨立地選自於下列所構成的群組:H 及OCF3
;(B) Het
為(1b) (1b) ,
其中,R6
為H;(C) L1
係選自於下列所構成的群組 (1c) , (1d) , (1e) ,
及 (1f)
, 其中:(1) Qx
為O,以及(2) R7
、R8 、R9
及R10
各自獨立地選自於H及CH3
所構成的群組;(D) Ar2
為(1g) (1g) ,
其中:(1) X1
係選自於N及CR13
所構成的群組,以及(2)R11
、R12 、R13
及R14
各自獨立地選自於下列所構成的群組:H、F以及Cl;(E)R15
為H;(F) Q1
為O;(G)Q2
為S;(H)R16
為(K)
;(I)R17
為(K)
;(J) L2
係(1h) (1h) ,
其中,R20
、R21 、R22 、R23
及R24
各自獨立地選自於下列所構成的群組:H、CH3
、CH2
CH2
CH3
、CH(CH3
)2
、CH2
OCH3
,及CH(CH3
)OCH3
;以及(K) R16
及R17
與Cx
(Q2
)(Nx
)
一起,係(1i) (1i) ,
其中,R18
及R19
各自獨立地為H。式1 分子之製備
許多式1之分子可描述為二種或多種互變異構物形式,如當R16
及R17
為H時(流程圖TAU)。為了簡化流程圖,所有分子皆描繪為存在為單一互變異構物。任一與所有積極可得到的互變異構物皆包含於本式1之範疇中,且不應推斷為該分子皆存在有其畫出形式之互變異構物。流程圖TAU
式1分子一般具有大約400道耳頓至大約1200道耳頓之分子量。醯疊氮之製備
於此揭示之式1分子可以製備自相對應之異氰酸酯1-2
,其中Ar1 、Het 、L1
,及Ar2
係如先前所揭示。於一些情況中,此等異氰酸酯並未單離出,而是由適當的前驅物於原位產生,並直接用於製備式1分子。一種此等適當的前驅物為胺類1-1
,其中Ar1 、Het 、L1
,及Ar2
係如先前所揭示,胺類1-1
可轉化成異氰酸酯1-2
,其係藉由使用數種一般試劑如光氣、二光氣或三光氣之一者,於混合溶劑系統中,如二氯甲烷與水或是二乙基醚與水,於一種鹼如碳酸氫鈉或三乙基胺存在下,在溫度大約-10 ℃至大約50 ℃下進行(流程圖1,步驟a)。流程圖1
任擇地,異氰酸酯可經由醯疊氮1-4
之柯提斯重排反應(Curtius rearrangement)而產生,其中Ar1 、Het 、L1
及Ar2
係如先前所揭示,該醯疊氮繼而自對應的羧酸1-3
製備,其中Ar1 、Het 、L1
及Ar2
係如先前所揭示。醯疊氮1-4
可藉由以氯甲酸乙酯與疊氮鈉處理該酸,於胺基鹼如三乙基胺存在下而形成,或者以二苯基磷疊氮處理,在胺基鹼如三甲基胺存在下而形成(流程圖1,步驟b)。之後醯疊氮1-4
進行熱誘發的柯提斯重排反應,而產生對應之異氰酸酯1-2
。取決於特定的醯疊氮之特性,此種重排反應可於溶劑中,如甲苯、乙腈或醚類溶劑如二烷或四氫呋喃,在室溫下自發性地發生,或者可能需要加熱至40 ℃至約100 ℃。醯疊氮1-4
並非總是完全經鑑定出,但可不需鑑定直接加熱而生產異氰酸酯1-2
。線型縮二脲之製備
單離的異氰酸酯1-2 ,
由對應的醯疊氮1-4 、
經由柯提斯重排反應而於原位製備的異氰酸酯1-2 ,
或是由對應的羧酸、
經由疊氮化合物形成及隨後的柯提斯重排反應而於原位製備的異氰酸酯1-2
,可以直接以脲2-1
予以處理,其中Q2
及L2
係如先前所揭示,於大約0.1當量至大約2當量之無機鹼,如碳酸銫或氫化鈉之存在下,產生縮二脲2-2
,其中Ar1 、Het 、L1
、Ar2 、Q2
及L2
係如先前所揭示(流程圖2,步驟a)。反應可以於大約0 ℃至大約100 ℃的溫度下進行,較佳為大約20 ℃至大約80 ℃,於非質子溶劑或溶劑混合物中,其選自於乙腈、丙酮、甲苯、四氫呋喃、二氯乙烷、二氯甲烷或其混合物,但較佳使用乙腈。流程圖2 經取代的線型縮二脲之製備
線型縮二脲2-2
可以用R16
- 鹵
予以處理,其中R16
係如先前所揭示,於質子溶劑如乙醇中,於鹼如醋酸鈉存在下,於溫度約0 ℃至大約60 º℃下進行,以產出經取代的線型縮二脲3-1
,其中Ar1 、Het 、L1
、Ar2 、Q2 、R16
及L2
係如先前所揭示(流程圖3,步驟a)。流程圖3 環狀縮二脲之製備
原位產生之線型縮二脲2-2
可以不需純化直接轉化為各種環化的類似物(流程圖4),或是其等可在環化之前自反應介質中單離出。環化可藉由以α-鹵化酯如溴乙酸甲酯處理,以形成2-亞胺基 1,3-硫族唑啉-4-酮4-1
(2-imino 1,3-chalcogenazolin-4-ones4-1
),其中Ar1 、Het 、L1
、Ar2 、Q2 、R18 、R19
及L2
係如先前所揭示(流程圖4,步驟a);以鄰二鹵化物如1-溴-2-氯乙烷或1,2-二氯乙烷處理,以形成2-亞胺基-1,3-硫族唑啉(2-imino-1,3-chalogenazolines)4-2
,其中Ar1 、Het 、L1
、Ar2 、Q2 、R18 、R19
及L2
係如先前所揭示(流程圖4,步驟b);以α-鹵化酮如氯化丙酮處理,以形成2-亞胺基-1,3-硫族唑酮(2-imino-1,3-chalcogenazoles)4-3
,其中Ar1 、Het 、L1
、Ar2 、Q2 、R18 、R19
及L2
係如先前所揭示(流程圖4,步驟c);1,3-二鹵丙烷如1-溴-3-氯-丙烷,以形成2-亞胺基-1,3-硫族哌啶(2-imino-1,3-chalcogenazinanes)4-4
,其中Ar1 、Het 、L1
、Ar2 、Q2 、R18 、R19
及L2
係如先前所揭示(流程圖4,步驟d);或是α,β-不飽和醯氯,如丙烯醯氯來處理,以形成2-亞胺基-1,3-硫族酮(2-imino-1,3-chalcogenazinones)4-5
,其中Ar1 、Het 、L1
、Ar2 、Q2 、R18 、R19
及L2
係如先前所揭示(流程圖4,步驟e)。在流程圖3的步驟a中,較佳使用醋酸鈉,於質子溶劑如乙醇或甲醇中,於溫度範圍大約20 ℃至大約70 º℃下進行。在流程圖3的步驟b中,較佳使用無機鹼如碳酸鉀,於溶劑如乙腈或(較佳)2-丁酮中,於大約0 ℃至大約80 ℃之間的溫度下進行。流程圖4
流程圖5中描述環狀縮二脲之另一製備方法。2-亞胺基-1,3-硫族雜環(2-Imino-1,3-chalcogenazoheterocycles)5-1
,其中Q2
Cx
Nx 、R16 、R17
及L2
係如先前所揭示,可以於沒有鹼的情況下或是存在大約0.1當量至大約2當量之無機鹼,如碳酸銫或氫化鈉之下,直接與單離的異氰酸酯1-2
反應,單離的異氰酸酯1-2
為由對應的醯疊氮1-4 、
經由柯提斯重排反應而於原位製備的異氰酸酯1-2 ,
或是由對應的羧酸、
經由疊氮化合物形成及隨後的柯提斯重排反應而於原位製備的異氰酸酯1-2
,以形成環狀硫代縮二脲5-2
,其中Ar1 、Het 、L1
、Ar2 、Q2 、R16 、R17
及L2
係如先前所揭示(流程圖5,步驟a)。反應可以於溫度大約0 ℃至大約100 ℃下進行,較佳為大約20 ℃至大約80 ℃,於非質子溶劑或溶劑混合物中,其選自於乙腈、丙酮、甲苯、四氫呋喃、1,2-二氯乙烷、二氯甲烷或其混合物,但較佳使用乙腈。環狀縮二脲4-1 、4-2 、4-3 、4-4
及4-5
,其中L1
含有烯烴,可以於過渡金屬催化劑如附於碳上之鈀或氧化鉑(IV)存在下,藉由氫予以處理而還原。流程圖5
任擇地,2-亞胺基-1,3-硫族雜環(2-Imino-1,3-chalcogenazoheterocycles)5-1
,可以4-硝基苯基氯甲酸酯反應,形成4-硝基苯基胺甲酸酯5-2
,其中Cx
(Q2
)(Nx
) 、R16 、R17
及L2
係如先前所揭示(流程圖5,步驟b)。此反應之實施可以等莫耳量之2-亞胺基-1,3-硫族雜環(2-Imino-1,3-chalcogenazoheterocycles)5-1
與氯甲酸酯,於極性非質子溶劑,如四氫呋喃、二烷或乙腈中,於存在大約0.1當量至大約2當量之無機鹼,如碳酸銫或碳酸鉀下,較佳於大概室溫下進行。4-硝基苯基胺甲酸酯5-2
可自濾液過濾出且濃縮,或者4-硝基苯基胺甲酸酯5-2
可直接使用(流程圖5,步驟c)。以胺類1-1
來處理4-硝基苯基胺甲酸酯5-2
,可產生環狀硫代縮二脲5-2
。步驟c之進行亦可於大約0.1當量至大約2當量,較佳大約1當量至大約1.2當量之無機鹼,如碳酸銫或碳酸鉀存在下,於大約0 ℃至大約100 ℃的溫度下進行,較佳於室溫下進行。環狀縮二脲5-2
,其中L1
含有烯烴,可以於過渡金屬催化劑,如附於碳上之鈀或氧化鉑(IV)存在下,藉由氫予以處理而還原。流程圖6
流程圖6中描述環狀縮二脲之另一製備方法。胺類1-1
可以與4-硝基苯基氯甲酸酯反應,形成4-硝基苯基胺甲酸酯6-1
,其中Ar1 、Het 、L1
及Ar2
係如先前所揭示(流程圖6,步驟a)。此反應之實施可以等莫耳量之胺類1-1
與氯甲酸酯,於極性非質子溶劑,如四氫呋喃、二烷或乙腈中,於存在大約0.1當量至大約2當量之無機鹼,如碳酸銫或碳酸鉀下,較佳於大概室溫下進行。4-硝基苯基胺甲酸酯6-1
可自濾液過濾出且濃縮,或者4-硝基苯基胺甲酸酯6-1
可直接使用(流程圖6,步驟b)。以2-亞胺基-1,3-硫族雜環(2-Imino-1,3-chalcogenazoheterocycles)5-1
來處理4-硝基苯基胺甲酸酯6-1
,可產生環狀硫代縮二脲5-2
。此反應之實施可以等莫耳量之硝基苯基胺甲酸酯6-1
與2-亞胺基-1,3-硫族雜環5-1
,於極性非質子溶劑乙腈中,於大約0.1當量至大約2當量之無機鹼如碳酸銫或碳酸鉀下,以及大約2當量之有機鹼如N,N
-二異丙基乙胺存在下,較佳於大概室溫下進行。流程圖7
流程圖7中描述環狀縮二脲之額外的製備方法。以2-亞胺基-1,3-硫族雜環5-1
來處理胺甲酸酯7-1
,其中Ar1 、Het 、L1
及Ar2
係如先前所揭示,可產生環狀硫代縮二脲5-2
。此反應之實施可以於密封管中、在非質子溶劑例如甲苯內,於大約80 ℃至大約140 ℃的溫度下進行(流程圖7,步驟a)。環狀縮二脲5-2
,其中L1
含有烯烴,可以於過渡金屬催化劑如附於碳上之鈀或氧化鉑(IV)存在下,藉由氫予以處理而還原。羧酸之製備
流程圖8及9中描述式1分子之製備所需要的羧酸8-7
,其中Ar1 、R7
及Ar2
係如先前所揭示,之製備方法。硼酸8-1
,其中Ar1
係如先前所揭示,可以用經取代的三唑予以處理,於一種銅催化劑如乙酸銅(II),及一種鹼諸如吡啶存在下,在一種溶劑如二氯甲烷中,在大約15℃至大約30℃的溫度下進行,以形成硝基三唑8-2
,其中Ar1
係如先前所揭示(流程圖8,步驟a)。硝基三唑8-2
可以於過渡金屬催化劑如附於碳上之鈀或氧化鉑(IV)存在下,藉由氫予以處理而還原,以形成胺類8-3
,其中Ar1
係如先前所揭示(流程圖8,步驟b)。胺類8-3
可以用醛類8-4
,其中Ar2
係如先前所揭示,予以處理,於一種還原劑例如硼氫化鈉存在下,在大約50℃至大約90℃的溫度下進行,以形成酯類8-5
,其中Ar1
及Ar2
係如先前所揭示(流程圖8,步驟c)。酯類8-5
可以用烷基鹵化物例如碘甲烷(iodomethane)予以處理,於一種鹼諸如氫化鈉之存在下,於極性非質子溶劑例如N,N
-二甲基甲醯胺中,在大約-10℃至大約30℃的溫度下進行,以形成胺類8-6
,其中Ar1 、R7
及Ar2
係如先前所揭示(流程圖8,步驟d)。酯類8-5
及8-6
可以於溶劑如四氫呋喃、甲醇、水或其等之混合物中,用金屬氫氧化物如氫氧化鉀、氫氧化鈉或氫氧化鋰,予以處理以形成羧酸8-7
(流程圖8,步驟e)。流程圖8
硼酸8-1
可以用經取代的三唑予以處理,於一種銅催化劑如乙酸銅(II),及一種鹼諸如吡啶存在下,在一種溶劑如二氯甲烷中,在大約15℃至大約30℃的溫度下進行,以形成酯類9-1
,其中Ar1
係如先前所揭示(流程圖9,步驟a)。酯類9-1
可以於溶劑如四氫呋喃、甲醇、水或其等之混合物中,用金屬氫氧化物如氫氧化鉀、氫氧化鈉或氫氧化鋰,予以處理以形成羧酸9-2
,其中Ar1
係如先前所揭示(流程圖9,步驟b)。羧酸9-2
可以在極性溶劑像是二氯乙烷、四氫呋喃或其等之混合物之中,於N,N
-二甲基甲醯胺存在下,用草醯氯予以處理,接著用苯胺9-3
予以處理,其中R10
及Ar2
係如先前所揭示,以形成醯氯,其繼而在一種鹼諸如三甲基胺存在下,用苯胺予以處理而形成羧酸9-4
,其中Ar1 、R10
及Ar2
係如先前所揭示(流程圖9,步驟c)。流程圖9 胺類之製備
流程圖10中描述式1分子之製備所需要的胺類10-4
,其中Ar1 、R7
及Ar2
係如先前所揭示,之製備方法。胺類8-3
可以用經取代的醯氯10-1
,Ar2
係如先前所揭示,予以處理,於一種鹼諸如吡啶存在下,在一種溶劑如二氯甲烷中,在大約-10 ℃至大約30℃的溫度下進行,以形成硝基醯胺10-2
,其中Ar1
及Ar2
係如先前所揭示(流程圖10,步驟a)。硝基醯胺10-2
可以用烷基鹵化物例如碘甲烷予以處理,於一種鹼諸如碳酸鉀存在下,於極性非質子溶劑例如N,N
-二甲基甲醯胺中,在大約-10℃至大約30℃的溫度下進行,以形成硝基醯胺10-3
,其中Ar1 、R7
及Ar2
係如先前所揭示(流程圖10,步驟d)。硝基醯胺10-2
及10-3
可以於過渡金屬催化劑如附於碳上之鈀或氧化鉑(IV)存在下,藉由氫予以處理而還原,以形成胺類10-4
(流程圖10,步驟c)。流程圖10 2- 亞胺基-1,3- 硫族雜環 之製備
流程圖11中描述式1分子之製備所需要的2-亞胺基-1,3-硫族雜環之製備方法。苯胺11-1
,其中L2
係如先前所揭示,可以用氯乙醯氯予以處理,在一種鹼諸如碳酸氫鈉存在下,於極性非質子溶劑如乙酸乙酯中,在溫度大約-10 ℃至大約30 ℃下進行,以形成醯胺11-2
,其中L2
係如先前所揭示(流程圖11,步驟a)。醯胺11-2
係用硫氰酸鉀予以處理,在一種鹼諸如碳酸銫存在下,於極性溶劑如丙酮中,在溫度大約50 ℃至大約75 ℃下進行,以形成2-亞胺基-1,3-硫族雜環11-3
,其中L2
係如先前所揭示(流程圖11,步驟b)。流程圖11 實施例
此等實施例係為了說明之目的,而不應解釋為將本揭示限制為僅此等實施例中揭露的具體例。
自商業來源獲得之起始原料、試劑及溶劑係未經進一步純化即使用。無水溶劑係購自Aldrich之Sure/Seal™,及以所收到的形式使用。熔點係在Thomas Hoover Unimelt毛細管熔點儀或是在Stanford Research Systems之OptiMelt自動化熔點系統上測得,及未經校正。使用「室溫」的實施例係在溫度範圍大約20 ℃至大約24 ℃的氣候控制實驗室中進行。分子係以其等依據ISIS Draw、ChemDraw或ACD Name Pro內的命名程式所命名之已知名稱顯示。若此等程式無法命名一分子,則此分子係依習用的命名規則來命名。除非另有說明,否則1
H NMR光譜數據係以ppm (δ)為單位及於300、400、500或600 MHz記錄;13
C NMR光譜數據係以ppm (δ)為單位及於75、100或150 MHz記錄,以及19
F NMR光譜數據係以ppm (δ)為單位及於376 MHz記錄。實施例1 :3- 硝基-1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑(C1) 之製備
將3-硝基-1H
-1,2,4-三唑(2.00 g,17.5 mmol)、[(4-(三氟甲氧基)苯基]硼酸(3.97 g,19.3 mmol)、分子篩(5.00 g)、二氯甲烷(103 mL)、乙酸銅(II) (4.78 g,26.3 mmol),及吡啶(2.84 mL,35.1 mmol)添加至250 mL圓底燒瓶中。反應混合物於30 ℃下攪拌過夜。過濾掉固體,以及有機物係用水清洗、乾燥、過濾以及濃縮。藉由急速管柱層析法予以純化,其係使用乙酸乙酯作為沖提液,提供如白色固體之標題化合物(1.00 g,21%):mp 121-123 ℃;1
H NMR (400 MHz, CDCl3
) δ 8.61 (s, 1H), 7.82 (m, 2H), 7.45 (dq,J
= 8.1, 1.0 Hz, 2H);19
F NMR (376 MHz, CDCl3
) δ -57.97;ESIMSm/z
274 ([M+H]+
)。實施例2 : 1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 胺 (C2) 之製備
將3-硝基-1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑(C1)
(1.00 g,3.65 mmol)、甲醇(14.6 mL)及附於碳上之鈀 (10%,0.194 g,0.182 mmol)添加至50 mL圓底燒瓶中。將燒瓶密封,繼而排氣且用氫氣來重新填充(氣球,3x)。反應混合物係於氫氣下予以攪拌歷時3小時。反應混合物係經Celite®過濾以及用甲醇來清洗。所得固體係於真空烘箱中乾燥過夜,提供如灰白色固體之標題化合物(0.8900 g,100%):1
H NMR (400 MHz, CDCl3
) δ 8.19 (s, 1H), 7.62 (m, 2H), 7.32 (m, 2H), 4.28 (s, 2H);19
F NMR (376 MHz, CDCl3
) δ -58.08;ESIMSm/z
244([M+H]+
)。實施例3 :甲基 4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 基 ) 胺基) 甲基 ) 苯甲酸酯(C3) 之製備
將1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-胺(C2)
(0.200 g,0.819 mmol)、4-甲醯基苯甲酸甲酯(0.134 g,0.819 mmol)、乙醇(1.6 mL,0.5 M)及分子篩,添加至反應小瓶。使反應加熱至78℃過夜。添加額外量的4-甲醯基苯甲酸甲酯(0.134 g,0.819 mmol),以及反應係以78 ℃予以加熱。使反應冷卻至室溫,以及添加硼氫化鈉(0.0310 g,0.819 mmol)。反應加熱至50℃歷時40分鐘。使反應濃縮,以及以乙酸乙酯來溶解粗殘餘物且經Celite®予以過濾。濾液係用含水碳酸氫鈉、鹽水予以清洗、乾燥、過濾以及濃縮。藉由使用乙酸乙酯/己烷之急速管柱層析法予以純化,提供標題化合物(0.321 g,99%):1
H NMR (400 MHz, CDCl3
) δ 8.18 (d,J
= 6.1 Hz, 1H), 8.08 - 7.98 (m, 3H), 7.65 - 7.58 (m, 2H), 7.52 - 7.40 (m, 3H), 7.31 (dd,J
= 8.1, 5.2 Hz, 2H), 4.81 - 4.67 (m, 3H), 4.62 (d,J
= 6.3 Hz, 1H), 4.37 (qd,J
= 7.1, 4.2 Hz, 3H), 1.86 (t,J
= 6.0 Hz, 1H), 1.39 (td,J
= 7.1, 4.8 Hz, 5H);19
F NMR (376 MHz, CDCl3
) δ -58.10;ESIMSm/z
393([M+H]+
)。
下列化合物係以實施例 3 中概述之流程相似的方式予以製備: 甲基 2- 氟- 4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 基 ) 胺基) 甲基 ) 苯甲酸酯 (C4) 從1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-胺(C2)
製備且單離為灰白色固體(52%):mp 126–128 ℃;1
H NMR (400 MHz, DMSO-d6
) δ 8.90 (d,J
= 4.0 Hz, 1H), 7.91 (d,J
= 8.4 Hz, 1H) 7.85 - 7.76 (m, 2H), 7.50 (t,J
= 7.8 Hz, 3H), 7.40 - 7.23 (m, 1H), 7.14 - 6.99 (m, 1H), 4.47 (br d,J
= 6.4 Hz, 2H), 3.83 (s, 3H);19
F NMR (282 MHz, DMSO-d6
) δ -57.07, -110.75;ESIMSm/z
411 ([M+H]+
)。甲基 3- 氯- 4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 基 ) 胺基) 甲基 ) 苯甲酸酯 (C5)
從1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-胺(C2)
製備且單離為淡黃色固體(58%):mp 125–127 ℃;1
H NMR (400 MHz, DMSO-d6
) δ 8.92 (s, 1H), 7.95 - 7.84 (m, 2H), 7.84 - 7.76 (m, 2H), 7.61 (d,J
= 8.3 Hz, 1H), 7.49 (d,J
= 8.3 Hz, 2H), 7.12 (t,J
= 6.1 Hz, 1H), 4.53 (d,J
= 6.4 Hz, 2H), 3.85 (s, 3H);19
F NMR (282 MHz, DMSO-d6
) δ -57.07, -110.75;ESIMSm/z
427 ([M+H]+
)。甲基 5 -(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 基 ) 胺基) 甲基 ) 吡啶 甲酸酯(C6)
從1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-胺(C2)
製備且單離為灰白色固體(56%):mp 145–147 ℃;1
H NMR (300 MHz, DMSO-d6
) δ 8.92 (s, 1H), 8.72 (s, 1H), 8.02 (d,J
= 8.3 Hz, 1H), 7.95 (dd,J
= 2.0, 9.0 Hz, 1H), 7.82 (d,J
= 10.0 Hz, 2H), 7.50 (d,J
= 9.3 Hz, 2H), 7.15 (t,J
= 6.3 Hz, 1H), 4.48 (d,J
= 7.0 Hz, 2H), 3.85 (s, 3H);19
F NMR (282 MHz, DMSO-d6
) δ -57.04;ESIMSm/z
394 ([M+H]+
)。實施例4 :甲基 4 -(( 甲基 (1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 基 ) 胺基) 甲基 ) 苯甲酸酯 (C7) 之製備
在0 ℃於惰性氛圍下,將氫化鈉(95%,0.329 g,13.7 mmol)添加至配於乾N,N
-二甲基甲醯胺(20 mL)之甲基 4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸酯(C3)(
1.80 g,4.58 mmol)
的攪拌混合物。反應混合物係於0℃下攪拌歷時15分鐘,接而經由注射器逐滴地添加碘甲烷(0.172 mL,2.77 mmol)。生成的反應混合物係於0℃下攪拌歷時30分鐘。反應混合物用飽和的氯化銨(5 mL)來驟冷,以及用二乙基醚(3 x 25 mL)予以萃取。組合的有機層係用冰冷的水及鹽水清洗,於無水硫酸鈉上乾燥、過濾以及濃縮。藉由急速管柱層析法予以純化,提供如灰白色固體之標題化合物(0.900 g,48%):1
H NMR (400 MHz, CDCl3
) δ 8.21 (s, 1H), 8.05 (d,J
= 5.4 Hz, 2H), 7.69 – 7.60(m, 2H), 7.38 (d,J
= 8.10 Hz, 2H), 7.31 (d,J
= 8.4 Hz, 2H), 4.74 (s, 2H), 3.90 (s, 3H), 3.05 (s, 3H);ESIMSm/z
408 ([M+H]+
)。
下列化合物係以實施例 4
中概述之流程相似的方式予以製備:
甲基 2-
氟
-4
-((
甲基
(1-(4-(
三氟甲氧基)
苯基)-1H
-1,2,4-
三唑
-3-
基
)
胺基)
甲基
)
苯甲酸酯
(C8)
從甲基2-氟-4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸酯(C4)
製備且單離為灰白色固體(49%):ESIMSm/z
425 ([M+H]+
)。甲基 3- 氯 -4 -(( 甲基 (1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 基 ) 胺基) 甲基 ) 苯甲酸酯 (C9)
從甲基3-氯-4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸酯(C5)
製備且單離為灰白色固體(45%):1
H NMR (400 MHz, CDCl3
) δ 8.21 (s, 1H), 8.05 (s, 1H), 7.87 (dd,J
= 2.0, 8.4 Hz, 1H), 7.64 (dd,J
= 2.4, 6.0 Hz, 2H), 7.37 (d,J
= 8.4 Hz, 1H), 7.30 (d,J
= 8.4 Hz, 2H), 4.83(s, 2H), 3.91 (s, 3H), 3.14 (s, 3H);ESIMSm/z
441 ([M+H]+
)。甲基 5 -(( 甲基 (1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 基 ) 胺基) 甲基 ) 吡啶 甲酸酯 (C10)
從甲基5-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)吡啶甲酸酯(C6)
製備且單離為灰白色固體(35%):1
H NMR (400 MHz, CDCl3
) δ 8.72 (s, 1H), 8.22 (s, 1H), 8.10 (d,J
= 7.6, 1H), 7.81 (dd,J
= 2.0, 8.0 Hz, 1H), 7.67 – 7.60 (m, 2H), 7.31 (d,J
= 8.4 Hz, 2H), 4.76 (s, 2H), 3.98 (d,J
= 11.2 Hz, 3H), 3.08 (s, 3H);ESIMSm/z
408 ([M+H]+
)。實施例5 : 4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 基 ) 胺基) 甲基 ) 苯甲酸 (C11) 之製備
將甲基 4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸酯(C3)
(0.321 g,0.818 mmol)及氫氧化鋰(0.184 g,2.46 mmol)溶解於四氫呋喃(2.18 mL)、甲醇(2.18 mL)及水(1.09 mL)中。反應混合物係於室溫下攪拌過夜。使反應濃縮,用水來稀釋,以及用鹽酸(2N)來酸化。過濾固體,並於真空烘箱中乾燥,提供如白色固體之標題化合物(0.157 g,50%):1
H NMR (400 MHz, DMSO-d6
) δ 8.90 (s, 1H), 7.94 - 7.84 (m, 2H), 7.84 - 7.74 (m, 2H), 7.56 - 7.41 (m, 4H), 5.75 (s, 1H), 4.45 (d,J
= 6.3 Hz, 2H);19
F NMR (376 MHz, DMSO-d6
) δ -57.04;ESIMSm/z
379 ([M+H]+
)。
下列化合物係以實施例 5
中概述之流程相似的方式予以製備:
2-
氟
-4-(((1-(4-(
三氟甲氧基)
苯基)-1H
-1,2,4-
三唑
-3-
基
)
胺基)
甲基
)
苯甲酸
(C12)
從甲基 2-氟-4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸酯(C4)
製備且單離為灰白色固體(89%):1
H NMR (400 MHz, DMSO-d6
) δ 12.9 (s, 1H), 8.92 (s, 1H), 7.85 – 7.79 (m, 3H), 7.49 (d,J
= 8.8 Hz, 2H), 7.27 (t,J
= 8.4 Hz, 2H), 4.55 (s, 3H);ESIMSm/z
397 ([M+H]+
)。3- 氯 -4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 基 ) 胺基) 甲基 ) 苯甲酸(C13)
從甲基 3-氯-4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸酯(C5)
製備且單離為灰白色固體(0.700 g,92%):1
H NMR (300 MHz, CDCl3
) δ 12.9 (s, 1H), 8.22 (s, 1H), 8.08 (s, 1H), 7.93 (d,J
= 9.0 Hz, 1H), 7.64 – 7.60 (m, 3H), 7.31 (d,J
= 9.3 Hz, 2H), 5.18 (s, 1H), 4.71 (d,J
= 5.1 Hz, 2H);ESIMSm/z
413 ([M+H]+
)。5-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 基) 胺基 ) 甲基 ) 吡啶 甲酸(C14)
從甲基 5-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)吡啶甲酸酯(C6)
製備且單離為灰白色固體(0.850 g,92%):1
H NMR (300 MHz, CDCl3
) δ 12.9 (s, 1H), 8.91 (s, 1H), 8.70 (d,J
= 1.5 Hz, 1H), 8.04 – 7.90 (m, 2H), 7.82 (d,J
= 6.3 Hz, 2H), 7.49 (d,J
= 9.0 Hz, 2H), 7.11 (t,J
= 6.6 Hz, 1H), 4.52 (s, 2H);ESIMSm/z
380 ([M+H]+
)。4-(( 甲基 (1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 基 ) 胺基) 甲基 ) 苯甲酸(C15)
從甲基 4-((甲基(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸酯(C7)
製備且單離為灰白色固體(89%):ESIMS m/z 393 ([M+H]+
)。2- 氟- 4-(( 甲基 (1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 基 ) 胺基) 甲基 ) 苯甲酸(C16)
從甲基 2-氟-4-((甲基(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸酯(C8)
製備且單離為灰白色固體(91%粗製)。該化合物係直接使用於下一個反應。3- 氯- 4-(( 甲基 (1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 基 ) 胺基) 甲基 ) 苯甲酸(C17)
從甲基 3-氯-4-((甲基(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸酯(C9)
製備且單離為灰白色固體(92%):ESIMSm/z
427 ([M+H]+
)。5-(( 甲基(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 基) 胺基 ) 甲基 ) 吡啶 甲酸(C18)
從甲基 5-((甲基(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)吡啶甲酸酯(C10)
製備且單離為灰白色固體(0.080 g,41%):1
H NMR (400MHz, DMSO-d6
) δ 13.20 (s, 1H), 9.01 (s, 1H), 8.66 (s, 1H), 8.01 (d,J
= 8.4Hz, 1H), 7.95 – 7.84 (m, 3H), 7.51 (d,J
= 8.4 Hz, 2H), 4.73 (s, 2H), 3.01 (s, 3H);ESIMSm/z
394 ([M+H]+
)。實施例6 :4-(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 甲醯胺基) 苯甲酸(C19) 之製備
於氮氣中,將裝有配於乾二氯甲烷(22 mL)及四氫呋喃(2.8 mL)之1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-羧酸(C28)
(0.700 g,2.56 mmol)及草醯氯(0.673 mL,7.69 mmol)之乾燥的圓底燒瓶(100 mL)中,添加4-胺苯甲酸(0.932 g,7.69 mmol)及N,N
-二甲基甲醯胺(0.198 µL,2.56 µmol)。反應混合物係於23℃下攪拌歷時48小時。反應混合物係用鹽酸(1N)來酸化。經由過濾來收集固體,並於真空烘箱中乾燥,以提供如黃色固體之標題化合物(0.880 g, 79%):1
H NMR (400 MHz, DMSO-d6
) δ 10.84 (s, 1H), 9.57 (s, 1H), 8.31 (s, 1H), 8.16 - 8.09 (m, 2H), 8.03 - 7.97 (m, 2H), 7.97 - 7.91 (m, 2H), 7.65 (d,J
= 8.7 Hz, 2H); 13C NMR (126 MHz, DMSO-d6
) δ 167.34, 157.77, 148.22, 144.60, 144.58, 142.76, 135.80, 130.68, 126.51, 123.09, 122.46, 122.44, 120.31。
下列化合物係以實施例 6
中概述之流程相似的方式予以製備:4-(N
- 甲基-1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 甲醯胺基) 苯甲酸(C20)
從1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-羧酸(C28) 及
4-(甲胺)苯甲酸製備且單離為白色固體(0.544 g,66%):mp 190-194 ℃;1
H NMR (400 MHz, CDCl3
) δ 8.37 (s, 1H), 8.07 - 8.01 (m, 2H), 7.60 - 7.53 (m, 2H), 7.35 - 7.27 (m, 4H), 3.59 (s, 3H);13
C NMR (101 MHz, CDCl3
) δ 169.98, 160.98, 158.40, 140.81, 134.75, 131.21, 126.48, 122.36, 121.40, 77.33, 77.21, 77.01, 76.69;ESIMSm/z
407 ([M+H]+
)。實施例7 : 4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 基 ) 胺基) 甲基 ) 苯甲醯疊氮(C21) 之製備
在0℃下,將二苯基磷疊氮(0.340 g,1.27 mmol)及三乙基胺(0.160 g,1.58 mmol),添加至配於四氫呋喃(15 mL)之4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C11)
(0.400 g,1.05 mmol)的攪拌溶液。攪拌反應混合物,以及讓其加溫至室溫歷經4小時。濃縮反應混合物。用水來稀釋殘餘物,以及固體化合物予以過濾及乾燥,以得到如灰白色固體之標題化合物(0.400 g,93%)。粗化合物係於下一個步驟直接使用不需進一步純化。
下列化合物係以實施例 7
中概述之流程相似的方式予以製備:4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 甲醯胺基 ) 苯甲醯疊氮(C22)
從4-(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-甲醯胺基)苯甲酸(C19)
製備且單離為灰白色固體(0.079 g,32%):1
H NMR (400 MHz, CDCl3
) δ 9.17 (s, 1H), 8.62 (s, 1H), 8.11 - 8.04 (m, 2H), 7.89 - 7.80 (m, 4H), 7.45 - 7.38 (m, 2H);19
F NMR (376 MHz, CDCl3
) δ -57.98。4-(N
- 甲基-1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑 -3- 甲醯胺基 ) 苯甲醯疊氮(C23)
從4-(N
-甲基-1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-甲醯胺基)苯甲酸(C20)
製備且單離為無色固體(0.189 g,76%):1
H NMR (400 MHz, CDCl3
) δ 8.37 (s, 1H), 7.98 (dq,J
= 9.1, 2.3 Hz, 2H), 7.61 - 7.54 (m, 2H), 7.36 - 7.30 (m, 2H), 7.30 - 7.24 (m, 2H), 3.58 (s, 3H);19
F NMR (376 MHz, CDCl3
) δ -58.04。實施例8 : (Z
)-1-(3-(2- 異丙基-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基 )-3-(4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基) 脲( (Z
)-1-(3-(2-isopropyl-5-methylphenyl)- 4-oxothiazolidin-2-ylidene)-3-(4-(((1-(4-(trifluoromethoxy)phenyl)-1H
-1,2,4-triazol-3-yl)amino)methyl)phenyl)urea) (F2) 之製備
4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲醯疊氮(C21)
(0.020 mg, 0.050 mmol)配於乙腈(0.99 mL)係以80 ℃加熱歷時2小時。使反應混合物冷卻至室溫,以及添加2-亞胺基-3-(2-異丙基-5-甲基苯基)噻唑烷-4-酮(0.012 g,0.050 mmol)。反應混合物係於室溫下攪拌歷時10分鐘。反應混合物係用乙酸乙酯來稀釋,以及裝載至矽膠上。藉由急速管柱層析法予以純化,其係使用0-100%乙酸乙酯/B作為沖提液,B為二氯甲烷:己烷(1:1),提供如白色固體之標題化合物(0.015 g,48%)。
下列化合物係以實施例 8
中概述之流程相似的方式予以製備:(Z
)-N
-(4-(3-(3-(2- 異丙基-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基) 脲基) 苯 基-1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 甲醯胺(F26)
從4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-甲醯胺基)苯甲醯疊氮(C22)
及2-亞胺基-3-(2-異丙基-5-甲基苯基)噻唑烷-4-酮製備且單離為黃色固體(0.075 g,59%)。(Z
)-N
-(4-(3-(3-(2- 異丙基-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基) 脲基) 苯 基 )-N
- 甲基-1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 甲醯胺(F27)
從4-(N
-甲基-1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-甲醯胺基)苯甲醯疊氮(C23)
及2-亞胺基-3-(2-異丙基-5-甲基苯基)噻唑烷-4-酮製備且單離為黃色固體(0.095 g,32%)。
下列化合物係以實施例 7 及8
中概述之組合流程相似的方式予以製備:(Z
)-1-(3-(2-(1- 甲氧基乙基)-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基)-3-(4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基) 脲(F1)
從4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C11)
及2-亞胺基-3-(2-(1-甲氧基乙基)-5-甲基苯基)噻唑烷-4-酮(C38)
製備且單離為灰白色固體(0.025 g,36%)。(Z
)-1-(3-(5- 甲基-2- 丙基苯 基)-4- 氧噻唑亞烷-2- 基)-3-(4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基) 脲(F3)
從4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C11)
及2-亞胺基-3-(5-甲基-2-丙基苯基)噻唑烷-4-酮(C40)
製備且單離為淡黃色固體(0.105 g,63%)。(Z
)-1-(3-(2-( 甲氧基甲基)-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基)-3-(4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基) 脲(F4)
從4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C11)
及2-亞胺基-3-(2-(甲氧基甲基)-5-甲基苯基)噻唑烷-4-酮(C39)
製備且單離為灰白色固體(0.060 g,36%)。(Z
)-1-(2- 氟-4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基)-3-(3-(5- 甲基-2- 丙基苯 基)-4- 氧噻唑亞烷-2- 基) 脲(F5)
從2-氟-4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C12)
及2-亞胺基-3-(5-甲基-2-丙基苯基)噻唑烷-4-酮(C40)
製備且單離為灰白色固體(0.053 g,32%)。(Z
)-1-(2- 氟-4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基)-3-(3-(2-( 甲氧基甲基)-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基) 脲(F6)
從2-氟-4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C12)
及2-亞胺基-3-(2-(甲氧基甲基)-5-甲基苯基)噻唑烷-4-酮(C39)
製備且單離為灰白色固體(0.011 g,10%)。(Z
)-1-(3- 氯-4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基)-3-(3-(2- 異丙基-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基) 脲(F7)
從3-氯-4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C13)
及2-亞胺基-3-(2-異丙基-5-甲基苯基)噻唑烷-4-酮製備且單離為淡黃色固體(0.090 g,52%)。(Z
)-1-(3- 氯-4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基)-3-(3-(5- 甲基-2- 丙基苯 基)-4- 氧噻唑亞烷-2- 基) 脲(F8)
從3-氯-4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C13)
及2-亞胺基-3-(5-甲基-2-丙基苯基)噻唑烷-4-酮(C40)
製備且單離為淡黃色固體(0.070 g,45%)。(Z
)-1-(3- 氯-4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基)-3-(3-(2-( 甲氧基甲基)-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基) 脲(F9)
從3-氯-4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C13)
及2-亞胺基-3-(2-(甲氧基甲基)-5-甲基苯基)噻唑烷-4-酮(C39)
製備且單離為灰白色固體(0.160 g,65%)。(Z
)-1-(2- 氟-4-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基)-3-(3-(2- 異丙基-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基) 脲(F10)
從2-氟-4-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C12)
及2-亞胺基-3-(2-異丙基-5-甲基苯基)噻唑烷-4-酮製備且單離為灰白色固體(0.019 g,11%)。(Z
)-1-(3-(2- 異丙基-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基)-3-(5-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 吡啶-2- 基) 脲(F11)
從5-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)吡啶甲酸(C14)
及2-亞胺基-3-(2-異丙基-5-甲基苯基)噻唑烷-4-酮製備且單離為灰白色固體(0.097 g,59%)。(Z
)-1-(3-(5- 甲基-2- 丙基苯 基)-4- 氧噻唑亞烷-2- 基)-3-(5-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 吡啶-2- 基) 脲(F12)
從5-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)吡啶甲酸(C14)
及2-亞胺基-3-(5-甲基-2-丙基苯基)噻唑烷-4-酮(C40)
製備且單離為灰白色固體(0.050 g,59%)。(Z
)-1-(3-(2-( 甲氧基甲基)-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基)-3-(5-(((1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 吡啶-2- 基) 脲(F13)
從5-(((1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)吡啶甲酸(C14)
及2-亞胺基-3-(2-(甲氧基甲基)-5-甲基苯基)噻唑烷-4-酮(C39)
製備且單離為灰白色固體(0.050 g,59%)。(Z
)-1-(3-(2-( 甲氧基甲基)-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基)-3-(5-(( 甲基(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 吡啶-2- 基) 脲(F14)
從5-((甲基(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)吡啶甲酸(C18)
及2-亞胺基-3-(2-(甲氧基甲基)-5-甲基苯基)噻唑烷-4-酮(C39)
製備且單離為淡黃色固體(0.038 g,25%)。(Z
)-1-(5-(( 甲基(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 吡啶-2- 基)-3-(3-(5- 甲基-2- 丙基苯 基)-4- 氧噻唑亞烷-2- 基) 脲(F15)
從5-((甲基(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)吡啶甲酸(C18)
及2-亞胺基-3-(5-甲基-2-丙基苯基)噻唑烷-4-酮(C40)
製備且單離為淡黃色固體(0.020 g,32%)。(Z
)-1-(3-(2- 異丙基-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基 ) -3-(5-(( 甲基(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 吡啶-2- 基) 脲(F16)
從5-((甲基(1-(4-(三氟甲氧基)苯基)-1H-1,2,4-三唑-3-基)胺基)甲基)吡啶甲酸(C18)
及2-亞胺基-3-(2-異丙基-5-甲基苯基)噻唑烷-4-酮製備且單離為淡黃色固體(0.075 g,25%)。(Z
)-1-(2- 氟-4-(( 甲基(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基)-3-(3-(2-( 甲氧基甲基)-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基) 脲(F17)
從2-氟-4-((甲基(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C16)
及2-亞胺基-3-(2-(甲氧基甲基)-5-甲基苯基)噻唑烷-4-酮(C39)
製備且單離為淡黃色固體(0.060 g,64%)。(Z
)-1-(3- 氯-4-(( 甲基(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基)-3-(3-(2-( 甲氧基甲基)-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基) 脲(F18)
從3-氯-4-((甲基(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C17)
及2-亞胺基-3-(2-(甲氧基甲基)-5-甲基苯基)噻唑烷-4-酮(C39)
製備且單離為灰白色固體(0.2 g,62%)。(Z
)-1-(3- 氯-4-(( 甲基(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基)-3-(3-(5- 甲基-2- 丙基苯 基)-4- 氧噻唑亞烷-2- 基) 脲(F19)
從3-氯-4-((甲基(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C17)
及2-亞胺基-3-(5-甲基-2-丙基苯基)噻唑烷-4-酮(C40)
製備且單離為淡黃色固體(0.09 g,37%)。(Z
)-1-(3- 氯-4-(( 甲基(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基)-3-(3-(2-( 異丙基-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基) 脲(F20)
從3-氯-4-((甲基(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C17)
及2-亞胺基-3-(2-異丙基-5-甲基苯基)噻唑烷-4-酮製備且單離為淡黃色固體(0.120 g,46%)。(Z
)-1-(2- 氟-4-(( 甲基(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基)-3-(3-(5- 甲基-2- 丙基苯 基)-4- 氧噻唑亞烷-2- 基) 脲(F21)
從2-氟-4-((甲基(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C16)
及2-亞胺基-3-(5-甲基-2-丙基苯基)噻唑烷-4-酮(C40)
製備且單離為灰白色固體(0.019 g,30%)。(Z
)-1-(2- 氟-4-(( 甲基(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基)-3-(3-(2-( 異丙基-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基) 脲(F22)
從2-氟-4-((甲基(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C16)
及2-亞胺基-3-(2-異丙基-5-甲基苯基)噻唑烷-4-酮製備且單離為灰白色固體(0.054 g,58%)。(Z
)-1-(4-(( 甲基(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基)-3-(3-(5- 甲基-2- 丙基苯 基)-4- 氧噻唑亞烷-2- 基) 脲(F23)
從4-((甲基(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C15)
及2-亞胺基-3-(5-甲基-2-丙基苯基)噻唑烷-4-酮(C40)
製備且單離為灰白色固體(0.060 g,45%)。(Z
)-1-(3-(2- 異丙基-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基 ) -3-(4-(( 甲基(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 胺基) 甲基) 苯基) 脲(F24)
從4-((甲基(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)胺基)甲基)苯甲酸(C15)
及2-亞胺基-3-(2-異丙基-5-甲基苯基)噻唑烷-4-酮製備且單離為淡黃色固體(0.070 g,45%)。實施例9 :4- 硝基-N
-(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 苯甲醯胺(C24) 之製備
將吡啶(0.994 mL,12.3 mmol)添加至配於二氯甲烷(20.5 mL)之1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-胺(C2)
(1.00 g,4.10 mmol)。使反應混合物冷卻至0 ℃,接而逐滴地添加配於二氯甲烷之4-硝苯甲醯氯(0.836 g,4.50 mmol)。溶液係於0℃下拌歷時2小時。反應混合物係用二氯甲烷予以稀釋,以及用鹽酸(2 N)來清洗。將層予以分離,以及以用二氯甲烷(3x)予以進一步清洗。將組合的有機層濃縮。藉由急速管柱層析法予以純化,其係使用二氯甲烷/甲醇作為沖提液,提供如白色固體之標題化合物(1.43 g,88%):mp 197-199 ℃;1
H NMR (400 MHz, CDCl3
) δ 8.88 (s, 1H), 8.38 (m, 3H), 8.14 (m, 2H), 7.75 (m, 2H), 7.38 (m, 2H);13
C NMR (101 MHz, CDCl3
) δ 162.45, 156.95, 150.15, 140.27, 138.93, 135.02, 128.72, 124.10, 122.39, 121.40, 60.41, 21.06, 14.21;ESIMSm/z
394 ([M+H]+
)。實施例10 :N
- 甲基-4- 硝基-N
-(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 苯甲醯胺(C25) 之製備
於氮氣下,將碳酸鉀(0.105 g,0.763 mmol)添加至反應小瓶內配於N,N
-二甲基甲醯胺(3.8 mL)之4-硝基-N-(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)苯甲醯胺(C24)
(0.300 g,0.763 mmol)。反應混合物予以攪拌歷時15分鐘過夜,以及冷卻至0 ℃。添加碘甲烷(0.0477 mL,0.763 mmol)。允許反應混合物加溫至室溫過夜。反應混合物用含水氯化銨來驟冷,以及用乙酸乙酯予以萃取。有機層係用鹽水清洗以及濃縮。藉由急速管柱層析法予以純化,其係使用乙酸乙酯/己烷作為沖提液,提供如黃色固體之標題化合物(0.193 g,62%):mp 122-124 ℃;1
H NMR (400 MHz, CDCl3
) δ 8.28 (s, 1H), 8.21 - 8.09 (m, 2H), 7.68 - 7.56 (m, 2H), 7.52 - 7.46 (m, 2H), 7.32 (dq,J
= 9.0, 0.9 Hz, 2H), 3.62 (s, 3H);13
C NMR (126 MHz, CDCl3
) δ 168.64, 161.84, 148.52, 142.25, 140.58, 140.55, 134.69, 128.92, 128.90, 123.30, 123.27, 122.49, 121.34, 120.78, 119.28, 35.82, 35.77;19
F NMR (471 MHz, CDCl3
) δ -58.06;ESIMSm/z
408 ([M+H]+
)。實施例11 :4- 胺基-N
- 甲基-N
-(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 苯甲醯胺(C26) 之製備
將N
-甲基-4-硝基-N
-(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)苯甲醯胺(C25)
(0.193 g,0.474 mmol)及附於碳上之鈀(0.0700 g,0.0660 mmol)添加至25 mL反應小瓶。添加乙酸乙酯(4.7 mL),以及將小瓶密封。使小瓶排氣,接而用氫氣來重新填充(氣球,3x)。反應混合物係於氫氣下以氣球予以攪拌歷時2小時。反應混合物經Celite®予以過濾以及濃縮。藉由急速管柱層析法予以純化,其係使用0-100%乙酸乙酯/B作為沖提液,B為1:1二氯甲烷/己烷,提供如白色固體之標題化合物(0.135 g,75%):mp 167-169 ℃;1
H NMR (400 MHz, CDCl3
) δ 8.30 (s, 1H), 7.60 - 7.50 (m, 2H), 7.36 - 7.28 (m, 4H), 6.57 - 6.43 (m, 2H), 3.84 (s, 2H), 3.54 (s, 3H);19
F NMR (376 MHz, CDCl3
) δ -58.06;ESIMSm/z
378 ([M+H]+
)。實施例12 :(Z
)-4-(3-(3-(2- 異丙基-5- 甲基苯 基)-4- 氧噻唑亞烷-2- 基) 脲基)-N
- 甲基-N
-(1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 基) 苯甲醯胺(F25) 之製備
將配於乙腈(0.3 mL)之4-硝苯基氯甲酸酯(0.0363 g,0.180 mmol)添加至配於乙腈(4 mL)之4-胺基-N
-甲基-N
-(1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-基)苯甲醯胺(C26)
(0.0680 g,0.180 mmol)。反應係於室溫下攪拌歷時30分鐘。添加碳酸銫(0.0587 g,0.180 mmol)、2-亞胺基-3-(2-異丙基-5-甲基苯基)噻唑烷-4-酮(0.0448 g,0.180 mmol),以及N,N
-二乙基異丙胺(0.0630 mL,0.360 mmol),以及使反應於室溫下攪拌。反應混合物係用乙酸乙酯稀釋,及以鹽水清洗。鹽水係用乙酸乙酯來萃取。有機層係於硫酸鈉上乾燥、過濾以及濃縮。藉由逆相管柱層析法予以純化,使用0-100%乙腈/水作為沖提液,提供如灰白色固體之標題化合物(0.0880 g,74%)。實施例13 :甲基 1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 羧酸酯(C27) 之製備
將1H
-1,2,4-三唑-3-羧酸甲酯(5.00 g,39.3 mmol)、(4-(三氟甲氧基)苯基)硼酸(8.10 g,39.3 mmol),及乙酸銅(II) (7.15 g,39.3 mmol)添加至反應燒瓶。將燒瓶密封且排氣/重新填充氮氣(3x)。添加二氯甲烷(157 mL),接著添加吡啶(4.77 mL,59.0 mmol)。允許反應混合物於室溫下攪拌過夜。添加水,並且反應混合物係經Celite®予以過濾。將濾液移至分液漏斗,以及將層予以分離。有機層係用水進一步清洗(3x)、組合、於硫酸鈉上乾燥、過濾以及濃縮。粗產物係以小量乙酸乙酯/己烷予以研磨及過濾,以提供如白色固體之標題化合物(2.17 g,19%):mp 156-158 ℃;1
H NMR (300 MHz, CDCl3
) δ 8.65 (s, 1H), 7.86 - 7.75 (m, 2H), 7.48 - 7.32 (m, 2H), 4.06 (s, 3H);19
F NMR (471 MHz, CDCl3
) δ -58.00;13
C NMR (126 MHz, CDCl3
) δ 159.89, 149.29, 134.81, 122.44, 122.07, 121.35, 119.29, 53.06;EIMSm/z
288 ([M]+
)。實施例14 :1-(4-( 三氟甲氧基) 苯基)-1H
-1,2,4- 三唑-3- 羧酸(C28) 之製備
將甲基 1-(4-(三氟甲氧基)苯基)-1H
-1,2,4-三唑-3-羧酸酯(C27)
(1.00 g,3.48 mmol)、水(8.70 mL),及四氫呋喃(26.1 mL)添加至圓底反應燒瓶。添加氫氧化鋰•水合物(0.438 g,10.5 mmol),以及反應混合物係於23℃下攪拌過夜。反應混合物係予以酸化,以提供如白色固體之標題化合物(0.928 g,93%):1
H NMR (400 MHz, DMSO-d6
) δ 13.62 (s, 1H), 9.45 (s, 1H), 8.16 - 7.92 (m, 2H), 7.64 (dt,J
= 7.8, 1.2 Hz, 2H)。實施例15 :1- 氟-2- 甲基-4- 硝基-5-( 丙-1- 烯-2- 基) 苯(C29) 之製備
將1-氯-5-氟-4-甲基-2-硝苯(1.50g,7.91 mmol)、4,4,5,5-四甲基-2-(丙-1-烯-2-基)-1,3,2-二戊硼烷(1.79 mL,9.50 mmol)、雙(三苯基膦)二氯化鈀(II) (0.444g,0.633 mmol),以及碳酸鈉(1.01g,9.50 mmol)添加至反應小瓶。添加水(2.85 mL)及二烷(11.4 mL)。將小瓶加蓋,以及係於具有外部IR-感測器監測小瓶側的溫度之Biotage Initiator®微波反應器中,以140 ℃加熱歷時30分鐘。使反應冷卻至室溫,用乙酸乙酯來稀釋,以及用水來清洗。水層係以乙酸乙酯(3x)進一步萃取。組合的有機層係於硫酸鎂上乾燥、過濾及濃縮。藉由急速管柱層析法予以純化,其係用0-40%乙酸乙酯/己烷予以沖提,提供如黃色液體之標題化合物(1.42g,88%):1
H NMR (400 MHz, CDCl3
) δ 7.81 (dd,J
= 7.0, 0.9 Hz, 1H), 6.95 (d,J
= 9.4 Hz, 1H), 5.17 (t,J
= 1.5 Hz, 1H), 4.97 - 4.86 (m, 1H), 2.33 (dd,J
= 2.0, 0.8 Hz, 3H), 2.06 (dd,J
= 1.6, 0.9 Hz, 3H);19
F NMR (376 MHz, CDCl3
) δ -108.66;EIMSm/z
195 ([M]+
)。實施例16 :4- 氟-2- 異丙基-5- 甲基苯胺(C30) 之製備
添加配於乙酸乙酯(29 mL)之1-氟-2-甲基-4-硝基-5-(丙-1-烯-2-基)苯(C29)
(1.41g,7.22 mmol)添加附於碳上之鈀(10 重量%,0.770g,0.720 mmol)添加至反應燒瓶。使燒瓶排氣,繼而用氫氣來重新填充(氣球) (3x)。反應混合物係於氫氣下以氣球予以攪拌過夜。反應混合物經Celite®予以過濾以及濃縮,以提供如黃色液體之標題化合物(1.10g,90%):1
H NMR (400 MHz, CDCl3
) δ 6.79 (d,J
= 11.1 Hz, 1H), 6.49 (d,J
= 7.0 Hz, 1H), 3.39 (s, 2H), 2.91 - 2.80 (m, 1H), 2.17 (d,J
= 2.0 Hz, 3H), 1.22 (d,J
= 6.8 Hz, 6H);13
C NMR (101 MHz, CDCl3
) δ 138.55, 122.03, 118.40, 118.35, 111.97, 111.73, 27.63, 22.29, 14.16;EIMSm/z
167 ([M]+
)。
下列化合物係以實施例 16
中概述之流程相似的方式予以製備:2-( 甲氧基甲基)-5- 甲基苯胺(C31)
從1-(甲氧基甲基)-4-甲基-2-硝苯(C46)
製備且單離為橘色油(1.6g,100%):1
H NMR (400 MHz, CDCl3
) δ 6.94 (d,J
= 7.3 Hz, 1H), 6.56 - 6.49 (m, 2H), 4.44 (s, 2H), 4.11 (s, 2H), 3.32 (s, 3H), 2.26 (s, 3H);13
C NMR (101 MHz, CDCl3
) δ 146.16, 139.28, 130.09, 119.27, 118.70, 116.44, 73.46, 57.26, 21.25;EIMSm/z
151 ([M]+
)。實施例17 :2- 氯-N
-(2- 氟-5- 甲基苯 基) 乙醯胺(C32) 之製備
將2-氟-5-甲基苯胺(3.00g,24.0 mmol)及乙酸乙酯(24.0 mL)添加至反應燒瓶。使反應冷卻至0℃。加入碳酸氫鈉(4.03g,47.9 mmol),接著於4分鐘期間逐滴地添加氯乙醯氯(2.30 mL,28.8 mmol)。允許反應混合物於0℃下攪拌歷時10分鐘,然後允許反應加溫至室溫且進一步攪拌歷時90分鐘。將水(15 mL)添加至反應,以及使相分離。有機層係用鹽水(20 mL)清洗,於硫酸鎂上乾燥、過濾以及濃縮,以提供標題化合物(4.83g,100%):1
H NMR (400 MHz, CDCl3
) δ 8.47 (s, 1H), 8.08 (dd,J
= 7.5, 2.1 Hz, 1H), 7.00 (dd,J
= 10.7, 8.4 Hz, 1H), 6.90 (dddd,J
= 8.3, 5.0, 2.2, 0.8 Hz, 1H), 4.21 (s, 2H), 2.34 (d,J
= 0.9 Hz, 3H);19
F NMR (376 MHz, CDCl3
) δ -135.59;13
C NMR (126 MHz, CDCl3
) δ 163.83, 151.92, 150.00, 134.42, 125.79, 121.94, 114.64, 42.92, 21.08;ESIMSm/z
201 ([M+H]+
)。
下列化合物係以實施例 17
中概述之流程相似的方式予以製備:2- 氯-N
-(2-(1- 甲氧基乙基)-5- 甲基苯 基) 乙醯胺(C33)
從2-(1-甲氧基乙基)-5-甲基苯胺(C45)
製備且單離為黃色油(2.19g,71%):1
H NMR (300 MHz, CDCl3
) δ 10.16 (s, 1H), 8.17 (s, 1H), 7.02 (d,J
= 7.7 Hz, 1H), 6.99 - 6.85 (m, 1H), 4.45 (q,J
= 6.7 Hz, 1H), 4.20 (dd,J
= 2.6, 1.1 Hz, 2H), 3.34 (d,J
= 1.1 Hz, 3H), 2.37 (d,J
= 1.0 Hz, 3H), 1.52 (dd,J
= 6.9, 1.0 Hz, 3H);13
C NMR (126 MHz, CDCl3
) δ 164.22, 138.56, 135.55, 128.26, 127.41, 125.20, 122.16, 80.90, 77.31, 77.05, 76.80, 56.25, 43.10, 21.37, 20.95。2- 氯-N
-(2-( 甲氧基甲基)-5- 甲基苯 基) 乙醯胺(C34)
從2-(甲氧基甲基)-5-甲基苯胺(C31)
製備且單離為橘色油(1.89 g,77%):1
H NMR (400 MHz, CDCl3
) δ 9.74 (s, 1H), 8.01 - 7.95 (m, 1H), 7.09 (d,J
= 7.6 Hz, 1H), 6.97 - 6.88 (m, 1H), 4.49 (s, 2H), 4.23 (s, 2H), 3.43 (s, 3H), 2.36 (s, 3H);13
C NMR (101 MHz, CDCl3
) δ 164.65, 139.40, 136.56, 129.19, 125.42, 124.08, 122.41, 73.55, 58.01, 43.06, 40.47;EIMSm/z
227 ([M]+
)。2- 氯-N
-(5- 甲基-2- 丙基苯 基) 乙醯胺(C35)
從5-甲基-2-丙基苯胺製備且單離為粉紅色固體(1.86g,92%): mp 108-111 ℃;1
H NMR (400 MHz, CDCl3
) δ 8.28 (s, 1H), 7.74 - 7.69 (m, 1H), 7.09 (d,J
= 7.8 Hz, 1H), 6.98 - 6.94 (m, 1H), 4.24 (s, 2H), 2.55 (dd,J
= 8.6, 6.8 Hz, 2H), 2.34 (s, 3H), 1.67 - 1.57 (m, 2H), 0.99 (td,J
= 7.3, 2.9 Hz, 3H);13
C NMR (101 MHz, CDCl3
) δ 132.21, 130.32, 129.67, 126.64, 123.34, 43.24, 33.16, 23.23, 13.94;EIMSm/z
225 ([M]+
)。2- 氯-N
-(4- 氟-2- 異丙基-5- 甲基苯 基) 乙醯胺(C36)
從4-氟-2-異丙基-5-甲基苯胺(C30)
製備且單離為橘色固體(1.20g,85%): mp 126-134 ℃;1
H NMR (400 MHz, CDCl3
) δ 8.13 (s, 1H), 7.50 (d,J
= 7.4 Hz, 1H), 6.94 (d,J
= 10.9 Hz, 1H), 4.24 (s, 2H), 3.05 - 2.88 (m, 1H), 2.24 (dd,J
= 2.0, 0.7 Hz, 3H), 1.24 (d,J
= 6.8 Hz, 6H);19
F NMR (376 MHz, CDCl3
) δ -118.99;EIMSm/z
243 ([M]+
)。實施例18 :3-(2- 氟-5- 甲基苯 基)-2- 亞胺基噻唑烷-4- 酮(C37) 之製備
將2-氯-N
-(2-氟-5-甲基苯基)乙醯胺(C32)
(2.00g,9.92 mmol)及丙酮(9.92 mL)添加至反應燒瓶。加入固體硫氰酸鉀(1.93g,19.8 mmol),以及以65 ℃加熱反應歷時3小時。使反應冷卻至室溫。添加碳酸銫(0.162g,0.496 mmol),以及反應係於室溫下攪拌歷時45分鐘。反應混合物係經Celite®予以過濾、以丙酮清洗,並濃縮。藉由急速管柱層析法予以純化,使用0-60%乙酸乙酯/己烷作為沖提液,提供如淡橘色固體之標題化合物(1.790g,80%):mp 120-122 ℃;1
H NMR (400 MHz, CDCl3
) δ 7.89 (s, 1H), 7.24 (s, 1H), 7.20 - 7.01 (m, 2H), 4.20 - 3.99 (m, 2H), 2.36 (s, 3H);19
F NMR (376 MHz, CDCl3
) δ -125.16;ESIMSm/z
225 ([M+H]+
)。
下列化合物係以實施例 18
中概述之流程相似的方式予以製備:2- 亞胺基-3-(2-(1- 甲氧基乙基)-5- 甲基苯 基) 噻唑烷-4- 酮(C38)
從2-氯-N
-(2-(1-甲氧基乙基)-5-甲基苯基)乙醯胺(C33)
製備且單離為橘色固體(1.80g,71%): mp 94-108 ℃;1
H NMR (300 MHz, CDCl3
) δ 7.51 (d,J
= 7.9 Hz, 1H), 7.34 (dd,J
= 8.0, 1.9 Hz, 1H), 7.00 6.86 (m, 1H), 4.21 4.05 (m, 2H), 3.12 (d,J
= 1.1 Hz, 2H), 2.38 (s, 3H), 1.42 1.31 (m, 3H);13
C NMR (75 MHz, CDCl3
) δ 210.86, 170.85, 139.07, 131.65, 129.19, 129.06, 127.13, 77.52, 77.09, 76.67, 74.46, 74.15, 69.51, 56.72, 56.54, 53.81, 31.76, 29.28, 23.35, 20.98。2- 亞胺基-3-(2-( 甲氧基甲基)-5- 甲基苯 基) 噻唑烷-4- 酮(C39)
從2-氯-N
-(2-(甲氧基甲基)-5-甲基苯基)乙醯胺(C34)
製備且單離為橘色固體(0.550g,25%):mp 66-71 ℃;1
H NMR (400 MHz, CDCl3
) δ 9.37 (s, 1H), 8.00 (s, 1H), 7.07 (d,J
= 7.6 Hz, 1H), 6.97 - 6.89 (m, 1H), 4.56 (s, 2H), 3.86 (s, 2H), 3.42 (s, 3H), 2.37 (s, 3H);13
C NMR (101 MHz, CDCl3
) δ 162.54, 139.50, 136.62, 129.24, 125.51, 123.55, 122.35, 73.76, 57.85, 37.87, 21.45;EIMSm/z
250 ([M]+
)。2- 亞胺基-3-(5- 甲基-2- 丙基苯 基) 噻唑烷-4- 酮(C40)
從2-氯-N
-(5-甲基-2-丙基苯基)乙醯胺(C35)
製備且單離為白色固體(1.76g,84%):mp 120-123 ℃;1
H NMR (400 MHz, DMSO-d6
) δ 9.67 (s, 1H), 7.17 (d,J
= 1.7 Hz, 1H), 7.11 (d,J
= 7.7 Hz, 1H), 7.00 - 6.93 (m, 1H), 4.11 (s, 2H), 2.52 - 2.48 (m, 2H), 2.25 (s, 3H), 1.50 (h,J
= 7.4 Hz, 2H), 0.88 (t,J
= 7.3 Hz, 3H);13
C NMR (126 MHz, DMSO-d6
) δ 164.20, 134.56, 134.13, 132.75, 128.76, 126.11, 125.70, 112.19, 36.01, 31.68, 22.32, 19.91, 13.23;EIMSm/z
248 ([M]+
)。3-(4- 氟-2- 異丙基-5- 甲基苯 基)-2- 亞胺基噻唑烷-4- 酮(C41)
從2-氯-N
-(4-氟-2-異丙基-5-甲基苯基)乙醯胺(C36)
製備且單離為棕色油(1.11g,80%):1
H NMR (400 MHz, CDCl3
) δ 7.86 (s, 1H), 7.07 (d,J
= 10.7 Hz, 1H), 6.93 (d,J
= 7.3 Hz, 1H), 4.12 - 4.00 (m, 2H), 2.72 - 2.59 (m, 1H), 2.25 (s, 3H), 1.17 (d,J
= 7.0 Hz, 6H);19
F NMR (376 MHz, CDCl3
) δ -114.93;ESIMSm/z
267 ([M+H]+
)。實施例19 :1-(4- 甲基-2- 硝基苯基) 乙-1- 酮(C42) 之製備
將4-甲基-2-硝基-1-(丙-1-烯-2-基)苯(11.4 g,64.3 mmol)、二氯甲烷(292 mL)及甲醇(29.2 mL)添加至反應燒瓶。使反應混合物冷卻至-78℃。使臭氧於反應混合物內起泡,以及反應混合物係於-78℃下攪拌歷時3小時。用氮沖洗反應混合物。加入二甲硫(14.0 mL,189 mmol),以及允許反應混合物攪拌且加溫至室溫過夜。使反應濃縮。藉由急速管柱層析法予以純化,其係使用乙酸乙酯/己烷作為沖提液,提供如油之標題化合物(8.90g,70%):1
H NMR (300 MHz, CDCl3
) δ 7.85 (dt,J
= 2.0, 1.0 Hz, 1H), 7.50 (ddt,J
= 7.8, 1.7, 0.8 Hz, 1H), 7.35 (dd,J
= 7.7, 0.9 Hz, 1H), 2.57 - 2.51 (m, 3H), 2.49 (q,J
= 0.9 Hz, 3H)。實施例20 :1-(4- 甲基-2- 硝基苯基) 乙-1- 醇(C43) 之製備
於氮氣氛圍下,將1-(4-甲基-2-硝基苯基)乙-1-酮(C42)
(8.91g,49.7 mmol)及甲醇(249 mL)添加至反應燒瓶。使反應混合物冷卻至0℃。加入硼氫化鈉(2.26g,59.7 mmol),以及使反應混合物於0℃下攪拌歷時1小時。允許反應混合物加溫至室溫過夜。反應混合物係用鹽酸(2N)來酸化,以及用二氯甲烷稀釋。將層予以分離,以及用二氯甲烷來萃取水相。組合的有機層係於硫酸鈉上乾燥、過濾及濃縮。藉由急速管柱層析法予以純化,其係使用乙酸乙酯/己烷作為沖提液,提供如綠色油之標題化合物(7.10g,75%):1
H NMR (400 MHz, CDCl3
) δ 7.73 - 7.66 (m, 2H), 7.45 (dd,J
= 8.0, 2.1 Hz, 1H), 5.45 - 5.26 (m, 1H), 2.42 (s, 3H), 1.54 (s, 3H)。實施例21 :1-(1- 甲氧基乙基)-4- 甲基-2- 硝苯(C44) 之製備
將1-(4-甲基-2-硝基苯基)乙-1-醇(C43)
(6.14g,33.9 mmol)及四氫呋喃(169 mL)添加至乾燥的圓底燒瓶。使反應混合物冷卻至0℃。於氮氣氛圍下,添加氫化鈉(60%油浸,2.03g,50.8 mmol)。反應混合物係於0℃下攪拌歷時30分鐘,繼而加入碘甲烷(3.18 mL,50.8 mmol)。允許反應混合物加溫至室溫且攪拌過夜。反應係用飽和的含水氯化銨予以稀釋,以及添加水。將層予以分離,以及以二氯甲烷(2x)萃取水相。組合的有機層係於硫酸鈉上乾燥、過濾及濃縮。藉由急速管柱層析法予以純化,其係使用乙酸乙酯/己烷作為沖提液,提供如黃色油之標題化合物(7.10g,98%):1
H NMR (400 MHz, CHCl3) δ 7.78 - 7.68 (m, 1H), 7.61 (d,J
= 8.0 Hz, 1H), 7.45 (ddd,J
= 8.1, 1.8, 0.9 Hz, 1H), 4.84 (q,J
= 6.3 Hz, 1H), 3.19 (d,J
= 0.8 Hz, 3H), 2.43 (s, 3H), 1.50 (dd,J
= 6.3, 0.8 Hz, 3H);13
C NMR (126 MHz, CDCl3
) δ 148.60, 138.44, 136.60, 134.47, 127.44, 124.41, 77.49, 77.23, 76.98, 74.87, 56.82, 23.44, 20.75。實施例22 :2-(1- 甲氧基乙基)-5- 甲基苯胺(C45) 之製備
將1-(1-甲氧基乙基)-4-甲基-2-硝苯(C44)
(7.00g,35.9 mmol)、氯化鎳(II) (4.65g,35.9 mmol)及甲醇(179 mL)添加至反應燒瓶。於氮氣氛圍下,每2-3分鐘以每份200-500 mg的方式將硼氫化鈉(2.94g,78.0 mmol)添加至反應混合物。反應係用丙酮(6 mL)來驟冷,並且濃縮至大概80 mL。粗混合物係用二氯甲烷來稀釋,以及用水清洗。將層予以分離,以及有機物係予以濃縮。藉由急速管柱層析法予以純化,其係使用乙酸乙酯/己烷作為沖提液,提供如橘色油之標題化合物(2.99g,45%):1
H NMR (300 MHz, CHCl3
) δ 6.87 (d,J
= 7.6 Hz, 1H), 6.51 (ddd,J
= 7.5, 1.7, 0.8 Hz, 1H), 6.47 (d,J
= 1.6 Hz, 1H), 4.36 (q,J
= 6.7 Hz, 1H), 4.22 (s, 2H), 3.26 (s, 3H), 2.24 (d,J
= 0.8 Hz, 3H), 1.56 - 1.46 (m, 3H);13
C NMR (126 MHz, CDCl3
) δ 144.87, 128.61, 122.59, 118.56, 116.95, 80.41, 77.31, 77.06, 76.81, 55.93, 21.09, 20.01。實施例23 :1-( 甲氧基甲基)-4- 甲基-2- 硝苯(C46) 之製備
在0℃下以小份方式,將氫化鈉(60%油浸,0.217g,5.42 mmol)添加至配於四氫呋喃(20 mL)之(4-甲基-2-硝基苯基)甲醇(0.823g,4.92 mmol)。立即觀察到氣體散展。反應混合物攪拌歷時30分鐘,然後添加碘甲烷(0.460 mL,7.39 mmol)。使反應混合物緩慢地加溫至室溫過夜。反應係以甲醇來驟冷,以及添加水及二氯甲烷。有機層係通經相分離器予以過濾並濃縮,以提供如橘色蠟之標題化合物(1.10g,100%):1
H NMR (400 MHz, CDCl3
) δ 7.88 (t,J
= 1.2 Hz, 1H), 7.63 (d,J
= 7.9 Hz, 1H), 7.49 - 7.41 (m, 1H), 4.80 (s, 2H), 3.48 (s, 3H), 2.43 (s, 3H);13
C NMR (126 MHz, CDCl3
) δ 156.37, 138.33, 134.42, 132.03, 128.47, 124.97, 71.07, 58.87, 20.80;EIMSm/z
180 ([M]+
)。
瞭解到一些試劑及反應條件與某些式1之分子或某些式1之分子製備中使用的某些分子內存在的某些官能性,可能是不相容的。在此等情況中,可能必需使用文獻中廣泛報導及熟習此項技術者所熟知的標準保護及去保護協定。此外,在一些情況中,可能必需執行本文中未述及之進一步例行的合成步驟,來完成所欲分子的合成。熟習此項技術者也會瞭解到,可以透過以不同於所述的順序來執行一些合成途徑的步驟,來完成所欲分子的合成。熟習此項技術者也會瞭解到,於所欲分子上執行標準的官能基相互轉變或是取代反應以導入或修飾取代基是可能的。生物 分析法
本文內含括以下對於甜菜夜蛾(Beet Armyworm) (甜菜夜蛾(Spodoptera exigua
)、甘藍銀紋夜蛾(Cabbage Looper) (粉紋夜蛾(Trichoplusia ni
),以及對黃熱病蚊(埃及斑蚊(Aedes aegypti
)的生物分析,因為其等造成損失。再者,甜菜夜蛾及甘藍銀紋夜蛾為範大廣泛的嚼食性害蟲之兩種良好的指標性物種。此外,碧桃蚜蟲(Green Peach Aphid)為範大廣泛的取食汁液害蟲之良好的指標性物種。和黃熱病蚊一起共四種指標性物種的結果顯示出,式1的分子於控制節肢動物門、軟體動物門,及圓形動物門的害蟲方面之廣泛用途(Drewes等人)。實施例A :對甜菜夜蛾(Beet Armyworm) ( 甜菜夜蛾 (Spodoptera exigua
) ,LAPHEG) (“BAW”) 與 甘藍銀紋夜蛾(Cabbage Looper) ( 粉紋夜蛾(Trichoplusia ni) ,TRIPNI) (“CL”) 之生物 分析
甜菜夜蛾對於紫花苜蓿、蘆筍、甜菜(beets)、柑橘、玉米、棉花、洋蔥、豌豆、胡椒、馬鈴薯、大豆、甜菜(sugar beets)、向日葵、菸草及番茄以及其他作物而言,為經濟上嚴重關切的害蟲。其原產於東南亞但是現在於非洲、澳洲、日本、北美及南歐可找到。幼蟲可以大規模取食,造成破壞性極大的作物損失。已知其對數種某些殺蟲劑有抗藥性。
甘藍銀紋夜蛾為全世界都可發現的嚴重害蟲。它會攻擊紫花苜蓿、豆類、甜菜(beets)、青花菜、甘藍、高麗菜、哈密瓜、花椰菜、芹菜、羽衣甘藍(collards)、棉花、黃瓜、茄子、甘藍(kale)、萵苣、甜瓜、芥菜、洋芹、豌豆、胡椒、馬鈴薯、大豆、菠菜、南瓜、番茄、蕪青(turnip)及西瓜,以及其他作物。此物種對於植物非常具破壞性,由於它貪婪的胃口。幼蟲每日會吃掉它們體重三倍的食物。取食處會明顯出現大量黏稠、濕潤之糞便,此會促成較高的疾病壓力,藉此對該處的植物造成繼發性的問題。已知其對數種某些殺蟲劑有抗藥性。
因此,基於上述因素,此等害蟲之控制係重要的。而且,控制此等已知為嚼食性害蟲之害蟲(BAW及CL)之分子,可用於控制嚼食植物之其他害蟲。
本文件中揭示之某些分子係使用下列實施例中所述之程序,來測試其對抗BAW與CL之能力。有關結果之報導,使用“BAW & CL 分級表
” (參見表格部分)。對 BAW 進行之生物分析
對BAW之生物分析係使用128孔之食物盤分析進行。將一至五隻第二齡期之BAW幼蟲置於食物盤之每一孔(3毫升),此食物盤已事先填充1毫升之人工食物,已施加50 μg/cm2
之測試分子(溶於50 μL之90:10丙酮-水之混合物)(至八個孔之每一者),之後讓其乾燥。盤係以一透明自黏性覆蓋物覆蓋,開孔以允許氣體交換,且於25℃,14:10亮-暗下保持五至七天。記錄每一孔之幼蟲死亡率百分比;接著將八個孔中之活性求平均值。結果在標題為「表 ABC : 生物分析 結果
」(參見表格部分)之表中示出。對 CL 進行之生物分析
對CL之生物分析係使用128孔之食物盤分析進行。將一至五隻第二齡期之CL幼蟲置於食物盤之每一孔(3毫升),此食物盤已事先填充1毫升之人工食物,已施加50 μg/cm2
之測試分子(溶於50 μL之90:10丙酮-水之混合物)(至八個孔之每一者),之後讓其乾燥。盤係以一透明自黏性覆蓋物覆蓋,開孔以允許氣體交換,且於25 ℃,14:10亮-暗下保持五至七天。記錄每一孔之幼蟲死亡率百分比;接著將八個孔中之活性求平均值。結果在標題為「表 ABC : 生物分析 結果
」(參見表格部分)之表中示出。實施例B :對黃熱病蚊( 埃及斑蚊(Aedes aegypti , AEDSAE) (“YFM”))) 進行 之 生物分析 .
YFM喜歡在白天叮咬人類,且最常在人類居住處或附近被發現。YFM為傳播數種疾病之媒介。YFM為一種可傳播登革熱與黃熱病毒之蚊子。黃熱病是第二危險之蚊子傳播疾病,僅次於瘧疾。黃熱病為急性病毒出血性疾病,且未接受治療之嚴重病患至多有高達50%會死於黃熱病。預計每年全球會有200,000個黃熱病病例,導致30,000人死亡。登革熱是一種討厭的病毒性疾病;由於其會產生劇烈疼痛,所以有時稱為"關節痛熱"或"心臟痛熱"。登革熱每年造成約20,000人死亡。因此,上述控制此害蟲之因子相當重要。此外,控制此已知為吸食性害蟲的害蟲(YFM)之分子,可用於控制患病的人類與動物體內其他的吸食性害蟲。
本文件中揭示之某些分子係使用下列段落中所述之程序,來測試其對抗YFM之能力。有關結果之報導,使用“YFM 分級表
”(參見表格部分)。
使用含有400 µg分子,其溶於100 µL二甲基亞碸(DMSO)中(相當於4000 ppm溶液)之主盤。組合的分子之主盤每孔含有15 µL。在此盤中,每孔加入135 µL之90:10水/丙酮混合物。機器人(Biomek® NXP Laboratory Automation Workstation)設定程式由主盤中分配15 µL吸取液至空的96-孔淺盤中(“子”盤)。每主盤產生6 reps(“子”盤)。產生之“子”盤之後立即經YFM幼蟲感染。
在該盤處理前一日,將蚊子卵置於含有肝粉末之Millipore水中,開始孵化(4 g.至400 mL中)。在使用機器人製備“子”盤後,以220 µL肝粉末/蚊幼蟲混合物(約1天大的幼蟲)感染子盤。該盤經蚊幼蟲感染後,使用非揮發性的上蓋覆蓋該盤,以降低乾燥情況。盤於室溫下維持3天,之後分級。3天後,觀察每一孔並依據死亡率評分。結果在標題為「表 ABC : 生物分析 結果
」(參見表格部分)之表中示出。農業上可接受的酸加成鹽類、鹽類衍生物、溶劑合物、酯類衍生物、多形體、同位素與放射性核種
式1分子可以調配成農業上可接受的酸加成鹽類。作為非限制性例子,胺官能基可與氫氯酸、氫溴酸、硫酸、磷酸、乙酸、苯甲酸、檸檬酸、丙二酸、水楊酸、蘋果酸、福馬酸、草酸、琥珀酸、酒石酸、乳酸、葡萄糖酸、抗壞血酸、馬來酸、天冬門酸、苯磺酸、甲磺酸、乙磺酸、羥甲磺酸,及羥乙磺酸形成鹽類。另外,作為非限制性例子,酸官能基可形成鹽類,包括自鹼金屬或鹼土金屬衍生及自氨及胺衍生者。陽離子之較佳例子可包括鈉、鉀,及鎂。
式1分子可以調配成鹽衍生物。作為非限制性例子,鹽衍生物可藉由使游離鹼與足夠量之所欲酸接觸產生鹽而製備。游離鹼可藉由將此鹽以適合的稀釋鹼水溶液處理而再生,鹼水溶液諸如稀釋的氫氧化鈉、碳酸鉀、氨,及碳酸氫鈉水溶液。作為許多案例中之範例,一種殺蟲劑如2,4-D,可藉由將其轉化為其二甲基胺鹽類而更具水溶性。
式1分子可以與溶劑調配成穩定的錯合物,從而使該錯合物在移除未錯合的溶劑後仍保持完整。此等錯合物通常被稱為「溶劑合物」。然而,較佳以水作為溶劑形成穩定的水合物。
含酸官能之式1分子可製備為酯類衍生物。這些酯類衍生物繼而可以類似於本文件揭示之分子的應用方式應用。
式1分子可製備為各種結晶性多形體。多形性於發展農用化學品上係重要的,因為相同分子之不同結晶多形體或結構的具有的不同的物理性質及生物效能。
式1分子可以用不同的同位素來製造。尤其重要的為具有2
H(亦稱為氘)或是3H(亦稱為氚)取代1
H之分子。式1分子可以用不同的放射性核種來製造。尤其重要的為具有14
C(亦稱為放射性碳)之分子。具有氘、氚、或是14
C取代之式1分子可以使用於生物研究,能夠追蹤化學及物理製程及半衰期研究,以及MoA研究。組合
在本發明之另一個具體例中,式1分子可與一種或多種活性成分組合使用(諸如,呈組成混合物之形式,或同時或依序施用)。
在本發明之另一個具體例中,式1分子可與一種或多種活性成分組合使用(諸如,呈組成混合物之形式,或同時或依序施用),該活性成分每一者皆具有與式1分子之作用模式(“MoA”)相同、類似但是更可能為-相異之MoA。
在另一個具體例中,式1分子可與一種或多種分子組合使用(諸如,呈組成混合物之形式,或同時或依序施用),該一種或多種分子具有殺蜱蟎、殺藻、殺卵、殺菌、殺真菌、除草、殺昆蟲、殺軟體動物、殺線蟲、滅鼠及/或殺病毒特性。
在另一個具體例中,式1分子可與一種或多種分子組合使用(諸如,呈組成混合物之形式,或同時或依序施用),該一種或多種分子為拒食劑、驅鳥劑、化學絕育劑、除草劑安全劑、誘蟲劑、驅蟲劑、驅哺乳動物劑、交配干擾劑、植物活化劑、植物生長調節劑及/或協力劑。
在另一個具體例中,式1分子可與一種或多種生物性殺蟲劑組合使用(諸如,呈組成混合物之形式,或同時或依序施用)。
在另一個具體例中,式1分子與活性成分之殺蟲組成物組合可以廣大變化範圍之重量比使用。舉例而言,二組分混合物,式1分子比活性成分之重量比,可以使用表B中的重量比。然而,一般而言,重量比小於約10:1至約1:10為較佳的。有時使用包含一種三、四、五、六、七、或更多組分的混合物亦為較佳的,該混合物包含式1分子及額外的二或三種活性成分。
式1分子與一種活性成分之重量比可以描述為X:Y
;其中X
為式1之分子的重量份且Y
為活性成分之重量份。X
重量份之數值範圍為0 <X
≤ 100且Y
重量份之數值範圍為0 <Y
≤ 100,以及通過圖表顯示於表C
中。作為非限制性實例,式1之分子與一種活性成分之重量比範圍可以為20:1。
式1分子與一種活性成分之重量比範圍可以描述為X1
:Y1
至X2
:Y2
,其中X
及Y
如上文所定義。
在一個具體例中,重量比範圍可為X1
:Y1
至X2
:Y2
,其中X1
>Y1
且X2
<Y2
。作為非限制性實例,式1分子與一種活性成分之重量比範圍可在約3:1與約1:3之間,含括端點。
在另一個具體例中,重量比範圍可為X1
:Y1
至X2
:Y2
,其中X1
>Y1
且X2
>Y2
。作為非限制性實例,式1分子與一種活性成分之重量比範圍可在約15:1與約3:1之間,含括端點。
在另一個具體例中,重量比範圍可為X1
:Y1
至X2
:Y2
,其中X1
<Y1
且X2
<Y2
。作為非限制性實例,式1分子與一種活性成分之重量比範圍可在約1:3與約1:20之間,含括端點。
如表B及C中所呈現,式1分子與一種活性成分之某些重量比,可以想見為協同性的。調配物
殺蟲劑常常不適合以單純形式使用。通常需要添加其他物質,以便該殺蟲劑能以允許方便施用、處理、輸送、儲存及最大殺蟲劑活性之所需濃度及適宜形式使用。因此,殺蟲劑係調配成例如餌劑、濃縮乳劑、粉劑、可乳化性濃縮液、燻蒸劑、膠劑、粒劑、微膠囊、種子處理劑、懸浮濃縮劑、懸乳劑(suspoemulsion)、錠劑、水溶性液劑、水分散性粒劑或是乾燥可流動劑、可濕性粉劑及超低體積溶液。
殺蟲劑最經常以由此等殺蟲劑的濃縮調配物所製備之含水懸浮液或乳劑的形式來施用。此等水溶性、水可懸浮或可乳化調配物為固體,通常稱為可濕性粉末、水可分散顆粒,或者為液體,通常稱為可乳化濃縮物或水性懸浮液。可濕性粉末,其可經壓緊以形成水可分散顆粒,包含殺蟲劑、載劑及界面活性劑之緊密混合物。殺蟲劑之濃度通常為約10重量%至約90重量%。載劑通常選自鎂鋁海泡石黏土(attapulgite clay)、蒙脫石黏土(montmorillonite clay)、矽藻土(diatomaceous earth)或純化矽酸鹽。包含約0.5%至約10%的可濕性粉劑之有效界面活性劑,見於磺酸化木質素、縮合萘磺酸鹽、萘磺酸鹽、烷基苯磺酸鹽、烷基硫酸鹽以及非離子性界面活性劑,諸如烷基苯酚的環氧乙烷加成物。
殺蟲劑之可乳化濃縮物包含溶解於載劑中合宜濃度之殺蟲劑,諸如每公升液體約50至約500公克,該載劑為水可混溶的溶劑或水不混溶的有機溶劑及乳化劑之混合物。適用的有機溶劑包括芳族類,尤其是二甲苯類與石油分餾物,尤其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,諸如包括松香衍生物在內之萜烯溶劑、脂族酮類諸如環己酮,及複合醇類諸如2-乙氧基乙醇。用於可乳化性濃縮液之適宜乳化劑係選自習用的陰離子性及非離子性界面活性劑。
水性懸浮液包含以在約5重量%至約50重量%範圍內之濃度,分散在水性載劑中之非水溶性殺蟲劑的懸浮液。懸浮液藉由以下方式製備:精細研磨殺蟲劑並將其劇烈混合至載劑中,該載劑包含水及界面活性劑。亦可添加諸如無機鹽及合成膠或天然膠之成分,從而增加水性載劑之密度及黏度。通常最有效的為藉由以儀器,諸如砂磨機、球磨機或活塞型均質器中製備水性混合物並對其進行均質化來同時研磨及混合殺蟲劑。懸浮液內的殺蟲劑可以予以微膠囊化於塑膠聚合物中。
油分散液(OD)包含以在約2重量%至約50重量%範圍內之濃度,微細地分散在有機溶劑及乳化劑之混合物中之非有機溶劑溶性殺蟲劑的懸浮液。一種或多種殺蟲劑可以溶解於有機溶劑中。適用的有機溶劑包括芳族類,尤其是二甲苯類與石油分餾物,尤其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,包括蔬菜油、種子油及植物油與種子油之酯類。用於油分散液之適宜乳化劑係選自習用的陰離子性及非離子性界面活性劑。油分散液調配物內添加增稠劑或膠凝劑,以改變液體之流變學或流動性質及防止分散粒子或液滴之分離及沈降。
殺蟲劑亦可以顆粒組成物之形式來施用,該等顆粒組成物尤其適用於施用至土壤中。顆粒組成物通常含有分散在載劑中之約0.5重量%至約10重量%之殺蟲劑,該載劑包含黏土或相似物質。該等組成物通常藉由以下方式製備:將該殺蟲劑溶解在適合之溶劑中並將其施用至顆粒載劑上,該顆粒載劑已經預成形為適當粒徑,在約0.5mm至約3mm範圍內。此等組成物亦可藉由以下方式調配:將該載劑及分子製成麵團狀或糊狀,然後壓碎並乾燥,從而得到所需顆粒粒徑。另一種顆粒為水可乳化顆粒(EG)。其為由以傳統的活性成分之水包油乳液方式施用之顆粒組成的調配物,於崩散或溶解於水中之後,溶解或稀釋於有機溶劑內。水可乳化顆粒含有一種或數種溶解或稀釋於合適的有機溶劑內之活性成分,其被聚合殼體或一些其他類型的可溶性或不溶性基質吸收。
含有殺蟲劑之塵劑係藉由以下方式製備:將呈粉末形式之殺蟲劑與適合之粉塵狀農業載劑,諸如高嶺黏土、經研磨火山岩及其類似載劑,緊密混合。塵劑可適當地含有約1%至約10%的殺蟲劑。塵劑可以施用作為拌種(seed dressing)或以粉塵鼓風機施用於葉片上。
同樣可行的以配於適當有機溶劑中的溶液形式施用之殺蟲劑,該有機溶劑通常為石油諸如噴霧油,該有機溶劑廣泛用於農業化學。
殺蟲劑亦可以氣溶膠組成物之形式來施用。在此等組成物中,將殺蟲劑溶解或分散在載劑中,該載劑為產生壓力之推進劑混合物。將氣溶膠組成物包裝在容器中,該混合物經由霧化閥而自該容器噴散。
當將殺蟲劑與食物或引誘劑或兩者混合時,形成殺蟲劑誘餌。當害蟲吃掉誘餌時,其等亦攝入殺蟲劑。誘餌可呈顆粒、凝膠、可流動粉末、液體或固體形式。誘餌可用於害蟲藏身處。
薰蒸劑為具有相對較高蒸氣壓之殺蟲劑,且因此可以濃度足以殺死土壤或密封空間中之害蟲的氣體形式存在。薰蒸劑之毒性與其濃度及曝露時間成比例。其等特徵在於具有良好的擴散能力,並藉由滲透至害蟲之呼吸系統中或經由害蟲之表皮吸收而起作用。施用薰蒸劑以便在氣密房間或建築物中或在專門腔室中,對防氣片(gas proof sheet)下之儲藏產品害蟲進行控制。
可藉由將殺蟲劑粒子或小滴懸浮在各種類型之塑膠聚合物中,而將殺蟲劑微膠囊化。藉由改變聚合物之化學性質或藉由改變加工中之因素,可形成各種大小、溶解度、壁厚度及滲透度之微膠囊。此等因素控制其中活性成分之釋放速度,而釋放速度又影響產品之殘留效能、作用速度及氣味。微膠囊可調配為懸浮濃縮劑或是水可分散顆粒。
油溶液濃縮物係藉由將殺蟲劑溶於一溶劑內而製備,該溶劑會將殺蟲劑留置於溶液中。殺蟲劑之油溶液由於溶劑本身具有殺蟲作用及溶解體被之蠟質覆蓋物而增加殺蟲劑的攝取速度,所以通常會提供比其他調配物更快的擊倒及殺死害蟲作用。油溶液之其他優點包括較好的儲藏穩定性、更好的裂縫滲透性及更好的油膩表面黏附性。
另一具體例為一種水包油型乳劑,其中該乳劑包含油性小球,該等油性小球各自提供有層狀液晶塗層,並分散在水相中,其中各油性小球包含至少一種具有農業活性之分子,並個別地塗佈有單層狀或寡層狀之層,該層包含:(1)至少一種非離子性親脂性界面活性劑,(2)至少一種非離子性親水性界面活性劑,及(3)至少一種離子性界面活性劑,其中該等小球具有小於800奈米之平均粒徑。其他調配物組分
一般而言,當式1揭示之分子使用於一調配物中時,此調配物亦可含有其他組分。此等組分包括但不限於(其係ㄧ個非詳盡無遺及非互相排除的清單)濕潤劑、展佈劑、黏著劑、滲透劑、緩衝劑、螯合劑、漂浮降低劑、相容劑、消泡劑、清潔劑及乳化劑。現即說明一些組分。
潤濕劑係ㄧ物質,當添加至一液體時,藉由降低該液體與其展佈表面之間的界面張力而增加該液體的展佈或滲透力。潤濕劑用於農業化學調配物中之兩種主要功能:在處理及製造期間增加粉末在水中之潤濕速率,從而製造可溶性液體之濃縮物或懸浮濃縮物;及在產品與水在噴霧罐中混合期間降低可濕性粉末之潤濕時間,並使水滲透進入水可分散顆粒中的情況改善。用於可濕性粉末、懸浮濃縮物及水可分散顆粒調配物中的潤濕劑之實例為:月桂基硫酸鈉;二辛基磺基丁二酸鈉;烷基酚乙氧化物;及脂族醇乙氧化物。
分散劑為吸附至粒子表面上、有助於保持粒子之分散狀態以及防止粒子重新聚集的物質。將分散劑添加至農業化學調配物中以有助於製造期間之分散及懸浮,並且有助於確保粒子在噴霧罐中重新分散至水中。其廣泛用於可濕性粉末、懸浮濃縮物及水可分散顆粒中。用作分散劑之界面活性劑具有牢固吸附至粒子表面上之能力,並對粒子重新聚集提供電荷或空間障壁。最常用的界面活性劑為陰離子型、非離子型或該等兩種類型之混合物。對於可濕性粉末調配物,最常用分散劑為木質素磺酸鈉。對於懸浮濃縮物而言,使用聚電解質,諸如鈉-萘磺酸鹽-甲醛-濃縮物來得到極好的吸附及穩定。亦使用三苯乙烯基苯酚乙氧化物磷酸酯。非離子物,諸如烷基芳基氧化乙烯濃縮物及EO-PO嵌段共聚物,有時與陰離子物組合起來作為用於懸浮濃縮物之分散劑。近年來,新型式之極高分子量聚合物界面活性劑已開發作為分散劑。此等具有極長之疏水性『主鏈』及大量氧化乙烯鏈,其形成『梳狀』界面活性劑之『齒』。此等高分子量聚合物可對懸浮濃縮物產生極好的長期穩定性,因為疏水性主鏈對粒子表面具有許多錨定點。用於農業化學調配物之分散劑之實例為:木質素磺酸鈉;萘磺酸鈉甲醛濃縮物;三苯乙烯基苯酚-乙氧化物-磷酸-酯;脂族醇乙氧化物;烷基乙氧化物;EO-PO嵌段共聚物;以及接枝共聚物。
乳化劑為使一種液相之液滴於另一液相中之懸浮液穩定之物質。在無乳化劑之情況下,兩種液體會分離成兩個不混溶的液相。最常用的乳化劑摻合物含有具有12個或12個以上環氧乙烷單元之烷基酚或脂族醇,及十二烷基苯磺酸之油溶性鈣鹽。範圍在大約8至大約18的親水親油平衡(「HLB」)值通常會提供良好穩定之乳液。乳液穩定性有時可藉由添加少量EO-PO嵌段共聚物界面活性劑來改進。
增溶劑為在濃度超過臨界微胞濃度時,在水中形成微胞之界面活性劑。接著,微胞能夠溶解(dissolve)或溶解(solubilize)微胞之疏水部分內之水不溶性物質。通常用於溶解作用之界面活性劑類型為非離子型、脫水山梨糖醇單油酸酯、脫水山梨糖醇單油酸酯乙氧化物及油酸甲酯。
界面活性劑有時單獨使用,或與其他添加劑,諸如作為佐劑之礦物油或植物油,一起使用於噴霧罐混合物,以改進殺蟲劑對目標之生物效能。用於生物增強之界面活性劑類型通常視殺蟲劑之性質及作用模式而定。然而,其等通常為非離子物,諸如:烷基乙氧化物;線性脂族醇乙氧化物;以及脂族胺乙氧化物。
農業調配物中的載劑或稀釋劑為添加至殺蟲劑中以得到所需強度產品之物質。載劑通常為具有較高吸收能力之物質,而稀釋劑通常為具有較低吸收能力之物質。載劑及稀釋劑係使用於塵劑、可濕性粉末、顆粒及水可分散顆粒之調配物。
有機溶劑主要用於可乳化濃縮物、水包油乳液、懸乳劑、油分散液及超低體積調配物之調配物,及在較少程度上用於顆粒調配物。有時使用溶劑的混合物。第一主要群組之溶劑為脂族石蠟油,諸如煤油或精製石蠟。第二主要群組(且最常見)包含芳族溶劑,諸如二甲苯及較高分子量之C9及C10芳族溶劑之餾份。當將調配物乳化至水中時,氯化烴係使用作防止殺蟲劑結晶之共溶劑。醇類有時用作共溶劑以增強溶劑功效。其他溶劑可包括植物油、種子油及植物油與種子油之酯類。
增稠劑或膠凝劑主要用於懸浮濃縮物、油分散液、乳液及懸乳劑之調配物,以改變液體之流變學或流動性質及防止分散粒子或液滴分離及沈降。增稠劑、膠凝劑及抗沈降劑通常屬於兩種類別,亦即水不溶性微粒及水溶性聚合物。可使用黏土及二氧化矽來製造懸浮濃縮物及油分散液調配物。此等物質類型之實例包括但不限於,蒙脫石、膨潤土、矽酸鎂鋁及鎂鋁海泡石。配於水基的懸浮濃縮物之水溶性多醣類多年來已用作增稠-膠凝劑。最常用之多醣類型為種子及海藻之天然萃取物或纖維素之合成衍生物。此等類型物質之實例包括但不限於,瓜爾膠;刺槐豆膠;角叉菜膠;海藻酸鹽;甲基纖維素;羧甲基纖維素鈉(SCMC);以及羥乙基纖維素(HEC)。其他類型的抗沈降劑係以改質澱粉、聚丙烯酸酯、聚乙烯醇及聚氧化乙烯為基礎。另一種良好的抗沈降劑為三仙膠。
微生物會導致調配產品之腐敗。因此,使用防腐劑來消除或降低其等之作用。該等試劑之實例包括但不限於:丙酸及其鈉鹽;山梨酸及其鈉或鉀鹽;苯甲酸及其鈉鹽;對羥基苯甲酸鈉鹽;對羥基苯甲酸甲酯;及1,2-苯并異噻唑啉-3-酮(BIT)。
界面活性劑之存在,經常造成水基調配物在製造及經由噴灑槽施用時在混合操作期間起泡。為了減少起泡之傾向,通常在製造階段期間或裝填至瓶中之前添加消泡劑。通常存在有兩種類型的消泡劑,亦即聚矽氧以及非聚矽氧。聚矽氧通常為二甲基聚矽氧烷之水性乳液,而非聚矽氧消泡劑為水不溶性油,諸如辛醇及壬醇,或二氧化矽。在該兩種情況下,消泡劑之功能為自空氣-水界面中替換界面活性劑。
「綠色」製劑(例如佐劑、界面活性劑、溶劑)可降低作物保護調配物之整體環境足跡。綠色試劑為生物可降解的,且通常衍生自天然及/或永續來源,例如植物及動物來源。特定實例為:植物油、種子油及其酯類,以及烷氧基化烷基聚葡糖苷。施用
式1的分子可施用於任何所在地。施用此等分子之特定的所在地包括紫花苜蓿、杏仁、蘋果、大麥、豆類、油菜、玉米、棉花、十字花科植物、花、飼料物種(黑麥草(Rye Grass)、蘇丹草(Sudan Grass)、高牛毛草(Tall Fescue)、肯塔基藍草(Kentucky Blue Grass)及三葉草(Clover))、水果、萵苣、燕麥、油籽作物、橘子、花生、梨、胡椒、馬鈴薯、水稻、高粱、大豆、草莓、甘蔗、甜菜、向日葵、煙草、蕃茄、小麥(舉例而言,硬紅冬麥(Hard Red Winter Wheat)、軟紅冬麥(Soft Red Winter Wheat)、白冬小麥(White Winter Wheat)、硬紅春麥(Hard Red Spring Wheat)及杜蘭春小麥(Durum Spring Wheat)),和其他有價值的作物生長之所在地或其種子待種植之處。
式1的分子亦可施用於植物,如作物生長之處,以及可造成此等植物的商業損失的害蟲水平低(甚至並無實際的存在)之區域。此所在地施用此等分子對於此所在地生長的植物為有利的。此等益處可以包括但不限於:協助植物生長出更好的根系;協助植物更佳地承受壓力生長條件;改進植物健康;改進植物產量(例如增加生物質及/或增加有價值成分之含量);改進植物活力(例如改進植物生長及/或葉子更綠);改進植物品質(例如改進某些成分之含量或組成);以及改進植物對非生物及/或生物脅迫之耐受性。
在栽種各種植物時,式1的化合物可以與硫酸銨一起施用,因這樣可以提供額外的益處。
式1分子可以施用於經基因改造以表現特殊性狀,諸如蘇力菌(Bacillus thuringiensis
) (舉例而言,Cry1Ab、Cry1Ac、Cry1Fa、Cry1A.105、Cry2Ab、Vip3A、mCry3A、Cry3Ab、Cry3Bb、Cry34Ab1/Cry35Ab1),其他殺昆蟲性毒素,或該等表現除草劑耐受性之植物,或是該等具有表現殺昆蟲性毒素、除草劑耐受性、營養強化作用或其他任一有利性狀之「堆疊式」外來基因者之植物上、之中或周圍。
式1分子可施用至待控制害蟲之植物葉子及/或果實部分。此等分子會直接與害蟲接觸,或害蟲於食用植物或吸取汁液或植物其他營養素時,會攝入此等分子。
式1分子亦可施用至土壤,且當以此方式施用時,可控制食用根與莖之害蟲。根可吸收此等分子藉此將其送至植物之葉子部分,以控制地面上部嚼食與汁液取食之害蟲。
可藉由在植物的不同部分施用(例如藉由噴灑一所在地)式1分子,利用殺蟲劑在植物中的系統性移動,而控制位於植物另一部分的害蟲。舉例而言,例如,可藉由滴灌或條施,藉由以例如種植前或種植後之土壤澆灌而處理土壤,或藉由種植前處理植物種子來達成控制食葉昆蟲。
式1的分子可以與誘餌一起施用。一般而言,在誘餌情況下,將誘餌置於地面,白蟻可與誘餌接觸及/或被吸引。亦可將誘餌施用至建築表面(水平、垂直或傾斜表面),該處螞蟻、白蟻、蟑螂與蒼蠅,皆會與誘餌接觸及/或被吸引。
式1分子可囊封在膠囊內、或置放於膠囊表面上。膠囊的大小可在奈米大小(直徑大約100-900奈米)至微米大小(直徑大約10-900微米)範圍內。
式1分子可以施用於害蟲之卵。由於一些害蟲之卵具有抗某些殺蟲劑之獨特能力,故可能需要重複施用此等分子以控制新出現之幼蟲。
式1分子可以施用作為種子處理。可對將發芽之所有類型的種子進行種子處理,包括經遺傳修飾以表現特殊性狀之植物的種子。代表性實例包括對無脊椎動物害蟲,諸如蘇力菌(Bacillus thuringiensis
),表現蛋白毒性或其他殺昆蟲毒素者,表現除草劑耐受性者,諸如「Roundup Ready」種子,或具有表現殺昆蟲毒素、除草劑耐受性、營養增強、耐旱性或任何其他有益特性之「堆疊式」外來基因者。另外,此等使用式1分子之種子處理可進一步增強植物耐嚴苛生長條件的能力更佳。由此產生較健康,較有活力之植物,此在收穫時節可導致更高的產量。一般而言,預期每100,000個種子約1公克至約500公克之此等分子會提供良好的益處,預期每100,000個種子約10公克至約100公克之量會提供更佳的益處,且預期每100,000個種子約25公克至約75公克之量會提供甚至更佳的益處。
式1的分子可與土壤改良領域中的一或多種活性成分一起使用。
式1分子可用於控制獸醫學領域或在非人類動物飼養領域中之內寄生蟲及外寄生蟲。此等分子可以舉例而言藉由,例如錠劑、膠囊、飲料、顆粒形式經口投與,藉由以例如浸泡、噴灑、傾倒、點藥及噴粉形式塗覆皮膚,以及藉由以例如注射劑形式的非經腸投與來施用。
式1分子亦可有利地用於家畜飼養,例如牛、雞、鵝、山羊、豬、綿羊及火雞。其等亦可有利地用於寵物,諸如馬、犬及貓。欲控制之特定害蟲將為會對該等動物造成麻煩之蒼蠅、跳蚤及壁蝨。適合的調配物與飲用水或飼料一起經口投與該等動物。適合的劑量及調配物視物種而定。
式1分子亦可用於控制寄生蟲,尤其是上列動物腸道中的寄生蟲。
式1分子亦可用於人類健康照護之治療方法。此等方法包括但不限於,以例如錠劑、膠囊、飲料、顆粒形式經口投與及藉由皮膚施用。
式1分子亦可施用於侵入性害蟲。全世界之害蟲正遷移至新環境(對於此害蟲而言),且此後在該新環境中變成新的侵入物種。此等分子亦可用於該等新的侵入物種以在該新環境中對其進行控制。
在使用或商業販售殺蟲劑之前,此類殺蟲劑會依據各種政府法規(地方、地區、州、國家和國際),進行漫長的評估過程。大量數據要求由監管機構指定,且必須由產品註冊者或代表產品註冊者之第三方,通常使用與全球資訊網連接之電腦,經由資料生成及提交來處理。之後,這些政府機關會檢視這些數據,若結論判定為安全,便會提供潛在使用者或販售者產品註冊核准證書。此後,在產品註冊通過與支持之地區,此使用者或販售者可使用或販售此殺蟲劑。
如式1之分子可經測試來決定其對抗害蟲之藥效。此外,式1之分子可與另一種活性成分混合以形成一種殺蟲組成物,然後使用習用的測試程序來測試該組成物,以判定其是否為協同性的。再者,可導入作用模式之研究,以決定該分子是否具有與其他殺蟲劑不同之作用模式。之後,此類收集之數據可經由如網際網路傳送至第三方。
因此,根據上述以及表格部分的表格,提供下列額外的細節(D)。1D.
一種具下式之分子 式1
其中:(A) Ar1
係選自於下列所構成的群組:呋喃基、苯基、嗒基、吡啶基、嘧啶基,或是噻吩基, 其中每個呋喃基、苯基、嗒基、吡啶基、嘧啶基,及噻吩基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 較佳地,Ar1
為(1a) (1a)
, 其中,R1
、R2 、R3 、R4
及R5
各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 更佳地,Ar1
為(1a) (1a)
, 其中,R1
、R2 、R3 、R4
及R5
各自獨立地選自於下列所構成的群組:H及(C1
-C4
)鹵烷氧基, 還更佳地,Ar1
為(1a) (1a)
, 其中,R1
、R2 、R3 、R4
及R5
各自獨立地選自於下列所構成的群組:H3
及OCF3
;(B) Het
為5或6員、飽和或不飽和之雜環,含有獨立地選自於氮、硫或氧之一或多個雜原子,以及其中Ar1
與L1
互相不為鄰位,但可為間位或對位,例如就五員環而言,其等為1,3,且就六員環而言,其等為1,3或1,4, 其中每個雜環可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、側氧、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 較佳地,Het
為(1b) (1b)
, 其中R6
可以選擇性地以選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、側氧、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 更佳地,Het
為(1b) (1b)
, 其中,R6
為H;(C) L1
係選自於下列所構成的群組:N(Rx
)-(C1
-C4
)烷基、N(Rx
)-(C3
-C8
)環烷基、N(Rx
)-(C2
-C6
)烯基、N(Rx
)-(C2
-C6
)炔基、N(Rx
)-S(O)n
-(C1
-C4
)烷基、(C1
-C4
)烷基-N(Rx
)-(C1
-C4
)烷基、(C1
-C4
)烷基-N(Rx
)-(C1
-C4
)烷基、(C1
-C4
)烷基-N(Rx
)、(C3
-C8
)環烷基-N(Rx
)、(C2
-C6
)炔基-N(Rx
)、(C1
-C4
)烷基-S(O)n
-N(Rx
)、C(O)-N(Rx
)、C(S)-N(Rx
)、N(Rx
)-C(O)、N(Rx
)-C(S)、C(O)-N(Rx
)-(C1
-C4
)烷基、C(S)-N(Rx
)-(C1
-C4
)烷基、(C1
-C4
)烷基-N(Rx
)-C(O),以及(C1
-C4
)烷基-N(Rx
)-C(S), 其中每個烷基、環烷基、烯基及炔基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基,以及(C2
-C6
)炔基; 較佳地,L1
係選自於下列所構成的群組 (1c)
, (1d)
, (1e)
,以及 (1f)
, 其中:(1) Qx
係各自獨立地選自於O及S所構成的群組,以及(2) R7
、R8 、R9
及R10
係各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基,以及(C2
-C6
)炔基; 更佳地,L1
係選自於下列所構成的群組 (1c)
, (1d)
, (1e)
,以及 (1f)
, 其中:(1) Qx
為O,以及(2) R7
、R8 、R9
及R10
各自獨立地選自於H及(C1
-C4
)烷基所構成的群組; 還更佳地,L1
係選自於下列所構成的群組 (1c)
, (1d)
, (1e)
,以及 (1f)
, 其中:(1) Qx
為O,以及(2) R7
、R8 、R9
及R10
各自獨立地選自於H及CH3
所構成的群組;(D) Ar2
係選自於下列所構成的群組:呋喃基、苯基、嗒基、吡啶基、嘧啶基,或是噻吩基, 其中每個呋喃基、苯基、嗒基、吡啶基、嘧啶基,及噻吩基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(=O)O-(C1
-C4
)烷基、苯基,以及苯氧基; 較佳地,Ar2
為(1g) (1g)
, 其中:(1) X1
係選自於N及CR13
所構成的群組,以及(2)R11
、R12 、R13 、
及R14
各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(=O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 更佳地,Ar2
為(1g) (1g)
, 其中:(1) X1
係選自於N及CR13
所構成的群組,以及(2)R11
、R12 、R13
及R14
各自獨立地選自於下列所構成的群組:H、F以及Cl;(E) R15
係選自於下列所構成的群組:H、(C1
-C4
)烷基、(C3
-C8
)環烷基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、C(O)-NRx
Ry
、C(O)-苯基、(C1
-C4
)烷基-NRx
Ry
、C(O)O-(C1
-C4
)烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基, 其中每個烷基、環烷基、烯基、炔基,及苯基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、側氧、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 較佳地,R15
為H;(F) Q1
係選自於O及S所構成的群組,較佳Q1
為O;(G)Q2
係選自於O及S所構成的群組,較佳Q2
為S;(H) R16
係選自於下列所構成的群組:(K)
、H、(C1
-C4
)烷基、(C3
-C8
)環烷基、(C2
-C6
)烯基、(C2
-C6
)炔基、C(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、(C1
-C4
)烷基苯基、(C1
-C4
)烷基-O-苯基、C(O)-(Het-1)、(Het-1)、(C1
-C4
)烷基-(Het-1)、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-NRx
Ry
、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-(Het-1)、(C1
-C4
)烷基-C(O)-(Het-1)、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基(NRx
Ry
)-C(O)OH、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-NRx
Ry
、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-N(Rx
)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基(N(Rx
)-C(O)O-(C1
-C4
)烷基)-C(O)OH、(C1
-C4
)烷基-C(O)-(Het-1)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C3
-C8
)環烷基、(C1
-C4
)烷基-OC(O)-(Het-1)、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基-N(Rx
)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-NRx
Ry
、(C1
-C4
)烷基-S(O)n
-(Het-1),以及(C1
-C4
)烷基-O-(Het-1), 其中每個烷基、環烷基、烯基、炔基、苯基,及(Het-1)可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)OH、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基)、苯基、苯氧基、Si((C1
-C4
)烷基)3
、S(O)n
-NRx
Ry
,以及(Het-1), 較佳地,R16
為(K)
;(I) R17
係選自於下列所構成的群組:(K)
、H、(C1
-C4
)烷基、(C3
-C8
)環烷基、(C2
-C6
)烯基、(C2
-C6
)炔基、C(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、(C1
-C4
)烷基苯基、(C1
-C4
)烷基-O-苯基、C(O)-(Het-1)、(Het-1)、(C1
-C4
)烷基-(Het-1)、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-NRx
Ry
、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-(Het-1)、(C1
-C4
)烷基-C(O)-(Het-1)、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基(NRx
Ry
)-C(O)OH、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-NRx
Ry
、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基-N(Rx
)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-C(O)-N(Rx
)(C1
-C4
)烷基(N(Rx
)-C(O)O-(C1
-C4
)烷基)-C(O)OH、(C1
-C4
)烷基-C(O)-(Het-1)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C3
-C8
)環烷基、(C1
-C4
)烷基-OC(O)-(Het-1)、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基-N(Rx
)-C(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-NRx
Ry
、(C1
-C4
)烷基-S(O)n
-(Het-1),以及(C1
-C4
)烷基-O-(Het-1), 其中每個烷基、環烷基、烯基、炔基、苯基,及(Het-1)可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)OH、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基、苯氧基、Si((C1
-C4
)烷基)3
、S(O)n
-NRx
Ry
,以及(Het-1), 較佳地,R17
為(K)
;(J) L2
係選自於下列所構成的群組:(C3
-C8
)環烷基、苯基、(C1
-C4
)烷基苯基、(C1
-C4
)烷基-O-苯基、(C2
-C6
)烯基-O-苯基、(Het-1)、(C1
-C4
)烷基-(Het-1),以及(C1
-C4
)烷基-O-(Het-1), 其中每個烷基、環烷基、烯基、苯基,及(Het-1)可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C1
-C4
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、O-(C1
-C4
)烷基、S-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基、苯氧基,以及(Het-1), 其中每個烷基、環烷基、烯基、苯基,及(Het-1)取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C1
-C4
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、O-(C1
-C4
)烷基、S-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基、苯氧基,以及(Het-1), 較佳地,L2
係(1h) (1h)
, 其中R20
、R21 、R22 、R23
及R24
各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C1
-C4
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、O-(C1
-C4
)烷基、S-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基、苯氧基,以及(Het-1), 其中每個烷基、環烷基、烯基、苯基,及(Het-1)取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、NRx
Ry
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C1
-C4
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、O-(C1
-C4
)烷基、S-(C1
-C4
)烷基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基、苯氧基,以及(Het-1), 更佳地,L2
係(1h) (1h)
, 其中,R20
、R21 、R22 、R23
及R24
各自獨立地選自於下列所構成的群組:H、(C1
-C4
)烷基,以及(C1
-C4
)烷基-O-(C1
-C4
)烷基;以及 還更佳地,L2
係(1h) (1h)
, 其中,R20
、R21 、R22 、R23
及R24
各自獨立地選自於下列所構成的群組:H、CH3
、CH2
CH2
CH3
、CH(CH3
)2
、CH2
OCH3
,及CH(CH3
)OCH3
;以及(K) R16
及R17
與Cx
(Q2
)(Nx
)
一起形成一個4-至7-員飽和或不飽和之雜環,其可以進一步含有選自於氮、硫或氧所構成的群組之一個或更多個雜原子, 其中每個雜環可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:側氧、R18
及R19
, 其中R18
及R19
係各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2
、側氧、硫酮基、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及(Het-1), 較佳地,R16
及R17
與Cx
(Q2
)(Nx
)
一起,係(1i) (1i)
, 其中R18
及R19
係各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2
、側氧、硫酮基、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及(Het-1), 更佳地,R16
及R17
與Cx
(Q2
)(Nx
)
一起,係(1i) (1i)
, 其中,R18
及R19
各自獨立地為H;(L) Rx
及Ry
係各自獨立地選自於下列所構成的群組:H、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)-(C1
-C4
)烷基、(C1
-C4
)烷基-OC(O)O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基,以及苯基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基,及苯基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)H、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及(Het-1);(M) (Het-1)
為5或6員、飽和或不飽和之雜環,含有獨立地選自於氮、硫或氧所構成的群組之一或多個雜原子, 其中每個雜環可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、側氧、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基,及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2
、(C1
-C4
)烷基、(C1
-C4
)鹵烷基、(C3
-C8
)環烷基、(C1
-C4
)烷氧基、(C1
-C4
)鹵烷氧基、(C2
-C6
)烯基、(C2
-C6
)炔基、S(O)n
-(C1
-C4
)烷基、S(O)n
-(C1
-C4
)鹵烷基、OSO2
-(C1
-C4
)烷基、OSO2
-(C1
-C4
)鹵烷基、C(O)-NRx
Ry
、(C1
-C4
)烷基-NRx
Ry
、C(O)-(C1
-C4
)烷基、C(O)O-(C1
-C4
)烷基、C(O)-(C1
-C4
)鹵烷基、C(O)O-(C1
-C4
)鹵烷基、C(O)-(C3
-C8
)環烷基、C(O)O-(C3
-C8
)環烷基、C(O)-(C2
-C6
)烯基、C(O)O-(C2
-C6
)烯基、(C1
-C4
)烷基-O-(C1
-C4
)烷基、(C1
-C4
)烷基-S(O)n
-(C1
-C4
)烷基、C(O)-(C1
-C4
)烷基-C(O)O-(C1
-C4
)烷基、苯基,以及苯氧基;(N) n
每一者係獨立地為0、1或2;以及式1的分子之N-氧化物、農業上可接受的酸加成鹽類、鹽類衍生物、溶劑合物、酯類衍生物、結晶性多形體、同位素、解析的立體異構物,以及互變異構物。2D.
如1D
之分子,其中(A) Ar1
為(1a) (1a)
, 其中,R1
、R2 、R3 、R4
及R5
各自獨立地選自於下列所構成的群組:H及(C1
-C4
)鹵烷氧基,(B) Het
為(1b) (1b)
, 其中,R6
為H;(C) L1
係選自於下列所構成的群組 (1c)
, (1d) , (1e)
,及 (1f) ,
其中:(1) Qx
為O,以及(2) R7
、R8 、R9
及R10
各自獨立地選自於H及(C1
-C4
)烷基所構成的群組;(D) Ar2
為(1g) (1g)
, 其中:(1) X1
係選自於N及CR13
所構成的群組,以及(2)R11
、R12 、R13
及R14
各自獨立地選自於下列所構成的群組:H、F以及Cl;(E)R15
為H;(F) Q1
為O;(G)Q2
為S;(H)R16
為(K)
;(I)R17
為(K)
;(J) L2
係(1h) (1h)
, 其中,R20
、R21 、R22 、R23
及R24
各自獨立地選自於下列所構成的群組:H、(C1
-C4
)烷基,以及(C1
-C4
)烷基-O-(C1
-C4
)烷基;以及(K) R16
及R17
與Cx
(Q2
)(Nx
)
一起,係(1i) (1i)
, 其中,R18
及R19
各自獨立地為H。3D.
如1D或2D之分子,其中(A) Ar1
為(1a) (1a)
, 其中,R1
、R2 、R3 、R4
及R5
各自獨立地選自於下列所構成的群組:H3
及OCF3
;(B) Het
為(1b) (1b)
, 其中,R6
為H;(C) L1
係選自於下列所構成的群組 (1c)
, (1d) , (1e)
,及 (1f) ,
其中:(1) Qx
為O,以及(2) R7
、R8 、R9
及R10
各自獨立地選自於H及CH3
所構成的群組;(D) Ar2
為(1g) (1g)
, 其中:(1) X1
係選自於N及CR13
所構成的群組,以及(2)R11
、R12 、R13
及R14
各自獨立地選自於下列所構成的群組:H、F以及Cl;(E)R15
為H;(F) Q1
為O;(G)Q2
為S;(H)R16
為(K)
;(I)R17
為(K)
;(J) L2
係(1h) (1h)
, 其中,R20
、R21 、R22 、R23
及R24
各自獨立地選自於下列所構成的群組:H、CH3
、CH2
CH2
CH3
、CH(CH3
)2
、CH2
OCH3
,及CH(CH3
)OCH3
;以及(K) R16
及R17
與Cx
(Q2
)(Nx
)
一起,係(1i) (1i)
, 其中,R18
及R19
各自獨立地為H。4D.
如1D、2D或3D中任一者之分子,其中該分子為 5D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含一活性成分。6D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含選自於下列之一種活性成分:殺蜱蟎劑、除藻劑、拒食劑、殺鳥劑(avicide)、殺菌劑、驅鳥劑、化學絕育劑、殺真菌劑、除草劑安全劑、除草劑、誘蟲劑、驅蟲劑、殺昆蟲劑、驅哺乳動物劑、交配干擾劑、殺蟎劑、殺線蟲劑、植物活化劑、植物生長調節劑、滅鼠劑、協力劑,以及殺病毒劑。7D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含選自於AIGA
之活性成分。8D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含AI–1
。9D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含AI–2
。10D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含羅提蘭 (Lotilaner)
。11D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含選自於表 A
之分子。12D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含選自於AIGA–2
之活性成分。13D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含陶斯松(chlorpyrifos)。14D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含六伏隆(hexaflumuron)。15D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含滅芬諾(methoxyfenozide)。16D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含多氟脲(noviflumuron)。17D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含賜諾特(spinetoram)。18D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含賜諾殺(spinosad)。19D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含氟啶蟲胺腈(sulfoxaflor)。20D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含選自於AIGA–2
之活性成分。21D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含亞醌蟎(acequinocyl)。22D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含亞滅培(acetamiprid)。23D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含乙醯蟲腈(acetoprole)。24D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含阿維菌素(avermectin)。25D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含谷速松(azinphos-methyl)。26D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含必芬蟎(bifenazate)。27D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含畢芬寧(bifenthrin)。28D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含胺甲(carbaryl)。29D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含加保扶(carbofuran)。30D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含克凡派(chlorfenapyr)。31D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含克福隆(chlorfluazuron)。32D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含可芬諾(chromafenozide)。33D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含可尼丁(clothianidin)。34D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含賽扶寧(cyfluthrin)。35D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含賽滅寧(cypermethrin)。36D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含第滅寧(deltamethrin)。37D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含汰芬隆(diafenthiuron)。38D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含因滅汀苯甲酸鹽(emamectin benzoate)。39D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含安殺番(endosulfan)。40D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含益化利(esfenvalerate)。41D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含乙蟲腈(ethiprole)。42D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含依殺蟎(etoxazole)。43D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含芬普尼(fipronil)。44D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含氟尼胺(flonicamid)。45D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含嘧蟎酯(fluacrypyrim)。46D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含γ-賽洛寧(gamma
-cyhalothrin)。47D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含合芬隆(halofenozide)。48D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含因得克(indoxacarb)。49D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含λ-賽洛寧(lambda
-cyhalothrin)。50D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含祿芬隆(lufenuron)。51D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含馬拉松(malathion)。52D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含納乃得(methomyl)。53D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含諾伐隆(novaluron)。54D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含百滅寧(permethrin)。55D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含啶蟲丙醚(pyridalyl)。56D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含畢汰芬(pyrimidifen)。57D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含賜派芬(spirodiclofen)。58D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含得芬諾(tebufenozide)。59D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含賽果培(thiacloprid)。60D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含賽速安(thiamethoxam)。61D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含硫敵克(thiodicarb)。62D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含脫芬瑞(tolfenpyrad)。63D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含ζ-賽滅寧。64D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含一生物性殺昆蟲劑。65D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自乙醯膽鹼酯酶(AChE) 抑制劑
之活性成分。66D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自乙醯膽鹼酯酶(AChE) 抑制劑
之活性成分。67D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自GABA- 閘控型氯離子通道拮抗劑
之活性成分。68D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自鈉離子通道調節劑
之活性成分。69D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自菸 鹼型乙醯膽鹼(nAChR) 協同劑
之活性成分。70D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自菸 鹼型乙醯膽鹼受器(nAChR) 別構活化物
之活性成分。71D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自氯離子通道活化劑
之活性成分。72D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自保幼激素模擬物
之活性成分。73D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自雜類非特異性( 多重位置) 抑制劑
之活性成分。74D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自弦音器官 (Chordotonal Organs ) 調節劑
之活性成分。75D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自蟎生長抑制劑
之活性成分。76D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自破壞昆蟲中腸膜之微生物
之活性成分。77D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自粒腺體ATP 合成酶抑制劑
之活性成分。78D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自經由破壞質子梯度之氧化性磷酸化非耦聯劑
之活性成分。79D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自菸 鹼型乙醯膽鹼受器(nAChR) 通道阻斷劑
之活性成分。80D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自幾丁質生合成抑制劑,第0 型
,之活性成分。81D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自幾丁質生合成抑制劑,第1 型
,之活性成分。82D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自雙翅目脫皮干擾劑
之活性成分。83D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自蛻皮激素受器協同劑
之活性成分。84D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自章魚胺受器協同劑
之活性成分。85D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自粒腺體複合物III 電子傳遞抑制劑
之活性成分。86D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自粒腺體複合物I 電子傳遞抑制劑
之活性成分。87D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自電壓- 依賴型鈉離子通道阻斷劑
之活性成分。88D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自乙醯基輔酶A 羧化酶抑制劑
之活性成分。89D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自粒腺體複合物IV 電子傳遞抑制劑
之活性成分。90D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自粒腺體複合物II 電子傳遞抑制劑
之活性成分。91D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自羅納丹受 器 (R yanodine receptor) 調節劑
之活性成分。92D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子,其進一步包含來自UN 組
之活性成分。93D.
如5D至且含括92D中任一者之殺蟲組成物,其中如式1分子比活性成分之重量比為100:1至1:100。94D.
如5D至且含括92D中任一者之殺蟲組成物,其中如式1分子比活性成分之重量比為50:1至1:50。95D.
如5D至且含括92D中任一者之殺蟲組成物,其中如式1分子比活性成分之重量比為20:1至1比20。96D.
如5D至且含括92D中任一者之殺蟲組成物,其中如式1分子比活性成分之重量比為10:1至1:10。97D.
如5D至且含括92D中任一者之殺蟲組成物,其中如式1分子比活性成分之重量比為5:1至1:5。98D.
如5D至且含括92D中任一者之殺蟲組成物,其中如式1分子比活性成分之重量比為3:1至1:3。99D.
如5D至且含括92D中任一者之殺蟲組成物,其中如式1分子比活性成分之重量比為2:1至1:2。100D.
如5D至且含括92D中任一者之殺蟲組成物,其中如式1分子比活性成分之重量比為1:1。101D.
如5D至且含括92D中任一者之殺蟲組成物,其中式1分子比活性成分之重量比為X:Y
;其中X
為式1之分子的重量份且Y
為活性成分之重量份;進一步地其中X
重量份之數值範圍為0 <X
≤ 100且Y
重量份之數值範圍為0 <Y
≤ 100;以及進一步地其中X
及Y
係選自於表C。102D.
如101D之殺蟲組成物,其中式1分子比活性成分之重量比範圍為X1
:Y1
至X2
:Y2
;進一步地其中X1
>Y1
且X2
<Y2
。103D.
如101D之殺蟲組成物,其中式1分子比活性成分之重量比範圍為X1
:Y1
至X2
:Y2
;進一步地其中X1
>Y1
且X2
>Y2
。104D.
如101D之殺蟲組成物,其中式1分子比活性成分之重量比範圍為X1
:Y1
至X2
:Y2
;進一步地其中X1
<Y1
且X2
<Y2
。105D
. 如5D至且含括104D中任一者之殺蟲組成物,其中該殺蟲組成物進一步包含硫酸銨。106D.
如5D至且含括105D中任一者之殺蟲組成物,其中該殺蟲組成物為協同性的。107D.
一種生產殺蟲組成物之方法,該方法包含混合如請求項1D、2D、3D或4D中任一項之分子與一或多種活性成分。108D.
一種測試如107D之殺蟲組成物之方法,以判定其是否為協同性的。109D.
一種殺蟲組成物,其包含如1D、2D、3D或4D中任一者之分子及種子。110D.
一種如1D、2D、3D或4D中任一者之分子,其中該分子係農業上可接受的酸加成鹽類的形式。111D.
一種如1D、2D、3D或4D中任一者之分子,其中該分子係鹽類衍生物的形式。112D.
一種如1D、2D、3D或4D中任一者之分子,其中該分子係溶劑合物的形式。113D.
一種如1D、2D、3D或4D中任一者之分子,其中該分子係酯類衍生物的形式。114D.
一種如1D、2D、3D或4D中任一者之分子,其中該分子係結晶性多形體的形式。115D.
一種如1D、2D、3D或4D中任一者之分子,其中該分子具有氘、氚、放射性碳或是其等之組合。116D.
一種如1D、2D、3D或4D中任一者之分子,其中該分子係一個或更多個立體異構物的形式。117D.
一種如1D、2D、3D或4D中任一者之分子,其中該分子係解析的立體異構物的形式。118D.
一種控制害蟲的方法,該方法包含施用殺蟲有效量的如1D、2D、3D或4D中任一者之分子至一所在地。119D.
一種控制害蟲的方法,該方法包含施用殺蟲有效量的如5D至且含括106D中任一者之殺蟲組成物至一所在地。120D.
如118D或119D之方法,其中該害蟲係選自於螞蟻、蚜蟲、床虱(bed bug)、甲蟲、蠹蟲(bristletails)、毛蟲、蟑螂、蟋蟀、蠼螋(earwigs)、跳蚤、蒼蠅、蚱蜢、螬、葉蟬、蝨、蝗蟲、蛆、蟎、線蟲(nematode)、飛蝨(planthopper)、木蝨(psyllids)、鋸蜂(sawflies)、介殼蟲、蠹魚(silverfish)、蛞蝓、蝸牛、蜘蛛、彈尾蟲、臭蟲、綜合綱(symphylans)、白蟻、薊馬(thrips)、壁蝨、胡蜂、粉虱,以及線蟲(wireworm)。121D.
如118D或119D之方法,其中該害蟲係選自於螯肢動物亞門(Subphyla Chelicerata) 、多足亞門(Myriapoda) ,或六足亞門(Hexapoda)
。122D.
如118D或119D之方法,其中該害蟲係選自於蛛形綱 (Arachnida) 、綜合綱 (Symphyla) , 或 昆蟲綱 (Insecta) 。 123D.
如118D或119D之方法,其中該害蟲係選自於虱目 (Order Anoplura)
。124D.
如118D或119D之方法,其中該害蟲係選自於鞘翅目 (Order Coleoptera)
。125D.
如118D或119D之方法,其中該害蟲係選自於革翅目 (Order Dermaptera)
。126D.
如118D或119D之方法,其中該害蟲係選自於蜚蠊目 (Order Blattaria)
。127D.
如118D或119D之方法,其中該害蟲係選自於雙翅目 (Order Diptera)
。128D.
如118D或119D之方法,其中該害蟲係選自於半翅目 (Order Hemiptera)
。129D.
如118D或119D之方法,其中該害蟲係選自於膜翅目 (Order Hymenoptera)
。130D.
如118D或119D之方法,其中該害蟲係選自於等翅目 (Order Isoptera)
。131D.
如118D或119D之方法,其中該害蟲係選自於鱗翅目 (Order Lepidoptera)
。132D.
如118D或119D之方法,其中該害蟲係選自於食毛目 (Order Mallophaga)
。133D.
如118D或119D之方法,其中該害蟲係選自於直翅目 (Order Orthoptera)
。134D.
如118D或119D之方法,其中該害蟲係選自於囓蟲目 ( Order Psocoptera )
。135D.
如118D或119D之方法,其中該害蟲係選自於蚤目 (Order Siphonaptera)
。136D.
如118D或119D之方法,其中該害蟲係選自於纓翅目 (Order Thysanoptera)
。137D.
如118D或119D之方法,其中該害蟲係選自於纓尾目 (Order Thysanura)
。138D.
如118D或119D之方法,其中該害蟲係選自於蜱蟎目 (Order Acarina)
。139D.
如118D或119D之方法,其中該害蟲係選自於真蜘蛛目 (Order Araneae )
。140D.
如118D或119D之方法,其中該害蟲係選自於結閥綱 (Class Symphyla )
。141D.
如118D或119D之方法,其中該害蟲係選自於粘管亞綱 (Subclass Collembola )
。142D.
如118D或119D之方法,其中該害蟲係選自於圓形動物門 (Phylum Nematoda)
。143D.
如118D或119D之方法,其中該害蟲係選自於軟體動物門 ( Phylum Mollusca )
。144D.
如118D或119D之方法,其中該害蟲係取食汁液之害蟲。145D.
如144D之方法,其中該害蟲係選自於蚜蟲、葉蟬、蛾、介殼蟲(scales)、薊馬(thrips)、木蝨(psyllids)、水蠟蟲(mealybugs)、臭蟲,以及粉虱。146D.
如144D之方法,其中該害蟲係選自於虱目(Order Anoplura)及半翅目(Order Hemiptera)。147D.
如144D之方法,其中該害蟲係選自於輪盾介殼蟲屬(Aulacaspis
spp.)、沫蟬屬(Aphrophora
spp.)、蚜蟲屬(Aphis
spp.)、粉虱屬(Bemisia
spp.)、介殼蟲屬(Coccus
spp.)、美洲蝽屬(Euschistus
spp.)、草盲蝽屬(Lygus
spp.)、長管蚜屬(Macrosiphum
spp.)、稻綠蝽屬(Nezara
spp.),以及縊管蚜屬(Rhopalosiphum
spp.)。148D.
如118D或119D之方法,其中該害蟲係嚼食性害蟲。149D.
如148D之方法,其中該害蟲係選自於毛蟲、甲蟲、蚱蜢及蝗蟲。150D.
如148D之方法,其中該害蟲係選自於鞘翅目(Coleoptera)及鱗翅目(Lepidoptera)。151D.
如148D之方法,其中該害蟲係選自於豆象屬(Acanthoscelides
spp.)、豆葉甲蟲屬(Cerotoma
spp.)、跳甲屬(Chaetocnema
spp.)、肖葉甲蟲屬(Colaspis
spp.)、圓頭犀金龜屬(Cyclocephala
spp.)、葉甲屬(Diabrotica
spp.)、葉象屬(Hypera
spp.)、鰓角金龜屬(Phyllophaga
spp.)、菜葉蚤屬(Phyllotreta
spp.)、禾象鼻蟲屬(Sphenophorus
spp.)、米象屬(Sitophilus
spp.)。152D.
如118D或119D之方法,其中該所在地係紫花苜蓿、杏仁、蘋果、大麥、豆類、油菜、玉米、棉花、十字花科植物、萵苣、燕麥、橘子、花生、梨、胡椒、馬鈴薯、水稻、高粱、大豆、草莓、甘蔗、甜菜、向日葵、煙草、蕃茄、小麥,和其他有價值的作物生長或其種子種植之處。153D.
如118D或119D之方法,其中該所在地係經遺傳修飾以表現特殊性狀之植物種植之處。154D.
如118D或119D之方法,其中該施用係於植物葉子及/或果實部分上實行。155D.
如118D或119D之方法,其中該施用係於土壤實行。156D.
如118D或119D之方法,其中該施用係藉由滴灌、條施,或是種植前或種植後之土壤澆灌來實行。157D.
如118D或119D之方法,其中該施用係於植物葉子及/或果實部分實行,或是藉由種植前處理植物種子來實行。158D.
一種方法,其包含施用如1D、2D、3D或4D中任一者之分子至種子。159D.
一種方法,其包含施用如1D、2D、3D或4D之分子至一所在地,該所在地包括非人類動物飼養領域,以控制寄生蟲、外寄生蟲及二者。
本文件中之標題僅為方便且不能用於解釋本文件之任何部份。表 表
B 表
C 表2. F 系列分子之結構和製備方法 * 依據實施例編號來製備 表3. C 系列分子之結構和製備方法 * 依據 實施例編號 來製備 表4 :表2 中化合物之分析數據 表ABC :生物結果
(無)
Claims (8)
- 一種具下式之分子 式1 其中:(A) Ar1 係選自於下列所構成的群組:呋喃基(furanyl)、苯基、嗒基、吡啶基、嘧啶基、或是噻吩基, 其中每個呋喃基、苯基、嗒基、吡啶基、嘧啶基、及噻吩基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基、及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及苯氧基;(B) Het 為5或6員、飽和或不飽和之雜環,含有獨立地選自於氮、硫或氧之一或多個雜原子,以及其中Ar1 與L1 互相不為鄰位,但可為間位或對位,例如就五員環而言,其等為1,3,且就六員環而言,其等為1,3或1,4, 其中每個雜環可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、側氧、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基、及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及苯氧基;(C) L1 係選自於下列所構成的群組:N(Rx )-(C1 -C4 )烷基、N(Rx )-(C3 -C8 )環烷基、N(Rx )-(C2 -C6 )烯基、N(Rx )-(C2 -C6 )炔基、N(Rx )-S(O)n -(C1 -C4 )烷基、(C1 -C4 )烷基-N(Rx )-(C1 -C4 )烷基、(C1 -C4 )烷基-N(Rx )-(C1 -C4 )烷基、(C1 -C4 )烷基-N(Rx )、(C3 -C8 )環烷基-N(Rx )、(C2 -C6 )炔基-N(Rx )、(C1 -C4 )烷基-S(O)n -N(Rx )、C(O)-N(Rx )、C(S)-N(Rx )、N(Rx )-C(O)、N(Rx )-C(S)、C(O)-N(Rx )-(C1 -C4 )烷基、C(S)-N(Rx )-(C1 -C4 )烷基、(C1 -C4 )烷基-N(Rx )-C(O)、以及(C1 -C4 )烷基-N(Rx )-C(S), 其中每個烷基、環烷基、烯基及炔基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、以及(C2 -C6 )炔基;(D) Ar2 係選自於下列所構成的群組:呋喃基、苯基、嗒基、吡啶基、嘧啶基、或是噻吩基, 其中每個呋喃基、苯基、嗒基、吡啶基、嘧啶基、及噻吩基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基、及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(=O)O-(C1 -C4 )烷基、苯基、以及苯氧基;(E) R15 係選自於下列所構成的群組:H、(C1 -C4 )烷基、(C3 -C8 )環烷基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、C(O)-NRx Ry 、C(O)-苯基、(C1 -C4 )烷基-NRx Ry 、C(O)O-(C1 -C4 )烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)O-(C1 -C4 )烷基, 其中每個烷基、環烷基、烯基、炔基、及苯基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、側氧、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及苯氧基;(F) Q1 係選自於O及S所構成的群組;(G) Q2 係選自於O及S所構成的群組;(H) R16 係選自於下列所構成的群組:(K) 、H、(C1 -C4 )烷基、(C3 -C8 )環烷基、(C2 -C6 )烯基、(C2 -C6 )炔基、C(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、(C1 -C4 )烷基苯基、(C1 -C4 )烷基-O-苯基、C(O)-(Het-1)、(Het-1)、(C1 -C4 )烷基-(Het-1)、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-NRx Ry 、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基-(Het-1)、(C1 -C4 )烷基-C(O)-(Het-1)、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基(NRx Ry )-C(O)OH、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基-NRx Ry 、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基-N(Rx )-C(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基(N(Rx )-C(O)O-(C1 -C4 )烷基)-C(O)OH、(C1 -C4 )烷基-C(O)-(Het-1)-C(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-(C3 -C8 )環烷基、(C1 -C4 )烷基-OC(O)-(Het-1)、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基-N(Rx )-C(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-NRx Ry 、(C1 -C4 )烷基-S(O)n -(Het-1)、以及(C1 -C4 )烷基-O-(Het-1), 其中每個烷基、環烷基、烯基、炔基、苯基、及(Het-1)可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、NRx Ry 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)H、C(O)OH、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基)、苯基、苯氧基、Si((C1 -C4 )烷基)3 、S(O)n -NRx Ry 、以及(Het-1);(I) R17 係選自於下列所構成的群組:(K) 、H、(C1 -C4 )烷基、(C3 -C8 )環烷基、(C2 -C6 )烯基、(C2 -C6 )炔基、C(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、(C1 -C4 )烷基苯基、(C1 -C4 )烷基-O-苯基、C(O)-(Het-1)、(Het-1)、(C1 -C4 )烷基-(Het-1)、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-NRx Ry 、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基-(Het-1)、(C1 -C4 )烷基-C(O)-(Het-1)、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基(NRx Ry )-C(O)OH、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基-NRx Ry 、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基-N(Rx )-C(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基(N(Rx )-C(O)O-(C1 -C4 )烷基)-C(O)OH、(C1 -C4 )烷基-C(O)-(Het-1)-C(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-(C3 -C8 )環烷基、(C1 -C4 )烷基-OC(O)-(Het-1)、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基-N(Rx )-C(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-NRx Ry 、(C1 -C4 )烷基-S(O)n -(Het-1)、以及(C1 -C4 )烷基-O-(Het-1), 其中每個烷基、環烷基、烯基、炔基、苯基、及(Het-1)可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、NRx Ry 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)H、C(O)OH、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、苯氧基、Si((C1 -C4 )烷基)3 、S(O)n -NRx Ry 、以及(Het-1);(J) L2 係選自於下列所構成的群組:(C3 -C8 )環烷基、苯基、(C1 -C4 )烷基苯基、(C1 -C4 )烷基-O-苯基、(C2 -C6 )烯基-O-苯基、(Het-1)、(C1 -C4 )烷基-(Het-1)、以及(C1 -C4 )烷基-O-(Het-1), 其中每個烷基、環烷基、烯基、苯基、及(Het-1)可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、NRx Ry 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)H、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C1 -C4 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、O-(C1 -C4 )烷基、S-(C1 -C4 )烷基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、苯氧基、以及(Het-1), 其中每個烷基、環烷基、烯基、苯基、及(Het-1)取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、NRx Ry 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)H、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C1 -C4 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、O-(C1 -C4 )烷基、S-(C1 -C4 )烷基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、苯氧基、以及(Het-1);(K) R16 及R17 與Cx (Q2 )(Nx ) 一起形成一個4-至7-員飽和或不飽和之雜環,其可以進一步含有選自於氮、硫及氧所構成的群組之一個或更多個雜原子, 其中每個雜環可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:側氧、R18 及R19 , 其中R18 及R19 係各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2 、側氧、硫酮基、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)H、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及(Het-1);(L) Rx 及Ry 係各自獨立地選自於下列所構成的群組:H、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)H、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、以及苯基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、及苯基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)H、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基 、以及(Het-1);(M) (Het-1) 為5或6員、飽和或不飽和之雜環,含有獨立地選自於氮、硫或氧所構成的群組之一或多個雜原子, 其中每個雜環可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、側氧、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基、及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及苯氧基;(N) n 每一者係獨立地為0、1或2;以及式1之分子的N-氧化物、農業上可接受的酸加成鹽類、鹽類衍生物、溶劑合物、酯類衍生物、結晶性多形體、同位素、解析的立體異構物,以及互變異構物。
- 如請求項1之分子,其中:(A) Ar1 為(1a) (1a) , 其中,R1 、R2 、R3 、R4 及R5 各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基、及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及苯氧基;(B) Het 為(1b) (1b) , 其中R6 可以選擇性地以選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、側氧、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基、及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及苯氧基;(C) L1 係選自於下列所構成的群組 (1c) 、 (1d) 、 (1e) 、及 (1f) , 其中:(1) Qx 係各自選自於O及S所構成的群組,以及(2) R7 、R8 、R9 及R10 係各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、以及(C2 -C6 )炔基;(D) Ar2 為(1g) (1g) , 其中:(1) X1 係選自於N及CR13 所構成的群組,以及(2)R11 、R12 、R13 、 及R14 各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基、及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(=O)O-(C1 -C4 )烷基、苯基、以及苯氧基;(E) R15 係選自於下列所構成的群組:H、(C1 -C4 )烷基、(C3 -C8 )環烷基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)O-(C1 -C4 )烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)O-(C1 -C4 )烷基, 其中每個烷基、環烷基、烯基、及炔基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、側氧、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及苯氧基;(F) Q1 係選自於O及S所構成的群組;(G) Q2 係選自於O及S所構成的群組;(H) R16 係選自於下列所構成的群組:(K) 、H、(C1 -C4 )烷基、(C3 -C8 )環烷基、(C2 -C6 )烯基、(C2 -C6 )炔基、C(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、(C1 -C4 )烷基苯基、(C1 -C4 )烷基-O-苯基、C(O)-(Het-1)、(Het-1)、(C1 -C4 )烷基-(Het-1)、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-NRx Ry 、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基-(Het-1)、(C1 -C4 )烷基-C(O)-(Het-1)、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基(NRx Ry )-C(O)OH、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基-NRx Ry 、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基-N(Rx )-C(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基(N(Rx )-C(O)O-(C1 -C4 )烷基)-C(O)OH、(C1 -C4 )烷基-C(O)-(Het-1)-C(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-(C3 -C8 )環烷基、(C1 -C4 )烷基-OC(O)-(Het-1)、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基-N(Rx )-C(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-NRx Ry 、(C1 -C4 )烷基-S(O)n -(Het-1)、以及(C1 -C4 )烷基-O-(Het-1), 其中每個烷基、環烷基、烯基、炔基、苯基、及(Het-1)可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、NRx Ry 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)H、C(O)OH、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基)、苯基、苯氧基、Si((C1 -C4 )烷基)3 、S(O)n -NRx Ry 、以及(Het-1);(I) R17 係選自於下列所構成的群組:(K) 、H、(C1 -C4 )烷基、(C3 -C8 )環烷基、(C2 -C6 )烯基、(C2 -C6 )炔基、C(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、(C1 -C4 )烷基苯基、(C1 -C4 )烷基-O-苯基、C(O)-(Het-1)、(Het-1)、(C1 -C4 )烷基-(Het-1)、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-NRx Ry 、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基-(Het-1)、(C1 -C4 )烷基-C(O)-(Het-1)、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基(NRx Ry )-C(O)OH、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基-NRx Ry 、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基-N(Rx )-C(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-C(O)-N(Rx )(C1 -C4 )烷基(N(Rx )-C(O)O-(C1 -C4 )烷基)-C(O)OH、(C1 -C4 )烷基-C(O)-(Het-1)-C(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基、(C1 -C4 )烷基-OC(O)-(C3 -C8 )環烷基、(C1 -C4 )烷基-OC(O)-(Het-1)、(C1 -C4 )烷基-OC(O)-(C1 -C4 )烷基-N(Rx )-C(O)O-(C1 -C4 )烷基、(C1 -C4 )烷基-NRx Ry 、(C1 -C4 )烷基-S(O)n -(Het-1)、以及(C1 -C4 )烷基-O-(Het-1), 其中每個烷基、環烷基、烯基、炔基、苯基、及(Het-1)可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、NRx Ry 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)H、C(O)OH、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、苯氧基、Si((C1 -C4 )烷基)3 、S(O)n -NRx Ry 、以及(Het-1);(J) L2 係(1h) (1h) , 其中R20 、R21 、R22 、R23 及R24 各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2 、NRx Ry 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)H、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C1 -C4 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、O-(C1 -C4 )烷基、S-(C1 -C4 )烷基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、苯氧基、以及(Het-1), 其中每個烷基、環烷基、烯基、苯基、及(Het-1)取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、NRx Ry 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)H、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C1 -C4 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、O-(C1 -C4 )烷基、S-(C1 -C4 )烷基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、苯氧基、以及(Het-1);(K) R16 及R17 與Cx (Q2 )(Nx ) 一起,係(1i) (1i) , 其中R18 及R19 係各自獨立地選自於下列所構成的群組:H、F、Cl、Br、I、CN、NO2 、側氧、硫酮基、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)H、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及(Het-1);(L) Rx 及Ry 係各自獨立地選自於下列所構成的群組:H、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)H、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、以及苯基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、及苯基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)H、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及(Het-1);(M) (Het-1) 為5或6員、飽和或不飽和之雜環,含有獨立地選自於氮、硫或氧所構成的群組之一或多個雜原子, 其中每個雜環可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H 、F、Cl、Br、I、CN、NO2 、側氧、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、以及苯氧基, 其中每個烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基、及苯氧基取代基可以選擇性地以一個或更多個獨立地選自於下列所構成的群組之取代基予以取代:H、F、Cl、Br、I、CN、NO2 、(C1 -C4 )烷基、(C1 -C4 )鹵烷基、(C3 -C8 )環烷基、(C1 -C4 )烷氧基、(C1 -C4 )鹵烷氧基、(C2 -C6 )烯基、(C2 -C6 )炔基、S(O)n -(C1 -C4 )烷基、S(O)n -(C1 -C4 )鹵烷基、OSO2 -(C1 -C4 )烷基、OSO2 -(C1 -C4 )鹵烷基、C(O)-NRx Ry 、(C1 -C4 )烷基-NRx Ry 、C(O)-(C1 -C4 )烷基、C(O)O-(C1 -C4 )烷基、C(O)-(C1 -C4 )鹵烷基、C(O)O-(C1 -C4 )鹵烷基、C(O)-(C3 -C8 )環烷基、C(O)O-(C3 -C8 )環烷基、C(O)-(C2 -C6 )烯基、C(O)O-(C2 -C6 )烯基、(C1 -C4 )烷基-O-(C1 -C4 )烷基、(C1 -C4 )烷基-S(O)n -(C1 -C4 )烷基、C(O)-(C1 -C4 )烷基-C(O)O-(C1 -C4 )烷基、苯基、及苯氧基;以及(N) n 每一者係獨立地為0、1或2。
- 如請求項1之分子,其中:(A) Ar1 為(1a) (1a) , 其中,R1 、R2 、R3 、R4 及R5 各自獨立地選自於下列所構成的群組:H及(C1 -C4 )鹵烷氧基;(B) Het 為(1b) (1b) , 其中,R6 為H;(C) L1 係選自於下列所構成的群組 (1c) 、 (1d) 、 (1e) 、及 (1f) , 其中:(1) Qx 為O,以及(2) R7 、R8 、R9 及R10 各自獨立地選自於H及(C1 -C4 )烷基所構成的群組;(D) Ar2 為(1g) (1g) , 其中:(1) X1 係選自於N及CR13 所構成的群組,以及(2)R11 、R12 、R13 及R14 各自獨立地選自於下列所構成的群組:H、F以及Cl;(E)R15 為H;(F) Q1 為O;(G)Q2 為S;(H)R16 為(K) ;(I)R17 為(K) ;(J) L2 係(1h) (1h) , 其中,R20 、R21 、R22 、R23 及R24 各自獨立地選自於下列所構成的群組:H、(C1 -C4 )烷基、以及(C1 -C4 )烷基-O-(C1 -C4 )烷基;以及(K) R16 及R17 與Cx (Q2 )(Nx ) 一起,係(1i) (1i) , 其中,R18 及R19 各自獨立地為H。
- 如請求項1之分子,其中:(A) Ar1 為(1a) (1a) , 其中,R1 、R2 、R3 、R4 及R5 各自獨立地選自於下列所構成的群組:H3 及OCF3 ;(B) Het 為(1b) (1b) , 其中,R6 為H;(C) L1 係選自於下列所構成的群組 (1c) 、 (1d) 、 (1e) 、及 (1f) , 其中:(1) Qx 為O,以及(2) R7 、R8 、R9 及R10 各自獨立地選自於H及CH3 所構成的群組;(D) Ar2 為(1g) (1g) , 其中:(1) X1 係選自於N及CR13 所構成的群組,以及(2)R11 、R12 、R13 及R14 各自獨立地選自於下列所構成的群組:H、F以及Cl;(E)R15 為H;(F) Q1 為O;(G)Q2 為S;(H)R16 為(K) ;(I)R17 為(K) ;(J) L2 係(1h) (1h) , 其中,R20 、R21 、R22 、R23 及R24 各自獨立地選自於下列所構成的群組:H、CH3 、CH2 CH2 CH3 、CH(CH3 )2 、CH2 OCH3 ,及CH(CH3 )OCH3 ;以及(K) R16 及R17 與Cx (Q2 )(Nx ) 一起,係(1i) (1i) , 其中,R18 及R19 各自獨立地為H。
- 如請求項1之分子,其中該分子為
。 - 一種殺蟲組成物,其包含如請求項1、2、3、4或5中任一項之分子,其進一步包含一活性成分。
- 一種控制害蟲的方法,該方法包含施用殺蟲有效量的如請求項1、2、3、4或5中任一項之分子至一所在地。
- 一種控制害蟲的方法,該方法包含施用殺蟲有效量的如請求項6之殺蟲組成物至一所在地。
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| US201562214348P | 2015-09-04 | 2015-09-04 |
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