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本文详细介绍了2,2-二甲基-3-(2,2-二氯乙烯基)-环丙烷羧酸-α-氰基-4-氟-3-苯氧基苄酯的光学异构体的全合成方法.通过比较选择出一条合成醇组份中间体-4-氟-3-苯氧基苯甲醛的较实用的路线;利用立体有择反应进行脱卤化氢环化合成了外消旋富顺式二氯菊酸.同时设计了一条合成α-苯基-β-对甲苯基乙胺(PTE)的新路线,以“优先结晶法”拆分得到(+)PTE和(一)PTE拆分剂.将外消旋顺式和反式二氯菊酸分别进行拆分、酯化,制得上述酯的几种光学活性异构体. 为了阐明酯的化学结构与生物活性的关系,还分别进行了杀虫药效测试,并证实了(+)-顺式异构体是一种高效含氟拟除虫菊酯杀虫剂.
This paper describes in detail the optical isomerisation of 2,2-dimethyl-3- (2,2-dichlorovinyl) -cyclopropanecarboxylic acid-α-cyano-4-fluoro-3-phenoxybenzyl ester Body synthesis method by comparing the selection of a synthetic alcohol component intermediate -4-fluoro-3-phenoxybenzaldehyde more practical route; the use of stereoselective reaction dehydrohalogenation cyclization of consumer A new route of synthesizing α-phenyl-β-p-tolyethylamine (PTE) was designed and the "(PTE) Resolving agent.Simultaneous resolution and esterification of racemic cis and trans-dichloro-chrysanthemic acid were carried out to prepare several optically active isomers of the above ester.In order to elucidate the relationship between the chemical structure of the ester and the biological activity, Insecticide efficacy tests were also conducted separately and confirmed that the (+) - cis-isomer is a highly effective pyrethroid insecticide.