氟丙菊酯合成工艺研究

Study on Synthetic Technology of Acrinathrin

研究了氟丙菊酯的合成工艺。通过取代反应、艾伯佐夫反应、维蒂烯反应和酯化反应完成碳骨架的构建,合成了中间体(1R,3S,Z)-3-(3-叔丁氧基-3-氧代丙1-烯基)-2,2-二甲基环丙甲酸-(S)-氰基(3-苯氧基苯基)甲酯(AMT)。通过消去反应和酯化反应将AMT分子中的叔丁酯基转换成六氟异丙基,完成氟丙菊酯的合成。确定了最优反应条件,优化后六步总收率达到71.92%,氟丙菊酯含量99.37%。所用工艺稳定性好,适合工业化生产。

The synthetic technology of acrinathrin was studied. The carbon skeleton was constructed by substitution reaction, arbuzov reaction, Witting reaction and esterification reaction, and the intermediate(1R, 3S, z)-3-(3-tert-butoxy-3-oxopropyl-1-enyl)-2,2-dimethylcyclopropanic acid-(s)-cyano(3-phenoxyphenyl)methyl ester(AMT) was synthesized. The tert butyl group in AMT molecule was converted into hexafluoroisopropyl by elimination reaction and esterification reaction to complete the synthesis of acrinathrin. The optimum reaction conditions were determined. After optimization, the total yield of six steps was 71.92 % and the content of acrinathrin was 99.37 %. The process has good stability and is suitable for industrial production.