关键词: 丙硫菌唑, 异丙基氯化镁, 缩合反应

Abstract: Taking 2-chrolobenzyl chrolide as the raw material, Prothioconazole was normally obtained via Grignard reaction, condensation and vulcanization reaction. However, this reported synthesis process was difficult to be applied industrially due to the low yield of Grignard reagent and huge amount of coupling byproduct formed. Chloro-cyclopropyl(benzyl)methanone, the product of condensation reaction of acid and ester, was taken as the key intermediate to synthesis prothioconazole in this work. Under the optimal reaction condition, 2-chlorophenylaceticacid and methyl 1-chrolocyclopropanecarboxylate were taken as the reactants, tetrahydrofuran as the solvent, the product ketone was obtained in the presence of the Grignard reagent i-PrMgCl. The content of the product was 98.2% after distillation and the yield was 83%. The synthesis process is suitable for industrial application with the advantages of high yield and easy to operate under mild operation condition.

Key words: prothioconazole, i-PrMgCl, condensation reaction