武汉工程大学学报2025，Vol.47Issue(6)：600-606,7.DOI:10.19843/j.cnki.CN42-1779/TQ.202309011
恩康唑的制备工艺研究
Study of the synthetic process of enilconazole
摘要
Abstract
Enilconazole,a broad-spectrum fungicide originally developed by Janssen Pharmaceutica(Belgium),is classified as a Category Ⅱ new veterinary drug in China,where there are no manufacturers with either its active pharmaceutical ingredient(API)or formulated products approvals.Based on a systematic analysis of existing synthetic routes,a novel green pathway was designed to overcome the critical limitations of conventional approaches—specifically,the hazardous nitration and high-pressure hydrogenation steps and the low overall yield(≤30％).The synthesis started with commercially available imidazole,which underwent regioselective N-alkylation with 3-chloro-1-propene in an ionic liquid medium.The resulting intermediate was then chemoselectively reduced using a sodium borohydride-boron trifluoride etherate system,thereby eliminating the need for high-pressure hydrogenation.Finally,O-alkylation catalyzed by potassium carbonate/PEG-400 afforded enilconazole API that consistently complied with European Pharmacopoeia specifications.关键词
恩康唑/原料药/合成工艺/优化Key words
enilconazole/active pharmaceutical ingredient(API)/synthetic process/optimization分类
医药卫生引用本文复制引用
黎浩,刘一粟,祝宏,张银博,袁航..恩康唑的制备工艺研究[J].武汉工程大学学报,2025,47(6):600-606,7.基金项目
武汉工程大学第十六届研究生教育创新基金(CX2024252) （CX2024252）
