摘要
以4-乙酰氧基氮杂环丁酮(2)为母核,与手性合成辅助剂溴丙酰基-螺环[2H-1,3-苯并噁嗪-2,1'-环己基]-3(4H)-酮(3)进行取代反应,水解得培南类关键中间体(3S,4S)-4-([R)-1-羰基乙基]-3-([R)-1-(t-丁基二甲基硅烷氧基)乙基]-2-丙内酰胺(1),总收率约为81%~87.6%[以4-乙酰氧基氮杂环丁酮(2)计]。
The key penems intermediate of(3S,4S)-4-[(1R)-1-Carboxyethyl]-3-[(1R)-1-(t-Buthyldime-thylsilyloxy) ethyl]-2-azetidione was synthesized from(3S,4R)-4-Acetoxy-3-[(R)-1-(tert-butyldimethylsilyl-oxy)ethyl]azetidin-2-one with chiral synthesis auxiliary agent 3-(2-bromopropanoyl)spiro[benzo[e]o-xazine-2,1'-cyclohexan]-4(3H)-one by substitution reaction,followed by hydrolysis.The overall yield was about 81%~87.6%(based on compound 2).
出处
《中兽医医药杂志》
2012年第2期20-21,共2页
Journal of Traditional Chinese Veterinary Medicine
基金
上海市科委科研计划项目
关键词
培南类
中间体
合成
bovine clinical mastitis
pathogenic bacteria
isolation
identification
drug sensitive test