摘要
甲苯经酰化、缩酮重排和水解转化成2-对甲苯基丙酸后,经溴代、酯化制成2-对溴代甲苯基丙酸乙酯,再在PEG-600和无水碳酸钾存在下,对2-乙氧羰基环戊酮进行烷基化后,直接水解、脱羧、成盐而得洛索洛芬钠,总收率35%。
A facile method for preparation of loxoprofen sodium is disclosed.Ethyl 2 ( p bromomethyl phenyl) propionate,prepared from toluene via acylation,ketalization,rearrangement,hydrolysis,bromination and esterification,was subjected to phase transfer ca talyzed alkylation with ethyl 2 oxocyclopentanecarboxylate,followed by hydrolysis with decarboxylation and salt formation in one pot procedure to afford loxoprofen sodium in about 35% overall yield.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
1998年第12期531-533,共3页
Chinese Journal of Pharmaceuticals
关键词
洛索洛芬钠
缩酮化
合成
重排
消炎镇痛药
loxoprofen sodium,ketalization,bromination,PTC,alkylation,synthesis