摘要
在叔丁醇钠和二甲基亚砜的存在下,2-(对溴甲基苯基)丙酸对2-乙氧羰基环戊酮进行C-烷基化,再经水解脱羧,成盐即得洛索洛芬钠,以2-(对溴甲基苯基)丙酸计算,总收率为72%。探索了不同溶剂和反应温度对烷基化收率的影响。
In the presence of sodium t- butoxide and DMSO,ethyl 2 - oxocyclopentanecarboxylate was subjected to C- alkylation with 2 - ( 4- bromomethylphenyl) propanoic acid with high regioselectivity to give 2 - [4 - ( 1 - ethoxycarbonyl- 2 - oxo- 1 - cyclopentanylmethyl) phenyl]propanoic acid ( 4) which was followed by hydrolysis,decarboxylation and saltformation to afford loxoprofen sodium in about72 % overall yield.The effects of reaction temperature and different solvents on yield of4 were also investigated.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2000年第1期1-2,共2页
Chinese Journal of Pharmaceuticals
关键词
洛索洛芬钠
C-烷基化
O-烷基化
合成
loxoprofen sodium
C- alkylation
O- alkylation
retro- Dieckmann reaction
synthesis
