摘要
以３－苯氧基甲苯为起始原料，经溴代、氰化、水解制成３－苯氧基苯乙酸（４）。在相转移催化剂存在下，用硫酸二甲酯使（４）α－单甲基化，不经分离直接成盐，即得苯氧布洛芬钙，总收率３６．５％。本法原料易得、操作简便、成本低，适宜于工业化生产。
A new and convenient synthetic process for synthesizing fenoprofen calcium was established.3-phenoxytoluene was brominated with NBS/AIBN/CCl4 to afford 3-phenoxybenzylbromide(2).(2)was subjected to cyanidation hydrolysis to produce 3-phenoxyphenyl acetic acids(4),α-monomethylation of which with (CH3)2SO4 in the presence of KOH/TEBAC/PEG-400,followed with calcium chloride to give fenoprofen calcium in overall yield of about 36.5%.This process is applicable to large-scalepreparatio.
出处
《华西药学杂志》
CAS
CSCD
北大核心
1996年第1期26-28,共3页
West China Journal of Pharmaceutical Sciences
关键词
消炎镇痛药
苯氧布洛芬
合成工艺
Fenoprofen calcium
Phase transfer catalysis
α-Monomethylation
Synthesis
