2－芳基丙酸类消炎镇痛药物的研究4苯氧布洛芬钙的新合成法  

STUDIES ON THE ANTIINFLAMMATORY DRUGS OF 2-ARYLPROPANOIC ACIDS 4 NEW SYNTHETIC METHOD FOR FENOPROFEN CALCIUM

作　　者：陈芬儿[1] 张珩[1] 管春生[1] 杨建设[1] 冯秀梅[1] 唐维高[1] 马丽芳[1] 

机构地区：[1]武汉化工学院合成药物研究室,成都华西医科大学药学院,四川联合大学化学系

出　　处：《华西药学杂志》1996年第1期26-28,共3页West China Journal of Pharmaceutical Sciences

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.

关 键 词：消炎镇痛药 苯氧布洛芬 合成工艺 

分 类 号：TQ463.4[化学工程—制药化工]