3-(4-甲磺酰基)苯基-2-环己基-2-丁烯酸-γ-内酯的合成  

Synthesis of 3-[4-(methylsulfonyl)phenyl]-2-cyclohexyl-2-crotonolactone

作　　者：张士英[1] 刘泓[1] 汪洁[1] 吴达俊[2] 

机构地区：[1]上海师范大学生命与环境科学学院,上海201418 [2]华东理工大学化学与制药学院,上海200237

出　　处：《中国现代应用药学》2005年第1期47-48,共2页Chinese Journal of Modern Applied Pharmacy

基　　金：上海市高等学校青年科学基金的资助(编号为 01QN87)

摘　　要：目的　设计并合成了标题化合物。方法　以对甲磺酰基苯乙酮为原料,经溴代、缩合和环合三步反应合成了产物。结果　总收率为 82. 5%,中间体和产物经核磁共振谱和质谱确证。结论　成功地合成了设计的化合物,而且摸索了反应条件,使反应具有时间短,收率高等优点。OBJECTIVE To modify the structure of Rofecoxib(COX-2 inhibitor) and synthesize the title compound.METHOD The title compound was synthesized from p-methylsulfonyl-acetophenone via bromination ,condensation and cyclization.RESULTS The total yield amounted to 82.5%. The structures were characterized by MS and 1H-NMR.CONCLUSION The new compound is synthesized and its process is improved with high yield and shortening reaction time.

关 键 词：溴化 罗非昔布 JTE-522 NS-398 环合反应 

分 类 号：TQ460.6[化学工程—制药化工]