新型抗感染药赛来昔布的合成新工艺  

New synthesis technology about celecoxib of a new anti-inflammatory

作　　者：姚德勇 王巧玲 

机构地区：[1]青岛康地恩药业有限公司,山东青岛266061

出　　处：《中国医药导报》2010年第16期29-30,共2页China Medical Herald

摘　　要：目的:研究一步法制备赛来昔布的合成方法。方法:以异丙醇为溶剂,对甲基苯乙酮与三氟乙酸乙酯为原料缩合得到1-(4-甲基苯基)-4,4,4-三氟-1,3-丁二酮,直接与对磺胺基苯肼盐酸盐在溶剂脱水环合。结果:本法总收率达83%。结论:赛来昔布新合成方法切实可行。objective：To improve the one stage synthetic method of celecoxib. Methods：In isopropyl alcohol,the conden-sation of 4-methylacetophenone with ethyl trifluoroacetate by means of sodium methoxide gives 1-（4-methylphenyl） -4,4,4-trifluorobutane which was cyclodehydrated with（4-sulfamoylphenyl） hydrazine hydrochloride to give celecoxib. Results：The total yield reached up to around 83%. Conclusion：The new synthesis process of celecoxib is practicable.

关 键 词：赛来昔布 环氧化酶 合成 

分 类 号：R914.5[医药卫生—药物化学]