摘要
本实验提出了改进抗结核临床筛选药PA-824(1)的合成方法,以2-溴-4-硝基咪唑和缩水甘油硅醚为原料,亲核进攻开环反应得到(S)-1-(叔丁基二甲基硅氧基)-3-(4-硝基-1H-咪唑-1-)丙烷-2-醇(4),然后用对三氟甲氧基苄溴与羟基反应得到的中间体(6)再脱保护基,直接环合得到PA-824(1),总收率44.0%。
An improved method for the synthesis of PA-824(1) was introduced in this paper, 2-bromine-4-nitroimidazole and diglycidyl glycidylether as starting materials, after nucleophilic attacktion, we obtained the intermediate (S)-1-(tert-butyl)dimethylsiloxy-3-(4-nitro-1H-imidazole)propane-2-ol(4), which was further reacted with 4-trifluoro methoxy benzyl bromide, then deprotected and cyclized to afford final compound PA-824(1)with 44.0% overall yield.
作者
张志鹏
段茹
王润卿
Zhang Zhipeng;Wang Runqing;Duan Ru(Suzhou lanxite biological technology co., LTD, Jiangsu, 215000;Affiliated Wuxi people’s Hospital of Nanjing Medical University, Jiangsu, 214000)
出处
《当代化工研究》
2016年第5期84-85,共2页
Modern Chemical Research
关键词
PA-824
抗结核
合成改进
临床筛选药
PA-824
anti-tuberculosis
synthesis improvement
clinical screening drugs
