4-[4-(5-氧代-1,5-二氢-[1,2,4]三唑-4-基)苯基]哌嗪-1-羧酸叔丁酯的合成工艺改进  

Improved synthesis of 4-[4-(5-oxo-1,5-dihydro-[1,2,4]triazoyl-4-yl) phenyl]piperazine-1-carboxylic t-butyl ester

作　　者：盛春泉[1] 张万年[1] 徐辉[1] 车晓颖[1] 张珉[1] 姚建忠[1] 缪震元[1] 

机构地区：[1]第二军医大学药学院全军药物化学重点实验室,上海200433

出　　处：《中国药物化学杂志》2006年第3期159-160,164,共3页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金项目(30430750)

摘　　要：目的改进三唑类抗真菌药物关键中间体4-[4-(5-氧代-1,5-二氢-[1,2,4]三唑-4-基)苯基]哌嗪-1-羧酸叔丁酯的合成工艺。方法以1-(4-硝基苯基)哌嗪为起始原料,经Boc保护、硝基还原、酰化、肼解、环合制得目标化合物。结果与结论新工艺反应条件温和,无需柱色谱纯化,总收率从39.10%提高至71.94%。Aim To improve the synthetic process of 4- [ 4- （ 5-oxo- 1, 5- dihydro- [ 1, 2, 4 ] triazoyl-4- yl） phenyl ] piperazine-1-carboxylic t-butyl ester, which is used as the key intermediate of triazole antifungal agents. Methods The product was synthesized from 1-（4-nitrophenyl）piperazine by Boc protection, reduction of nitro group, acylation, hydrazinolysis and cyclization. Results and conclusion The new synthetic process has several advantages such as facile reaction condition, convenient operation and purification without chromatography. The overall yield is improved from 39.10 % to 71.94 %.

关 键 词：药物化学 工艺改进 化学合成 抗真菌 药物中间体 

分 类 号：TQ465[化学工程—制药化工]