氢化可的松的合成工艺改进  

Improvement on the Synthesis of Hydrocortisone

作　　者：潘建洪 方从申 陈凯 顾光志 PAN Jian-hong;FANG Cong-shen;CHEN Kai;GU Guang-zhi(Taizhou Xianju Pharmaceutical Co., Ltd., Taizhou, Zhejiang 317016, China)

机构地区：[1]台州仙琚药业有限公司

出　　处：《浙江化工》2019年第10期14-17,共4页Zhejiang Chemical Industry

摘　　要：以17α-羟基孕甾-4,9(11)-二烯-3,20-二酮-21-醋酸酯为原料,经溴羟化、脱溴及水解等三步反应合成目标化合物氢化可的松。溴代物不经分离并采用氢化三丁基锡代替传统的铬试剂进行脱溴反应,减少了操作步骤及三废排放量,并使反应总收率达到68%。产物结构经1HNMR、13CNMR及熔点等数据确证。The desired product hydrocortisone was synthesized via hxdroxybromination, debromination and hydrolysis by using 17α-Hydroxy-11-deoxycorticosterone-21-acetate as the raw material. The brominated intermediate was not isolated, and the debromination was realized via applying tributyltin hydride as debromination reagent rather than the traditional chromium. The synthetic process was simplified, and waste was reduced, leading to the increasement of the total yield to 68%. The structure of product was confirmed by 1H NMR, 13C NMR and MS(ESI).

关 键 词：氢化可的松 脱溴 17α-羟基孕甾-4 9(11)-二烯-3 20-二酮-21-醋酸酯 溴羟化 

分 类 号：TQ460.6[化学工程—制药化工]