醋酸氢化可的松合成工艺改进  

Improvement of the Synthesis Process of Hydrocortisone Acetate

作　　者：江海 柳山 王佳佳 金旦妮 JIANG Hai;LIU Shan;WANG Jiajia;JIN Danni(Taizhou Xianju Pharmaceutical Co.,Ltd.,Taizhou,Zhejiang 317016,China)

机构地区：[1]台州仙琚药业有限公司,浙江台州317016

出　　处：《浙江化工》2024年第12期32-37,共6页Zhejiang Chemical Industry

摘　　要：针对原工艺存在溴羟化反应收率低、选择性差等问题,开发了一种醋酸氢化可的松的制备方法。以企业自产的21-氯代氢化可的松为原料,经亲核取代、溴羟化及脱溴3步反应合成目标化合物醋酸氢化可的松,具有工艺原辅料成本低、反应选择性好等优点,总收率达71.2%。产物结构经^(1)H NMR、^(13)C NMR和MS(ESI)等谱图确证。In order to solve the problems of low yield and poor selectivity of bromohydroxylation reaction in the original process,a preparation method for hydrocortisone acetate was developed.Using the 21-chlorohydrocortisone produced by the company as raw material,the target compound hydrocortisone acetate was synthesized by a three-step reaction of nucleophilic substitution,bromohydroxylation and debromination,which has the advantages of low cost of process raw materials and good reaction selectivity,with a total yield of 71.2%.The structure of the product was confirmed by ^(1)H NMR,^(13)C NMR and MS(ESI).

关 键 词：21-氯氢化可的松 醋酸氢化可的松 溴羟化 脱溴 

分 类 号：TQ460.6[化学工程—制药化工]