一种SGLT-2抑制剂Ertugliflozin关键中间体的简便合成  

New Method for the Synthesis of 3-aryl-2,5-Dihydrofurans

作　　者：杨清鑫[1] 杨靖翔[1] 刘亦斌 李兴伟 陈友喜 张春桃[1] 

机构地区：[1]湖南中医药大学,湖南长沙410208 [2]上海阳帆医药科技有限公司,上海201203

出　　处：《化工时刊》2013年第4期21-24,共4页Chemical Industry Times

摘　　要：报道了一种以2-氯-5-溴苯甲酸为底物经酰化,还原,甲酰化等多步反应得到4-氯-3-(4-乙氧基苄基)苯甲醛的简便合成,提供了一种SGLT-2抑制剂Ertugliflozin关键中间体的新合成方法,该方法所用原料和试剂廉价易得,合成路线简洁,操作简便,收率高,有利降低生产成本,提高生产效率。A facile synthesis of 4 - chloro - 3 - （4 - Bbenzyl） benzaldehyde was reported. The synthesis was performed by the acylation, reduction and hydroformylation of 2 - chloro -5 -bromo -benzoic acid. This procedure offered easy access to obtain key intermediates of Ertugliflozin in an accessible materials and facile conditions with good yields, even to reduce costs and improve production efficiency.

关 键 词：SGLT-2抑制剂 Ertugliflozin 2-氯-5-溴苯甲酸 甲酰化 

分 类 号：TQ463[化学工程—制药化工]