伊格列净的合成  

Synthesis of ipragliflozin

作　　者：张淋淋[1] 李江红[1] 杨晨[1] 任凤英[1] 石克金[1] 陈林[1] 苟小军[1] 丁小东[2] 

机构地区：[1]药食同源植物资源开发四川省高校重点实验室,四川抗菌素工业研究所,成都大学,四川成都610052 [2]四川大学分析测试中心,四川成都610064

出　　处：《化学研究与应用》2016年第12期1789-1791,共3页Chemical Research and Application

基　　金：药食同源植物资源开发四川省高校重点实验室开放基金资助项目(10Y201607)

摘　　要：以苯并噻吩和2-氟-5-溴苯甲醛为原料,经过加成,还原得到中间体2-(5-溴-2-氟苄基)苯并噻吩,该中间体与2,3,4,6-四-O-三甲基硅烷基-D-吡喃葡萄糖酸-1,5-内酯经缩合,甲醚化,还原得目标化合物伊格列净,总收率50.12%,纯度98.71%,其结构经1H NMR及MS确证。2-[（ 5-Bromo-2-fluorophenyl） methyl]-benzothiophene was synthesized from benzothiophene and 2-fluoro-5-bromobenzaldehyde,via addition and reduction,which was condensed with 2,3,4,6-tetra-O-trimethylsilyl-D-glucono-1,5-lactone.Finally,via the removal of the methoxy to obtain ipragliflozin with an overall yield of 50. 12% and a purity of 98.71%. The target compound was confirmed by 1^H NMR and MS.

关 键 词：伊格列净 SGLT2抑制剂 合成 降糖药 

分 类 号：O629.11[理学—有机化学]