卡格列净关键中间体合成研究  

Synthesis of Key Intermediate of Canagliflozin

作　　者：钟铮[1] 王娅平[1] 冯卫生[1] 

机构地区：[1]河南中医药大学药学院,郑州450046

出　　处：《河南科学》2016年第8期1241-1244,共4页Henan Science

摘　　要：以对氟溴苯和2-溴噻吩为原料合成2-(4-氟苯基)噻吩(2)时,反应时间8 h,反应温度20℃时收率最高;以2和2-甲基-5-溴苯甲酸为原料合成5-溴-2-甲基苯基-2-(4-氟苯基)噻吩甲酮(4)时,反应温度20℃,反应时间10 h时收率最高;以4为原料合成2-(5-溴-2-甲基苄基)-5-(4-氟苯基)噻吩(1)时,反应温度100℃,锌粉用量为3倍物质的量时收率最高.In the synthesis of 2-（4-fluorophenyl）thiophene（2）,the 1-bromo-4-fluorobenzene and 2-bromothiophenewas used as starting material,the highest yield was obtained when reaction time was 8 h at 20 ℃;2 and 5-bromo-2-methylbenzoic acid was used to prepare 5-bromo-2-methylphenyl-2-（4-fluorophenyl）thiophene ketone（4）,thehighest yield was obtained when reaction time was 10 h at 20 ℃ ;in the preparation of 2-（5- bromo- 2-methylbenzyl）-5-（4-fluorophenyl）thiophene（1）,the best mole ratio of Zn dust to 4 was 3∶1 and the favorabletemperature was 100 ℃.

关 键 词：卡格列净 中间体 合成 

分 类 号：R971.1[医药卫生—药品]