卡格列净关键中间体合成研究

摘要

In the synthesis of 2-(4-fluorophenyl)thiophene(2),the 1-bromo-4-fluorobenzene and 2-bromothiophene was 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),the highest 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 favorable temperature was 100℃.%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。