摘要
目的:合成抗2型糖尿病药物那格列奈。方法:以对异丙基苯甲醛为原料,经氧化、催化氢化、在高温高压碱性条件下,将顺式-对异丙基环已甲酸异构化为反武．异构体,然后与D-苯丙氨酸甲酯盐酸盐缩合、水解,合成那格列奈。结果:反应中间体以及目标产物的化学结构均经过了光谱分析确证,反应总收率为28．7％。结论:本方法步骤简单,易于工业化生产。
Objective：To synthesize nateglinide, an anti-type 2 diabetic agent. Methods： Starting from 4-isopropylbenzaldehyde, trans-4-isopropylcyclohexanecarboxylic acid was isomerized to cis-isomer via oxidation, catalytic hydrogenation and then high temperature and high pressure in alkali aqueous. Nateglinide was synthesized after the cis-isomer was reacted with D-phenylalanine and hydrolysis. Results： The structures of intermediates and the target product were verified by spectroscopic analysis. The overall yield was 28.7%. Conclusion： The simplified method to synthesize nateglinide was warranted to have further pilot manufacture.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2006年第18期1564-1566,共3页
Chinese Journal of New Drugs
基金
广东省自然科学基金(4300235)
