Synthesis of (+)-ambrisentan
10.11665/j.issn.1000-5048.20170307
- VernacularTitle:安立生坦的合成研究
- Author:
Qingyang ZHANG
;
Jiuan LYU
;
Haiyu HU
- Keywords:
ambrisentan;
L-phenylglycinamide;
resolution reagent;
pulmonary arterial hypertension;
synthesis;
process improvement
- From:
Journal of China Pharmaceutical University
2017;48(3):293-296
- CountryChina
- Language:Chinese
-
Abstract:
A five-step synthetic method of ambrisentan starting from benzophenone was developed.The reaction methods of resolution and substitution were optimized.A stable,facilitating method of detection and efficient resolution reagent,L-phenylglycinamide,was used and helped to obtain highly optical pure intermediates.In the substitution reaction,NaOH was chosen as the base,which is safe and suitable for the industry.This method was mild,easily operated with a total yield up to 31.0％,and may have a good application prospect.
