中国药科大学学报2017，Vol.48Issue(3)：293-296,4.DOI:10.11665/j.issn.1000-5048.20170307
安立生坦的合成研究
Synthesis of (+)-ambrisentan
张青扬 1吕久安 2胡海宇1
作者信息
- 1. 中国医学科学院、北京协和医学院药物研究所,活性物质发现与适药化研究北京重点实验室,北京100050
- 2. 北京红惠新医药科技有限公司,北京102600
- 折叠
摘要
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.关键词
安立生坦/L-苯甘氨酰胺/拆分试剂/肺动脉高血压/合成/工艺改进Key words
ambrisentan/L-phenylglycinamide/resolution reagent/pulmonary arterial hypertension/synthesis/process improvement分类
医药卫生引用本文复制引用
张青扬,吕久安,胡海宇..安立生坦的合成研究[J].中国药科大学学报,2017,48(3):293-296,4.
