摘要
2-羟基-3-甲氧基-3,3-二苯基丙酸经拆分得到粗品(S)-2-羟基-3-甲氧基-3,3-二苯基丙酸后,与4,6-二甲基-2-甲磺酰基嘧啶在氢氧化锂一水合物存在条件下发生亲核反应,经氨气成盐精制得到肺动脉高压治疗药安贝生坦,总收率约32%。
Ambrisentan for the treatment of pulmonary arterial hypertension was synthesized from 2-hydroxy- 3-methoxy-3,3-diphenylpropionic acid via resolution to give the crude （S）-2-hydroxy-3-methoxy-3,3-diphenylpropionic acid, which was subjected to condensation with 4,6-dimethyl-2-methylsulfonyl pyrimidine in the presence of lithium hydroxide monohydrate and purification by salt formation with ammonia with an overall yield about 32 %.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2015年第11期1165-1166,共2页
Chinese Journal of Pharmaceuticals
关键词
安贝生坦
肺动脉高压
合成
氢氧化锂一水合物
ambrisentan
pulmonary arterial hypertension
synthesis
lithium hydroxide monohydrate
