[R-(R',S')]-[(2-甲基-1-丙酰氧基丙氧基)(4-苯基丁基)氧膦基]乙酸的合成

Synthesis of [R-(R~*,S~*)]-[(2-Methyl-1-propionyloxypropoxy)-(4-phenylbutyl)phosphinyl]acetic acid

选用苄基氯 ,经过芳香族烯烃的游离基加成、缩合、氢解脱苄基等反应以及光学异构体的拆分 ,合成了福辛普利 ( fosinopril)的重要中间体 [R- ( R* ,S* ) ]- [( 2 -甲基 - 1 -丙酰氧基丙氧基 ) ( 4 -苯基丁基 )氧膦基 ]乙酸 。

A key intermediate, [R (R *,S *)] [(2 methyl 1 propionyloxypropoxy) (4 phenylbutyl) phosphinyl]acetic acid, of fosinopril was synthesized from benzyl chloride by free radical addition of aryl olefin, condensation, debenzylation and resolution of the optical isomers.