Iniparib的合成

Synthesis of Iniparib

对氨基苯甲酸经酰化、硝化、水解、重氮化及碘代反应制得4-碘-3-硝基苯甲酸,再依次与氯化亚砜、氨水反应生成聚腺苷二磷酸核糖聚合酶抑制剂iniparib,总收率约35%。

Iniparib, a poly-ADP-ribose polymerase inhibitor, was synthesized from 4-aminobenzoic acid by acetylation, nitration, hydrolysis, diazotization and iodination to give 4-iodo-3-nitrobenzoic acid, which was subjected to reaction with SOC12 and ammonium hydroxide successively with an overall yield of about 35 %,