抗肿瘤药Galunisertib的合成

Synthesis of Antitumor Agent Galunisertib

以4-氨基苯甲腈为起始原料,依次经胺醇交换、脱水环合、酯缩合、氨化环合及水解等5步反应合成Galunisertib,其结构经1HNMR和MS确证,总收率56.2%,纯度99.63%。

Galunisertib was synthesized from 4 - aminobenzonitrile as starting material by a five - step reaction of amine - alcohol exchange, dehydration eyelization, condensation, amination - eyelization and hydrolysis. The structure was eolffirmed by 1 H - NMR and MS. The total yield and purity- were 56.2% and 99.63% respectively.