摘要
Rucaparib是首个进入临床实验的聚腺苷二磷酸核糖聚合酶(PARP)抑制剂。笔者以5-氟-2-甲基苯甲酸为起始原料经过12步反应得到Rucaparib。这是一条安全低毒、操作简易的全新合成路线,总收率达5.38%,其中间体及最终产物结构均经过MS和1H NMR确证。
Rucaparib is the first PARP inhibitor which entered into the clinical trial.It was prepared in 5.38% overall yield in 12 steps by using 5-fluoro-2-methylbenzoic acid as the starting material.The synthetic process was designed as a novel method with less toxicity and easy operation.The structures of the intermediates and the final product were identified with MS and 1H NMR.
出处
《精细化工中间体》
CAS
2012年第5期48-52,共5页
Fine Chemical Intermediates
基金
中央高校基本科研业务费专项资金资助(JKY2011062)
