聚腺苷二磷酸核糖聚合酶抑制剂Rucaparib的合成研究  

Synthesis of Rucaparib——A Poly(ADP-ribose)Polymerase Inhibitor

作　　者：耿元硕[1] 胡珀[1] 王欣[1] 刘超[1] 李志裕[1] 

机构地区：[1]中国药科大学药物化学教研室,江苏南京210009

出　　处：《精细化工中间体》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)

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.

关 键 词：PARP抑制剂 Rucaparib 合成 

分 类 号：R737.902[医药卫生—肿瘤]