奥拉帕尼合成路线图解

Graphical synthetic routes to olaparib

奥拉帕尼(olaparib,1),化学名4-[3-(4-环丙基羰基-哌嗪-1-羰基)-4-氟-苄基]-2H-酞嗪-1-酮[1](分子式:C24H23FN4O3,分子量:434.4630),商品名Lynparza,为小分子口服ADP聚合酶(PARP1)抑制剂。2014年经美国FDA批准用于治疗基因缺陷相关的晚期卵巢癌(BRCA)[2],此外,奥拉帕尼具有选择性地抑制共济失调毛细血管扩张症基因(ATM)缺陷的肿瘤细胞增殖的作用[3]。

Olaparib(Lynparza) w as the inhibitor of poly (ADP-ribose)polymerase(PARP) enzymes that had been recently approved for the treatment of ovarian cancer.The article summarized the synthesis of olaparib and its key intermediates based on different starting materials and synthetic routes.