标题:
Abemaciclib合成路线图解Graphical Synthetic Routes of Abemaciclib
作者:
张浩, 陈奉泉, 张剑
关键字:
Abemaciclib, 合成, CDK4/6Abemaciclib, Synthesis, CDK4/6
期刊名称:
《Hans Journal of Medicinal Chemistry》, Vol.4 No.4, 2016-11-28
摘要:
Abemaciclib (Bemaciclib, LY-2835219)化学名称为N-[5-[(4-乙基-1-哌嗪)甲基]2-吡啶基]-5-氟-4-[4-氟-1-异丙基-2-甲基-1H-苯并咪唑-6-基]-2-嘧啶胺，是礼来公司研发的细胞周期蛋白依赖性激酶(cyclin-dependent kinase, CDK)4/6抑制剂。其单一用药对转移性乳腺癌有显著疗效，于2015年10月被美国FDA授予“突破性疗法”认证。本文综述了Abemaciclib及关键中间体的合成。
Abemaciclib (Bemaciclib, LY-2835219), whose chemical name is N-[5-[(4-ethyl-1-piperazinyl) methyl]-2-pyridinyl]-5-fluo-ro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]-2- pyrimidinamine, is a significant inhibitor of the cyclin-dependent kinase (CDK) 4/6 researched by Lilly, showing single-agent activity in metastatic breast cancer. Abemaciclib was granted “Breakthrough therapy designation” by the FDA in October 2015. In this paper, we summarized the synthesis of Abemaciclib and key intermediate.