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Finn, R.S., Aleshin, A. and Slamon, D.J. (2016) Targeting the Cyclin-Dependent Kinases (CDK) 4/6 in Estrogen Receptor-Positive Breast Cancers. Breast Cancer Research, 18, 17.


  • 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.