HJMCe  >> Vol. 4 No. 4 (November 2016)

    Graphical Synthetic Routes of Abemaciclib

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张 浩,张 剑:潍坊医学院药学院医用化学教研室,山东 潍坊;
陈奉泉:山东大学药学院药物化学教研室,山东 济南

Abemaciclib合成CDK4/6Abemaciclib Synthesis CDK4/6


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.

张浩, 陈奉泉, 张剑. Abemaciclib合成路线图解[J]. 药物化学, 2016, 4(4): 38-41. http://dx.doi.org/10.12677/HJMCe.2016.44005


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