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.
出处
《药物化学》
2016年第4期38-41,共4页
Hans Journal of Medicinal Chemistry
基金
山东省自然科学基金(BS2015YY016)。
