非对映选择性合成 GK-GKRP 破坏剂 AMG-3969。
Nonracemic synthesis of GK-GKRP disruptor AMG-3969.
机构信息
Therapeutic Discovery, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.
出版信息
J Org Chem. 2014 Apr 18;79(8):3684-7. doi: 10.1021/jo500336e. Epub 2014 Apr 10.
PMID:24678849
Abstract
A nonracemic synthesis of the glucokinase-glucokinase regulatory protein disruptor AMG-3969 (5) is reported. Key features of the synthetic approach are an asymmetric synthesis of the 2-alkynyl piperazine core via a base-promoted isomerization and a revised approach to the synthesis of the aminopyridinesulfonamide with an improved safety profile.
摘要
报道了葡萄糖激酶-葡萄糖激酶调节蛋白变构抑制剂 AMG-3969（5）的非对映体合成。该合成方法的关键特点是通过碱促进的异构化实现 2-炔基哌嗪核心的不对称合成，以及改进的安全概况下合成氨基吡啶磺酰胺的方法。
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