Nonracemic Synthesis of GK鈥揋KRP Disruptor AMG-3969

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• 作者：Matthew P. Bourbeau ; Kate S. Ashton ; Jie Yan ; David J. St. Jean ; Jr.
• 刊名：Journal of Organic Chemistry
• 出版年：2014
• 出版时间：April 18, 2014
• 年：2014
• 卷：79
• 期：8
• 页码：3684-3687
• 全文大小：231K
• 年卷期：v.79,no.8(April 18, 2014)
• ISSN：1520-6904

文摘

A nonracemic synthesis of the glucokinase鈥揼lucokinase 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.