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Nonracemic Synthesis of GK–GKRP Disruptor AMG-3969

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journal contribution
posted on 18.04.2014, 00:00 by Matthew P. Bourbeau, Kate S. Ashton, Jie Yan, David J. St. Jean
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.