jo500336e_si_001.pdf (2.04 MB)
Nonracemic Synthesis of GK–GKRP Disruptor AMG-3969
journal contribution
posted on 2014-04-18, 00:00 authored by Matthew P. Bourbeau, Kate S. Ashton, Jie Yan, David
J. St. JeanA 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.