Type 2 diabetes is a rapidly expanding public health problem affecting over 220 million people worldwide. One promising area of current research involves small-molecule allosteric activators of the glucokinase (GK) enzyme to lower blood glucose and normalize insulin secretion. Herein we report the syntheses of glucokinase activators containing nitrogen linked 5- and 6- membered heterocycles as represented by structures I and II, respectively. During this work a novel method for the synthesis of 4-sulfonyl-2-pyridones was developed. Additionally, selective N alkylation reaction conditions were optimized to allow for regio- and steroselective synthesis of I and II . 

Synthetic challenges in the discovery of heterocyclic glucokinase activators for treatment of diabetes

242nd National Meeting (2011)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.