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Synfacts 2011(10): 1044-1044  
DOI: 10.1055/s-0030-1261041
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of Glucokinase Activator MK-0941

Contributor(s): Philip Kocienski
N. Yoshikawa*, F. Xu*, J. D. Arredondo, T. Itoh
Merck Research Laboratories, Rahway, USA
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Publication History

Publication Date:
20 September 2011 (online)

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Significance

Glucokinase is an enzyme located primarily in the liver and pancreatic β-cells that catalyzes the phosphorylation of glucose to glucose-6-phosphate. It plays a key role in regulating hepatic glucose production. MK-0941 is a gluco-kinase activator that was of interest for the treatment of type II diabetes. The short, large-scale synthesis depicted features sequential O-arylation and O-alkylation of the resorcinol derivative A.