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Synfacts 2010(11): 1212-1212  
DOI: 10.1055/s-0030-1258709
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of a Glycogen Synthase Kinase-3 Inhibitor

Contributor(s): Philip Kocienski
N. A. Magnus*, C. P. Ley, P. M. Pollock, J. P. Wepsiec
Eli Lilly and Company, Indianapolis, USA
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Publikationsdatum:
21. Oktober 2010 (online)

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Significance

Glycogen synthase kinase-3 (GSK-3) is involved in signaling from the insulin receptor and inhibitors of it are expected to lower plasma glucose similar to insulin. It is under development for the treatment of type 2 diabetes. The target bisarylmaleimide was synthesized in seven steps in 33% overall yield from 5-fluoroindole (A).