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Synfacts 2006(9): 0866-0866  
DOI: 10.1055/s-2006-942047
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Synthesis of Glucokinase Activators

Contributor(s): Philip Kocienski
S. Heuser*, D. G. Barrett, M. Berg, B. Bonnier, A. Kahl, M. L. De La Puente, N. Oram, R. Riedl, U. Roettig, G. S. Gil, E. Seger, D. J. Steggles, J. Wanner, A. G. Wiechert
Eli Lilly Reserach Laboratories, Hamburg, Germany, Lilly CPR&D, Mont-Saint-Guibert, Belgium; Lilly, Madrid, Spain; Lilly Research Centre, Windlesham, UK
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Publication History

Publication Date:
23 August 2006 (online)

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Significance

The target sulfonamide molecules (and their sulfone congeners) are potential drugs for the regulation of glucose levels by activation of glucokinase in the liver and pancreas. A markworthy step in the synthesis is the SNAr reaction (C to D) in which exchange of the Br by an SMe group was accompanied by S-demethylation. Transition-metal catalysis was not necessary.