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Synthesis 2010(24): 4193-4198
DOI: 10.1055/s-0030-1258298
DOI: 10.1055/s-0030-1258298
PAPER
© Georg Thieme Verlag
Stuttgart ˙ New York
Microwave-Assisted Synthesis of KN-93, a Potent and Selective Inhibitor of Ca²+/Calmoduline-Dependent Protein Kinase II
Further Information
Received
1 July 2010
Publication Date:
14 October 2010 (online)
Publication History
Publication Date:
14 October 2010 (online)
Abstract
Convenient synthetic routes to KN-93, N-(2-{[[(2E)-3-(4-chlorophenyl)prop-2-enyl](methyl)amino]methyl}phenyl)-N-(2-hydroxyethyl)-4-methoxybenzenesulfonamide, a well-known Ca²+/calmoduline-dependent protein kinase II (CaMKII) inhibitor, are described. The methods proposed start from easily available reagents and allow ready preparation of the final compound in moderate overall yields. Most of the synthetic steps proposed were microwave assisted.
Key words
Heck reaction - sulfonamides - enzymes - multicomponent reaction - medicinal chemistry
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