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Synthesis of novel 5-substituted pyrazole derivatives as cannabinoid antagonists

Alekseeva, OO., Mahadevan, A., Wiley, J., Martin, BR., & Razdan, RK. (2005). Synthesis of novel 5-substituted pyrazole derivatives as cannabinoid antagonists. Tetrahedron Letters, 46(12), 2159-2161.

Abstract

A facile seven-step sequence was developed from 4'-bromopropiophenone, utilizing a Suzuki-type coupling with an alkene, to give several novel 5-substituted pyrazole derivatives in overall yields of 11-31%. They are potent CB1 antagonists and have binding affinities similar to SR 141716A. Like SR 141716A, they may prove to be clinically useful for the treatment of obesity. (C) 2005 Elsevier Ltd. All rights reserved

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