Microwave-assisted and continuous flow multistep synthesis of 4-(pyrazol-1-yl) carboxanilides

D Obermayer, TN Glasnov…

Index: Obermayer, David; Glasnov, Toma N.; Kappe, C. Oliver Journal of Organic Chemistry, 2011 , vol. 76, # 16 p. 6657 - 6669

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Citation Number: 47

Abstract

A series of 4-(pyrazol-1-yl) carboxanilides active as inhibitors of canonical transient receptor potential channels were synthesized in an efficient three-step protocol using controlled microwave heating. The general synthetic strategy involves condensation of 4- nitrophenylhydrazine with appropriate 1, 3-dicarbonyl building blocks, followed by reduction of the nitro group to the amine, which is then amidated with carboxylic acids. Compared to ...