Tetrahedron

Regiocontrolled synthesis of 3-and 5-aminopyrazoles, pyrazolo [3, 4-d] pyrimidines, pyrazolo [3, 4-b] pyridines and pyrazolo [3, 4-b] quinolinones as MAPK inhibitors

MC Bagley, M Baashen, VL Paddock, D Kipling…

Index: Bagley, Mark C.; Baashen, Mohammed; Paddock, Victoria L.; Kipling, David; Davis, Terence Tetrahedron, 2013 , vol. 69, # 39 p. 8429 - 8438

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Citation Number: 10

Abstract

Abstract Microwave irradiation of a hydrazine and 3-methoxyacrylonitrile, ethoxymethylenemalononitrile or ethyl acetoacetate provides rapid access to 3-or 5- substituted pyrazoles in excellent yield and with total regiocontrol in a process that can be switched from one regioisomer to the other by choice of conditions. Subsequent reaction, either by microwave-assisted hydrolysis and cyclocondensation with formamide, Hantzsch ...