Direct synthesis of pyrazoles from esters using tert-butoxide-assisted C-(C=O) coupling

Abstract

This paper describes the direct synthesis of pyrazoles from esters that comprises two sequential reactions: tert-butoxide-assisted C-C(=O) coupling reaction to yield beta-ketonitrile or alpha,beta-alkynone intermediates, and condensation by hydrazine addition. The method reported allows for easy control of the regioselectivity and structure of substituents at N-1, C-3, C-4 and/or C-5 positions.