Tetrahedron

Regioselective synthesis of 1, 3, 5-and 1, 3, 4, 5-substituted pyrazoles via acylation of N-Boc-N-substituted hydrazones

A Tinarelli, P Righi, G Rosini, D Andreotti, R Profeta…

Index: Tinarelli, Alessandro; Righi, Paolo; Rosini, Goffredo; Andreotti, Daniele; Profeta, Roberto; Spada, Simone Tetrahedron, 2011 , vol. 67, # 3 p. 612 - 617

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Citation Number: 10

Abstract

Acylation of N-Boc-N-methylhydrazones followed by TFA treatment affords regioselective access to substituted pyrazoles. Both regioisomers of 1-methyl-3, 5-disubstituted-1H- pyrazoles can be selectively obtained. This procedure can also be employed for the regioselective preparation of fully substituted 1H-pyrazoles.