One‐Pot Synthesis of Highly Substituted 1H‐Pyrazole‐5‐carboxylates from 4‐Aryl‐2,4‐diketoesters and Arylhydrazines

Abstract

A one‐pot synthesis of highly substituted 1H‐pyrazole‐5‐carboxylates 1 has been developed starting from easily available 4‐aryl‐2,4‐diketoesters 2 and arylhydrazine hydrochlorides 3. More active 2‐carbonyl group of 2 was blocked with methoxyamine hydrochloride to give 2‐methoxy imine intermediates, which were then subjected to condensation cyclization with 3 in situ to provide the desired products 1. In addition, the geometrical configuration of 1aa was unambiguously confirmed by single crystal X‐ray crystallography.