An Efficient Synthesis of 1,3‐Disubstituted Pyrazoles from 2‐Acylaziridines

Abstract

AbstractWe developed an efficient and environmentally benign method for pyrazole synthesis by condensation between 2‐acylaziridines and hydrazine‐CO2 salts in high yields. The sequential reactions involved include an acid‐catalyzed intramolecular aziridine ring opening and a subsequent benzylamine elimination. In additional to the ease of handling the hydrazine as a solid without any smell, all of the processes were carried out with no organic solvent, except for a small amount of phenol as an acid catalyst.