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

초록

We 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.

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