Lithium Chloride Catalyzed Aza-Michael Addition of Pyrazoles to α,β-Unsaturated Imides

Abstract

A lithium chloride catalyzed aza-Michael reaction of pyrazoles to α,β-unsaturated imides has been developed. A range of aromatic and aliphatic α,β-unsaturated imides are found to be suitable for the established method, providing the corresponding aza-Michael adducts in up to 93% yields. The inexpensive catalyst, good substrate tolerance, and ease of scale-up make this procedure highly practical.

Key words

Michael addition - α,β-unsaturated imides - pyrazoles - nitrogen heterocycles - regioselectivity

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