Abstract

The stereoselective one-pot synthesis of polysubstituted 1,4-diazepine derivatives has been achieved via a new solvent- and catalyst-free multicomponent domino reaction from β-ketoamides. This green and experimentally simple sequence is conducted from easily accessible achiral starting materials, does not require any harmful reagents, and results in a high increase in molecular complexity and diversity. Moreover, water is the only byproduct liberated during the reaction.

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