Catalyst- and solvent-free regioselective ring opening of aziridines with amines: application in the gram-scale synthesis of the α,β-diamino propionic derivative, aspergillomarasmine A

Abstract

A green and efficient approach for synthesizing α,β-diamino propionic derivatives was developed through the ring opening of α-C-alkyloxycarbonyl aziridine. This method features catalyst- and solvent-free conditions, high regioselectivity, and wide substrate scope including solid amines, and realizes the gram-scale synthesis of aspergillomarasmine A.