UV-Light-Induced N-Acylation of Amines with α-Diketones

Abstract

Herein, we develop a mild method for <i>N</i>-acylation of primary and secondary amines with α-diketones induced by ultraviolet (UV) light. Forty-six examples with various functional groups are explored at room temperature with irradiation by three 26 W UV lamps (350-380 nm). The yield reaches 97%. The gram scale experiment product yield is 76%. Moreover, this system can be applied to the synthesis of several amino acid derivatives. Mechanistic studies show that benzoin is generated <i>in situ</i> from benzil under UV irradiation.