Herein, we develop a mild method for -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 from benzil under UV irradiation.
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| http://dx.doi.org/10.1021/acs.orglett.1c01599 | DOI Listing |
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