Minisci C–H Alkylation of Heterocycles with Unactivated Alkyl Iodides Enabled by Visible Light Photocatalysis

In this work, we developed a general catalytic strategy
that allows
Minisci C–H alkylation of a variety of heterocycles using unactivated
alkyl halide as an alkyl radical source under visible light photocatalysis.
Mild reaction conditions, employing 4CzIPN as an organophotocatalyst
and aerial oxygen as a green terminal oxidant, a broad scope, good
functional group tolerance, and late-stage C–H alkylation of
bioactive and pharmaceutically relevant molecules are advantages of
the protocol. Preliminary mechanistic studies indicate the involvement
of the α-amino alkyl radical and the alkyl radical and further
involvement of aerial oxygen under our reaction conditions.