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A new protocol is herein described for the direct generation of alkylated indolo/benzoimidazo[2,1-
a
]isoquinolin-6(5
H
)-one derivatives by using Hantzsch esters as alkylation radical precursors using a photoredox/K
2
S
2
O
8
system. This oxidative alkylation of active alkenes involves a radical cascade cyclization process and a sequence of Hantzsch ester single electron oxidation, C-C bond cleavage, alkylation, arylation and oxidative deprotonation.
A visible-light-promoted alkylation/cyclization of active alkenes
via
radical cascade cyclization for the preparation of functionalized isoquinolinones by using Hantzsch esters as alkylation radical precursors.