A highly efficient
Friedel–Crafts type hydroxyalkylation
at the C3 position of indolizines with (hetero)arylglyoxals has been
achieved by the action of hexafluoroisopropanol (HFIP) under mild
reaction conditions, leading to direct access to a variety of polyfunctionalized
indolizines in excellent yields. Installation of more diverse functional
groups at the C3 site of indolizine scaffold was realized via further
elaboration of the resulting α-hydroxyketone moiety, allowing
for expansion of indolizine chemical space.
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