C3 Functionalization of Indolizines via HFIP-Promoted Friedel-Crafts Reactions with (Hetero)arylglyoxals

通过HFIP促进的傅克反应,利用(杂)芳基乙二醛对吲哚嗪进行C3官能化。

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Abstract

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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