Abstract

An I2/tert‐butyl hydroperoxide (TBHP)‐mediated [2+1+1+1] cycloadditions/oxidative aromatization reactions for the synthesis of indolizines using the one‐pot cascade process have been developed. A variety of aryl methyl ketones react with pyridine/isoquinoline and TBHP in the transition‐metal‐free reaction. This method utilizes readily available starting materials and TBHP acted in this reaction not only as oxidant and radical initiator but also as a methylene source, therefore providing a novel method of atom economy for the synthesis of indolizines.

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