Thermodynamic Controlled Regioselective C1-Functionalization of Indolizines with 3-Hydroxyisoindolinones via Brønsted Acid Catalyzed aza-Friedel-Crafts Reaction.

A Brønsted acid catalyzed aza-Friedel-Crafts reaction of indolizines with 3-hydroxyisoindolinones has been established, which constructs isoindolinone derivatives bearing a tetrasubstituted stereocenter in good to high yields and enantioselectivities. Notably, this strategy provides a new access to C1-functionalization of indolizines with excellent regioselectivities. Moreover, this intriguing C1-regioselective transformation was induced under thermodynamic control.