Brønsted-acid-catalyzed selective Friedel-Crafts monoalkylation of isatins with indolizines in water

Org Biomol Chem. 2020 Sep 30;18(37):7330-7335. doi: 10.1039/d0ob01714k.

Abstract

The controlled mono-addition of indolizines to isatins under very mild conditions is described. The reaction occurs in water using diphenylphosphate as the catalyst, which is dramatically accelerated by surfactant addition. 3-Hydroxy-3-indolizinyl-2-oxindole scaffolds were synthesized in up to >99% yield. Notably, in organic solvents only bis-addition products were observed.

Publication types

  • Research Support, Non-U.S. Gov't