Highly Atroposelective Synthesis of Arylpyrroles by Catalytic Asymmetric Paal-Knorr Reaction

J Am Chem Soc. 2017 Feb 8;139(5):1714-1717. doi: 10.1021/jacs.6b09634. Epub 2017 Jan 26.

Abstract

A general and efficient method for accessing enantiomerically pure arylpyrroles by utilizing the catalytic asymmetric Paal-Knorr reaction has been developed for the first time. A wide range of axially chiral arylpyrroles were obtained in high yields with good to excellent enantioselectivities. The key to success is the use of the combined-acid catalytic system involving a Lewis acid and a chiral phosphoric acid for achieving effective enantiocontrol. Noteworthy is that an unexpected solvent-dependent inversion of the enantioselectivity was observed in the above-mentioned asymmetric reaction.

Publication types

  • Research Support, Non-U.S. Gov't