Rhodium-Catalyzed N-Arylation Addition of Arylboronic Acids to Ketimines

Abstract

Herein, we report rhodium catalyzed N-arylation via addition of arylboronic acids to electron-deficient α-iminoesters which can be prepared in high efficiency by using easily accessible β-carbonyl esters. The reaction is highly regiospecific to achieve the N-aryl addition efficiently with up to 99% yield under mild conditions. The corresponding product can be further efficiently converted into indoles and a series of other important building blocks.

Keywords

Rhodium catalyzed / N-Arylation addition / Amines / Umpolung / Indole / C—C coupling

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