Modular Synthesis of Polysubstituted Quinolin-3-amines by Oxidative Cyclization of 2-(2-Isocyanophenyl)acetonitriles with Organoboron Reagents

Abstract

Polysubstituted quinolin-3-amines are vital structural motifs because of their broad biological activities as well as versatile transformational abilities. However, they are not easily accessible. We disclose a protocol with Mn(III) acetate as a mild one-electron oxidant promoting a radical process to construct polysubstituted quinolin-3-amines. 2-(2-Isocyanophenyl)acetonitriles and organoboron reagents are suitable substrates for this reaction. The remarkable advantages of this protocol are the practical method, mild approach, high reaction efficiency, and good compatibility of functional groups, providing straightforward access to functional quinoline derivatives.

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