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Facile amidinations of 2-aminophenylboronic acid promoted by boronate ester formation†
Brighid B. Pappin,Taylor A. Garget,Peter C. Healy,Michela I. Simone
Organic & Biomolecular Chemistry Pub Date : 01/03/2019 00:00:00 , DOI:10.1039/C8OB02696C
Abstract

Amidine synthesis by amine addition to nitriles normally requires high temperatures or harsh catalysts. Here, we report that boronate esters can facilitate amidination of proximal amines with moderate heating. With amidines present in a number of drugs and the synthetic handle provided by the boron, this chemistry should find useful applications.

Graphical abstract: Facile amidinations of 2-aminophenylboronic acid promoted by boronate ester formation
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