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Issue 4, 2019
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Facile amidinations of 2-aminophenylboronic acid promoted by boronate ester formation

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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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Publication details

The article was received on 31 Oct 2018, accepted on 02 Jan 2019 and first published on 03 Jan 2019


Article type: Communication
DOI: 10.1039/C8OB02696C
Citation: Org. Biomol. Chem., 2019,17, 803-806
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    Facile amidinations of 2-aminophenylboronic acid promoted by boronate ester formation

    B. B. Pappin, T. A. Garget, P. C. Healy, M. I. Simone, M. J. Kiefel and T. A. Houston, Org. Biomol. Chem., 2019, 17, 803
    DOI: 10.1039/C8OB02696C

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