Issue 14, 2018

Palladium-catalyzed primary amine-directed regioselective mono- and di-alkynylation of biaryl-2-amines

Abstract

The first example of the palladium-catalyzed primary amine-directed C(sp2)–H alkynylation of biaryl-2-amines has been developed by using (bromoethynyl)triisopropylsilane as an alkynylating reagent. This protocol exhibits a broad substrate scope, excellent regioselectivity and gram-scale synthesis. Significantly, the versatility of this straightforward method was further demonstrated by controlled mono- and di-alkynylation.

Graphical abstract: Palladium-catalyzed primary amine-directed regioselective mono- and di-alkynylation of biaryl-2-amines

Supplementary files

Article information

Article type
Communication
Submitted
11 Dec 2017
Accepted
21 Jan 2018
First published
22 Jan 2018

Chem. Commun., 2018,54, 1746-1749

Palladium-catalyzed primary amine-directed regioselective mono- and di-alkynylation of biaryl-2-amines

G. Jiang, W. Hu, J. Li, C. Zhu, W. Wu and H. Jiang, Chem. Commun., 2018, 54, 1746 DOI: 10.1039/C7CC09308J

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