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Highly Regioselective Organocatalytic SNAr Amination of 2,4-Dichloropyrimidine and Related Heteroaryl Chlorides

Lovelle, Lucie (2017) Highly Regioselective Organocatalytic SNAr Amination of 2,4-Dichloropyrimidine and Related Heteroaryl Chlorides. European journal of organic chemistry. pp. 3222-3228. ISSN 1099-0690; 1434-193X

Abstract

A highly efficient and regioselective method for the SNAr amination of 2,4-dichloropyrimidine with oxazolidin-2-one and related weakly nucleophilic amines is disclosed using sodium sulfinate and tetrabutylammonium bromide as catalysts. The presented strategy facilitates the synthesis of various aminopyrimidines in a regio- and chemoselective manner. Furthermore, this approach was successfully applied to the amination of various activated N-heteroaromatic substrates.

Item Type: Article
Date Deposited: 27 Jun 2017 00:45
Last Modified: 27 Jun 2017 00:45
URI: https://oak.novartis.com/id/eprint/32016

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