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Molecules 2012, 17(4), 4533-4544;

Large-Scale Solvent-Free Chlorination of Hydroxy-Pyrimidines, -Pyridines, -Pyrazines and -Amides Using Equimolar POCl3

School of Chemistry and Molecular Engineering, East China University of Science and Technology, Shanghai, 200237, China
College of Chemistry and Chemical Engineering, Shanghai University of Engineering Science, Shanghai, 201620, China
Authors to whom correspondence should be addressed.
Received: 7 March 2012 / Revised: 31 March 2012 / Accepted: 6 April 2012 / Published: 16 April 2012
(This article belongs to the Special Issue Solvent-Free Synthesis)
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Chlorination with equimolar POCl3 can be efficiently achieved not only for hydroxypyrimidines, but also for many other substrates such as 2-hydroxy-pyridines, -quinoxalines, or even -amides. The procedure is solvent-free and involves heating in a sealed reactor at high temperatures using one equivalent of pyridine as base. It is suitable for large scale (multigram) batch preparations. View Full-Text
Keywords: solvent-free; chlorination; phosphorous oxychloride (POCl3) solvent-free; chlorination; phosphorous oxychloride (POCl3)

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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Wang, H.; Wen, K.; Wang, L.; Xiang, Y.; Xu, X.; Shen, Y.; Sun, Z. Large-Scale Solvent-Free Chlorination of Hydroxy-Pyrimidines, -Pyridines, -Pyrazines and -Amides Using Equimolar POCl3. Molecules 2012, 17, 4533-4544.

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