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Molecules 2012, 17(4), 4533-4544; doi:10.3390/molecules17044533

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

1,2, 2, 2, 2, 2, 1,*  and 2,*
1 School of Chemistry and Molecular Engineering, East China University of Science and Technology, Shanghai, 200237, China 2 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.
Keywords: solvent-free; chlorination; phosphorous oxychloride (POCl3) solvent-free; chlorination; phosphorous oxychloride (POCl3)
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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