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Facile Generation of a Library of 5-Aryl-2-arylsulfonyl-1,3-thiazoles

Peter W. Sheldrake*, Mizio Matteucci, Edward McDonald*

*Medicinal Chemistry Team, The Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, Belmont, Sutton, Surrey SM2 5NG, UK, Email:,

P. W. Sheldrake, M. Matteucci, E. McDonald, Synlett, 2006, 460-462.

DOI: 10.1055/s-2006-926243

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Treatment of N,N-diformylaminomethyl aryl ketones with phosphorus pentasulfide and triethylamine in chloroform gives 5-arylthiazoles in good yield. The 5-aryl-1,3-thiazole core has been successfully functionalised at the 2-position to yield, over two steps, a large array of 5-aryl-2-arylsulfonyl-1,3-thiazoles.

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Key Words

heterocycles, 1,3-thiazoles, phosphorus pentasulfide

ID: J60-Y2006-4270