LETTER	Synlett 2006: 0460-0462   DOI: 10.1055/s-2006-926243
© Georg Thieme Verlag Stuttgart · New York
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 e-Mail: peter.sheldrake@icr.ac.uk; e-Mail: ted.mcdonald@icr.ac.uk.;
Received 8 November 2005

Abstract

Treatment of N,N-diformylaminomethyl aryl ketones with phosphorus pentasulfide/triethylamine in chloroform gives 5-arylthiazoles directly 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 in a ­parallel fashion.

Key words

heterocycles - 1,3-thiazole - lithiation - phosphorus ­pentasulfide