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Communication | Regular issue | Vol 48, No. 12, 1998, pp.2485-2488
Published online, 1st January, 1970
DOI: 10.3987/COM-98-8351
Substitutions at the Thiazole Moiety of Epothilone

Michael Sefkow* and Gerhard Höfle

*Gesellschaft fur Biotechnologische Forschung mbH, Mascheroder Weg 1, D-38124 Braunschweig, Germany

Abstract

Epothilone A is metalated at low temperature with an excess of butyllithium preferentially at C19 of the thiazole moiety. After addition of various carbon and heteroatom electrophiles the corresponding substitution products were obtained. Some of them have similar cytotoxic activity than the starting material.