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Note | Regular issue | Vol 55, No. 4, 2001, pp.753-761
Published online, 1st January, 1970
DOI: 10.3987/COM-00-9104
A Facile Synthesis and Chemical Properties of 3,4-Dihydro-2H-1,5,2-benzo[f]dithiazepin-3-ones with Potential Anticancer Activity

Elzbieta Pomarnacka,* Anita Kornicka, and Franciszek Saczewski

*Department of Chemical Technology of Drug, Medical University of Gdansk, 107 Gen. J. Hallera Str., 80-416 Gdansk, Poland

Abstract

The syntheses of 3,4-dihydro-2H-1,5,2-benzo[f]dithiazepin-3-one 1,1-dioxides (8-11, 14, 17-20) and corresponding 1,1,5,5-tetraoxides (12, 13) are described. Reactivity of these compounds in their alcoholysis, alkaline hydrolysis and alkylation is also reported. Evaluation performed at the US National Cancer Institute (Bethesda) revealed the in vitro antitumor activity of 7-chloro-3,4-dihydro-8-methyl-4-phenyl-2H-1,5,2-benzo[f]dithiazepin-3-one 1,1-dioxide (11).