SYNTHESIS OF A LIBRARY OF 1,5,2-DITHIAZEPINE 1,1-DIOXIDES. PART 1: A ONE-POT SULFONYLATION/THIA-MICHAEL PROTOCOL

[摘要]：A novel one-pot sulfonylation/intramolecular thia-Michael protocol is reported for the synthesis of 1,5,2-dithiazepine 1,1-dioxides. Sulfonylation between cysteine ethyl ester/cysteamine and 2-chloroethanesulfonyl chloride, followed by in situ intramolecular thia-Michael addition, was achieved and afforded the titled 1,5,2-dithiazepine-1,1-dioxide scaffolds. Diversification was demonstrated for future library synthesis.

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