1562-31-8

Four vinyl sulfonate ester derivatives, methyl ethenesulfonate (MES), ethyl ethenesulfonate (EES), 2,2,2-trifluoroethyl ethenesulfonate (TFES), and 2,2,2-trichloroethyl ethenesulfonate (TCLES), which are protected forms of vinyl sulfonic acids, were polymerized by reversible addition-fragmentation chain transfer (RAFT) polymerization. Polymers having relatively narrow molecular weight distributions and pre-determined molecular weights were obtained by the polymerization of all monomers using a suitable xanthate-type chain transfer agent (CTA). The RAFT polymerizations of EES and TCLES were found to proceed in controlled fashions under suitable conditions, as confirmed by the formation of narrow polydispersity products, molecular weights controlled by the monomer/chain transfer agent ratio, and linear increases in molecular weight with conversion. Deprotection of the ethyl group of poly(EES) by LiBr in refluxing 2-butanone proceeded smoothly to give water-soluble poly(lithium vinyl sulfonate). Poly(potassium vinyl sulfonate) was also obtained by the deprotection of poly(TCLES) using potassium tert-butoxide. The syntheses of thermoresponsive block copolymers involving poly(lithium vinyl sulfonate) segments were conducted by RAFT polymerization of N-isopropylacrylamide using poly(EES) macro-CTA, followed by deprotection. The thermally-induced phase separation behavior and assembled structures of the block copolymers were also studied in aqueous solution.

There is provided a means to produce industrially a highly pure 2-hydroxy-4-oxa-5-thiatricyclo[4.2.1.03,7]nonane 5,5-dioxide derivative in high yield from highly pure and industrially available raw materials. The production method for a sultone derivative of the present invention comprises a step (A) to obtain a sulfonic acid derivative by hydrolyzing a sulfonyl halide derivative represented by the following chemical formula 1: or an enantiomer thereof and a step (B) to obtain a corresponding sultone derivative represented by the following chemical formula 2: or an enantiomer thereof by treating the sulfonic acid derivative with a oxidizing agent.

The inhibition of NAD synthesis or salvage pathways has been proposed as a novel target for antitumoral drugs. Two molecules with this mechanism of action are at present undergoing clinical trials. In searching for similar novel molecules, we exploited co

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