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Treatment of N-t-butylbenzenesulfonamide with an excess of BuLi,followed by the reaction with methyl 2-(4-methylphe- nyl)propanoate,gave the corresponding 2-carboxybenzenesulfonamide,which underwent a sequence of consecutive N-deprotective cyclization process mediated by TMSCl-NaI-MeCN reagent to afford the N-sulfonylimine.Following the bromination and ring expansion,3-methyl-3-(4-methylphenyl)-2H-benzo[e][1,2]thiazine-1,1,4-trione was obtained.Optical resolution of the racemic benzosultam using(-)-menthoxyacetyl chloride,furnished the optically pure(+)-and(-)-3-methyl-3-(4-methylphenyl)-2H- benzo[e][1,2]thiazine-1,1,4-triones,which were fluorinated with FCIO_3 to produce the corresponding chiral N-F agents.
Treatment of Nt-butylbenzenesulfonamide with an excess of BuLi, followed by the reaction with methyl 2- (4-methylphe- nyl) propanoate, gave the corresponding 2-carboxybenzenesulfonamide, which underwent a sequence of consecutive N-deprotective cyclization process mediated by TMSCl- NaI-MeCN reagent to afford the N-sulfonylimine. Popular bromination and ring expansion, 3-methyl-3- (4-methylphenyl) -2H- benzo [e] [1,2] thiazine-1,1,4-trione was obtained. Optical resolution of the racemic benzosultam using (-) - menthoxyacetyl chloride, furnished the optically pure (+) - and (-) - 3-methyl- , 2] thiazine-1,1,4-triones, which were fluorinated with FCIO_3 to produce the corresponding chiral NF agents.