Herein, we report the first examples of the Mitsunobu alkylation of β-alkoxycarbonyl 2-nitrobenzenesulfones. Wang resin was acylated with α-halocarboxylic acids followed by the reaction with 2-nitrothiophenols. After oxidation with m-chloroperbenzoic acid, the immobilized β-alkoxycarbonyl 2-nitrobenzensulfones were subjected to alkylation with various alcohols. The reaction outcome strongly depended on the selection of the alkylating species. After the reduction of the nitro group, acid-mediated cleavage and subsequent cyclization, the C²-(di)substituted benzothiazin-3(4H)-one 1,1-dioxides were obtained in high crude purities and good overall yields.

在此，我们报道了β-烷氧基羰基2-硝基苯砜的Mitsunobu烷基化的第一个例子。Wang树脂用α-卤代羧酸酰化，然后与2-硝基硫代苯酚反应。与氧化后米氯过苯甲酸，固定化β -烷氧基羰2- nitrobenzensulfones进行烷基化与各种醇。反应结果在很大程度上取决于烷基化物质的选择。在硝基还原，酸介导的裂解和随后的环化之后，以高的粗纯度和良好的总收率获得了C ^2-（二）取代的苯并噻嗪-3（4 H）-1，1-二氧化物。