Sulfonamides, especially primary aryl sulfonamides are very important scaffolds not only because of the wide applications as pharmacophores in drugs, but also the derivatization for other sulfonamides and different sulfur-containing compounds. Among the aryl sulfonamides, most syntheses of electron-rich (hetero)aryl sulfonamides are still severely limited by the classic chlorosulfonation or oxidative chlorination reactions with significant drawbacks. In this work, by the proposed and unique tert-butyl sulfonylcarbamate intermediate generated in situ from easily accessed tert-butyl chlorosulfonylcarbamate and diisopropylethylamine, a catalyst-free, mild and very pratical aminosulfonylation protocol for a wide scope of electron-rich (hetero)arene substrates with good to excellent yields was reported.

中文翻译：

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利用氯磺酰氨基甲酸叔丁酯与二异丙乙胺对富电子（异）芳烃进行直接氨基磺酰化


磺胺类药物，尤其是伯芳基磺酰胺是非常重要的支架，不仅因为在药物中作为药效团的广泛应用，而且还因其它对其他磺胺类药物和不同含硫化合物的衍生化作用。在芳基磺酰胺中，大多数富电子（杂）芳基磺酰胺的合成仍然受到经典氯磺化或氧化氯化反应的严重限制，具有明显的缺点。在这项工作中，通过由易于获得的氯磺酰氨基甲酸叔丁酯和二异丙基乙胺原位生成的拟议和独特的叔丁基磺酰氨基甲酸酯中间体，报道了一种无催化剂、温和且非常实用的氨基磺酰化方案，适用于广泛的富电子（异）芳烃底物，产率从好到极好。