Primary Sulfonamide Synthesis Using the Sulfinylamine Reagent N-Sulfinyl-O-(tert-butyl)hydroxylamine, t-BuONSO,Organic Letters

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Primary Sulfonamide Synthesis Using the Sulfinylamine Reagent N-Sulfinyl-O-(tert-butyl)hydroxylamine, t-BuONSO
Organic Letters ( IF 4.9 ) Pub Date : 2020-11-25 , DOI: 10.1021/acs.orglett.0c03505
Thomas Q. Davies ₁ , Michael J. Tilby ₁ , David Skolc ₂ , Adrian Hall ₂ , Michael C. Willis ₁

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Sulfonamides have played a defining role in the history of drug development and continue to be prevalent today. In particular, primary sulfonamides are common in marketed drugs. Here we describe the direct synthesis of these valuable compounds from organometallic reagents and a novel sulfinylamine reagent, t-BuONSO. A variety of (hetero)aryl and alkyl Grignard and organolithium reagents perform well in the reaction, providing primary sulfonamides in good to excellent yields in a convenient one-step process.

中文翻译：

使用亚磺胺试剂N-亚磺酰基-O-（叔丁基）羟胺，t- BuONSO合成伯磺酰胺

磺酰胺在药物开发的历史中起着决定性的作用，并在今天继续流行。特别地，伯磺酰胺在市售药物中是常见的。在这里，我们描述了从有机金属试剂和新型亚磺胺试剂t- BuONSO直接合成这些有价值的化合物的方法。多种（杂）芳基和烷基格氏试剂和有机锂试剂在反应中表现良好，可通过便捷的一步法提供伯磺酰胺，收率高至优异。

更新日期：2020-12-18

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