六甲基二硅氮烷介导的磺酰胺和胺与甲酰胺的脒化反应

Hexamethyldisilazane-Mediated Amidination of Sulfonamides and Amines with Formamides.

作者信息

Chou Yu-Chen, Lin Wei-Han, Lin Xiu-Yi, Kuo Chin-Ling, Zeng Wan-Qin, Lu I-Chung, Liang Chien-Fu

机构信息

Department of Chemistry, National Chung Hsing University, Taichung 402, Taiwan.

出版信息

J Org Chem. 2022 Nov 18;87(22):15327-15332. doi: 10.1021/acs.joc.2c01902. Epub 2022 Oct 27.

DOI:10.1021/acs.joc.2c01902

PMID:36302512

Abstract

Hexamethyldisilazane was reacted with formamides to generate ,-disubstituent formimidamide, after which a reaction with sulfonamides was induced to form sulfonylformamidines. This protocol can be applied for arylformamidine formation in which anilines are used as substrates under optimized conditions. The advantages of this method are high efficiency, structural diversity in products with good yields, and applicability in large-scale operations.

摘要

六甲基二硅氮烷与甲酰胺反应生成α,α-二取代甲脒，之后诱导其与磺酰胺反应形成磺酰基甲脒。该方案可用于在优化条件下以苯胺为底物形成芳基甲脒。该方法的优点是效率高、产物结构多样且产率良好，以及适用于大规模操作。