Synthesis of Differentially Substituted 1,2-Diamines through Advances in C–H Amination Technology
作者:David E. Olson、D. Allen Roberts、J. Du Bois
DOI:10.1021/ol302895f
日期:2012.12.21
A general, high yielding method for the synthesis of 1,2-diamine derivatives is described that capitalizes on selective, rhodium-catalyzed C–H insertion of hydroxylamine-based sulfamate esters. The resulting Troc-protected oxathiadiazinane heterocycles are easily modified and can be reduced under the mild action of NaI to afford differentially substituted diamine products. This technology offers a
描述了一种合成1,2-二胺衍生物的通用,高产方法,该方法利用了基于铑的羟胺基氨基磺酸酯的选择性铑催化CH插入。所得的Troc保护的oxathiadiazzaneane杂环易于修饰,可以在NaI的温和作用下还原,得到差异取代的二胺产物。该技术相对于用于二胺合成的相关的C–H和π键胺化策略提供了许多显着的改进。