We report a general chemoselective strategy for amide bond formation with poorly nucleophilic amines in the presence of reactive primary alcohols or amines as the competing nucleophiles. The selectivity for less reactive amines over competing alcohols was achieved using TCFH and catalytic Oxyma as a highly reactive, inexpensive, and safe reagent combination. By temporarily masking more reactive amines as imines through the use of electron-deficient aldehydes, the hindered amines could be similarly coupled with high efficiency and selectivity.

中文翻译：

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由 TCFH 催化 Oxyma 和瞬时亚胺保护实现的一般化学选择性受阻酰胺偶联


我们报道了在反应性伯醇或胺作为竞争亲核试剂存在的情况下，与亲核性差的胺形成酰胺键的一般化学选择性策略。使用 TCFH 和催化 Oxyma 作为高反应性、廉价且安全的试剂组合，实现了对反应性较低胺的选择性，而不是竞争性醇类。通过使用缺电子醛暂时将更多的反应性胺掩盖为亚胺，受阻胺可以类似地以高效率和选择性耦合。