Intermolecular C(sp3)−H Amination of Complex Molecules,Angewandte Chemie International Edition

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Intermolecular C(sp3)−H Amination of Complex Molecules
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2018-03-22 , DOI: 10.1002/anie.201713225
Nicholas D. Chiappini ₁ , James B. C. Mack ₁ , J. Du Bois ₁

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A general and operationally convenient method for intermolecular amination of C(sp³)−H bonds is described. This technology allows for efficient functionalization of complex molecules, including numerous pharmaceutical targets. The combination of pivalonitrile as a solvent, Al₂O₃ as an additive, and phenyl sulfamate as a nitrogen source affords differential reaction performance and substrate scope. Mechanistic data strongly implicate a pathway for catalyst decomposition that initiates with solvent oxidation, thus providing rationale for the marked influence of pivalonitrile on this reaction process.

中文翻译：

分子间的C（sp3）-H分子间胺化

描述了一种用于C（sp ³）-H键的分子间胺化的通用且操作方便的方法。这项技术可以使复杂的分子有效地功能化，包括众多的药物靶标。新戊腈作为溶剂，Al ₂ O ₃作为添加剂和氨基磺酸苯酯作为氮源的组合提供了不同的反应性能和底物范围。机理数据强烈暗示了由溶剂氧化引发的催化剂分解途径，从而为新戊腈对该反应过程的显着影响提供了理论依据。

更新日期：2018-03-22

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