Intermolecular C(sp3)-H Amination of Complex Molecules
Intermolecular C(sp3)-H Amination of Complex Molecules
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DOI：
10.1002/anie.201713225
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发表时间：
2018-04-23
影响因子：
16.6
通讯作者：
Du Bois, J.
中科院分区：
文献类型：
--
作者：
Chiappini, Nicholas D.;Mack, James B. C.;Du Bois, J.
本文介绍了一种通用的、操作简便的C（sp（3））-H键分子间胺化反应方法。该技术允许复杂分子的有效功能化，包括许多药物靶标。新戊腈作为溶剂、Al 2 O3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催化剂分解的途径，引发溶剂氧化，从而提供了新戊腈对该反应过程的显着影响的基本原理。
A general and operationally convenient method for intermolecular amination of C(sp(3))-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.