Iron-Catalyzed Amination of Strong Aliphatic C(sp3)–H Bonds,Journal of the American Chemical Society

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Iron-Catalyzed Amination of Strong Aliphatic C(sp3)–H Bonds
Journal of the American Chemical Society ( IF 14.4 ) Pub Date : 2020-09-05 , DOI: 10.1021/jacs.0c07810
Sandip Kumar Das ₁ , Satyajit Roy ₁ , Hillol Khatua ₁ , Buddhadeb Chattopadhyay ₁

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A concept for intramolecular denitrogenative C(sp3)-H amination of 1,2,3,4-tetrazoles bearing unactivated primary, secondary and tertiary C-H bonds is discovered. This cata-lytic amination follows an unprecedented metalloradical activation mechanism. The utility of the developed method is showcased with the short synthesis of a bioactive mole-cule. Moreover, an initial effort has been embarked for the enantioselective C(sp3)-H amination through the catalyst design. Collectively, this study underlines the development of C(sp3)-H bond functionalization chemistry that should find wide application in the context of drug discovery and natural product synthesis.

中文翻译：

强脂肪族 C(sp3)-H 键的铁催化胺化

发现了带有未活化的一级、二级和三级 CH 键的 1,2,3,4-四唑的分子内脱氮 C(sp3)-H 胺化的概念。这种催化胺化遵循前所未有的金属自由基活化机制。通过生物活性分子的短时间合成展示了所开发方法的实用性。此外，通过催化剂设计的对映选择性 C(sp3)-H 胺化已经开始了初步努力。总的来说，这项研究强调了 C(sp3)-H 键官能化化学的发展，它应该在药物发现和天然产物合成的背景下得到广泛应用。

更新日期：2020-09-05

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