Iron-Catalyzed Amination of Strong Aliphatic C(sp3)-H Bonds
Iron-Catalyzed Amination of Strong Aliphatic C(sp3)-H Bonds
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DOI：
10.1021/jacs.0c07810
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发表时间：
2020-09-23
影响因子：
15
通讯作者：
Chattopadhyay, Buddhadeb
中科院分区：
文献类型：
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作者：
Das, Sandip Kumar;Roy, Satyajit;Chattopadhyay, Buddhadeb
发现了带有未活化的伯、仲和叔C-H键的1，2，3，4-四唑分子内脱氮C（sp（3））-H胺化的概念。这种催化胺化遵循一种前所未有的金属自由基活化机制。该方法的实用性与生物活性分子的短合成展示。此外，通过催化剂的设计，对不对称选择性的C（sp（3））-H胺化反应进行了初步的尝试。总的来说，这项研究强调了C（sp（3））-H键功能化化学的发展，应该在药物发现和天然产物合成的背景下找到广泛的应用。
A concept for intramolecular denitrogenative C(sp(3))-H amination of 1,2,3,4-tetrazoles bearing unactivated primary, secondary, and tertiary C-H bonds is discovered. This catalytic amination follows an unprecedented metalloradical activation mechanism. The utility of the method is showcased with the short synthesis of a bioactive molecule. Moreover, an initial effort has been embarked on for the enantioselective C(sp(3))-H amination through the catalyst design. Collectively, this study underlines the development of C(sp(3))-H bond functionalization chemistry that should find wide application in the context of drug discovery and natural product synthesis.