A catalytic system for intermolecular benzylic C(sp³)–H amination is developed utilizing 1,2,3,4-tetrazole as a nitrene precursor via iron catalysis. This method enables direct installation of 2-aminopyridine into the benzylic and heterobenzylic position. The method selectively aminates 2° benzylic C(sp³)–H bond over the 3° and 1° benzylic C(sp³)–H bonds. Experimental studies reveal that the C(sp³)–H amination undergoes via the formation of a benzylic radical intermediate. This study reports the discovery of new method for 2-pyridine substituted benzylamine synthesis using inexpensive, biocompatible base metal catalysis that should have wide application in the context of medicinal chemistry and drug discovery.

中文翻译：

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铁催化的苄基 C(sp3)–H 键的分子间胺化

利用 1,2,3,4-四唑作为氮烯前体，通过铁催化开发了分子间苄基 C(sp ^{3 )–H 胺化催化体系。}该方法能够将 2-氨基吡啶直接安装到苄基和杂苄基位置。该方法选择性地胺化 2° 苄基 C(sp ³ )–H 键，超过 3° 和 1° 苄基 C(sp ³ )–H 键。实验研究表明，C(sp ³ )–H 胺化是通过形成苄基自由基中间体进行的。本研究报告了使用廉价、生物相容性贱金属催化合成 2-吡啶取代的苄胺的新方法的发现，该方法应在药物化学和药物发现方面具有广泛的应用。