A Multifunctional Reagent Designed for the Site-Selective Amination of Pyridines
A Multifunctional Reagent Designed for the Site-Selective Amination of Pyridines
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DOI：
10.1021/jacs.0c03537
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发表时间：
2020-05-13
影响因子：
15
通讯作者：
Cohen, Ryan D.
中科院分区：
文献类型：
--
作者：
Fier, Patrick S.;Kim, Suhong;Cohen, Ryan D.
我们报道了一种多功能试剂的发展，用于吡啶直接转化为Boc-保护的2-氨基吡啶，具有精确的位点选择性和化学选择性。该新型试剂以200 g规模在单一步骤中制备，在温和条件下在标题反应中反应，无需对空气或水分采取预防措施，并且耐受几乎所有常见的功能。实验和原位光谱监测技术为独特的反应机制提供了详细的见解和意想不到的发现。
We report the development of a multifunctional reagent for the direct conversion of pyridines to Boc-protected 2-aminopyridines with exquisite site selectivity and chemoselectivity. The novel reagent was prepared on 200-g scale in a single step, reacts in the title reaction under mild conditions without precautions toward air or moisture, and is tolerant of nearly all common functionality. Experimental and in situ spectroscopic monitoring techniques provide detailed insights and unexpected findings for the unique reaction mechanism.