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Access to 2-pyridinylamide and imidazopyridine from 2-fluoropyridine and amidine hydrochloride
Organic & Biomolecular Chemistry ( IF 3.2 ) Pub Date : 2020-11-03 , DOI: 10.1039/d0ob01904f
Yibiao Li 1 , Shuo Huang 1 , Jiaming Li 1 , Jian Li 1 , Xiaoliang Ji 1 , Jiasheng Liu 1 , Lu Chen 1 , Shiyong Peng 1 , Kun Zhang 1
Affiliation  

Under catalyst-free conditions, an efficient method to synthesize 2-pyridinylamides has been developed, and the protocol uses inexpensive and readily available 2-fluoropyridine and amidine derivatives as the starting materials. Simultaneously, the copper-catalysed approach to imidazopyridine derivatives has been established with high chemoselectivity and regiospecificity. The results suggest that the nitrogen-heterocycles containing iodide substituents can also be compatible for the reaction via the cascade Ullmann-type coupling, and the nucleophilic substitution reaction provides the target products in a one-pot manner.

中文翻译:

从2-氟吡啶和盐酸脒获得2-吡啶酰胺和咪唑吡啶

在无催化剂条件下,开发了一种合成 2-吡啶酰胺的有效方法,该协议使用廉价且易于获得的 2-氟吡啶和脒衍生物作为起始材料。同时,铜催化的咪唑并吡啶衍生物方法已被建立,具有高化学选择性和区域特异性。结果表明,含有碘化物取代基的氮杂环也可以通过级联Ullmann型偶联与反应相容,并且亲核取代反应以一锅方式提供目标产物。
更新日期:2020-11-09
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