School of Biotechnology and Health Sciences, Wuyi University, Jiangmen, Guangdong Province 529090, China.
Org Biomol Chem. 2018 Nov 7;16(41):7564-7567. doi: 10.1039/c8ob02129e. Epub 2018 Oct 5.
Under catalyst-free conditions, an efficient method for the synthesis of 2-aminopyridine derivatives through the nucleophilic substitution and hydrolysis of 2-fluoropyridine and acetamidine hydrochloride has been developed. This amination uses inexpensive acetamidine hydrochloride as the ammonia source and has the advantages of a high yield, high chemoselectivity and wide substrate adaptability. The results suggest that other N-heterocycles containing fluorine substituents can also complete the reaction via these reaction conditions and yield the target products.
在无催化剂条件下，开发了一种通过 2-氟吡啶和乙脒盐酸盐的亲核取代和水解反应合成 2-氨基吡啶衍生物的有效方法。该胺化反应以廉价的乙脒盐酸盐作为氨源，具有产率高、化学选择性高和底物适应性广的优点。结果表明，其他含氟取代基的 N-杂环也可以通过这些反应条件完成反应，并生成目标产物。
