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Transition-metal-free access to 2-aminopyridine derivatives from 2-fluoropyridine and acetamidine hydrochloride

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Abstract

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.

Graphical abstract: Transition-metal-free access to 2-aminopyridine derivatives from 2-fluoropyridine and acetamidine hydrochloride

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Publication details

The article was received on 30 Aug 2018, accepted on 28 Sep 2018 and first published on 28 Sep 2018


Article type: Communication
DOI: 10.1039/C8OB02129E
Citation: Org. Biomol. Chem., 2018, Advance Article
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    Transition-metal-free access to 2-aminopyridine derivatives from 2-fluoropyridine and acetamidine hydrochloride

    Y. Li, S. Huang, C. Liao, Y. Shao and L. Chen, Org. Biomol. Chem., 2018, Advance Article , DOI: 10.1039/C8OB02129E

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