2-Aminopyridines represent an important class of heterocyclic compounds due to their broad biological activities and medicinal significance. Herein, we report an efficient transition-metal-free synthesis of 2-aminopyridines from readily available phenylacetonitrile, benzonitrile, and phenylacetylene derivatives mediated by KN(SiMe3)2. This method exhibits a broad substrate scope (49 examples, 14–97% yields) and excellent scalability, highlighting its potential applications in medicinal chemistry. A plausible mechanism for the transformation was demonstrated.
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Hongwei Bai
Nanjing Tech University
Yan‐En Wang
Hebei Agricultural University
Huan-E Lao
Nanjing Tech University
Organic Letters
Nanjing Tech University
Hebei Agricultural University
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Bai et al. (Wed,) studied this question.
synapsesocial.com/papers/68c1cc2e54b1d3bfb60f424d — DOI: https://doi.org/10.1021/acs.orglett.5c02776