Metal-Free Sustainable N-α-C(sp3)-H Functionalization of Arylmethylamines with Arylmethylketones to Synthesis of Kröhnke Pyridines Under Solvent-free Condition
摘要
An efficient “one pot” direct N-α-C(sp3)-H functionalization of arylmethylamines towards synthesis of substituted 2,4,6-triarylpyridines has developed. Fascinatingly, this method features O2 as an oxidant, metal-free simple reaction operation and the dual role of arylmethylamines. The self-oxidative coupling of readily available simple methylamines followed by their sequential deamination/cyclization cascade with arylmethylketones has accomplished anticipated 2,4,6-triarylpyridines (20 examples) up to 95% yield with good functional groups tolerance. The straightforward reaction condition in the presence of an oxidant O2 and generated H2O as a sole byproduct made this process environmentally friendly.
Graphical Abstract