铜催化醇与氨基吡啶在有氧条件下合成酰胺

Copper-catalyzed Synthesis of Amides from Alcohols and Aminopyridines Under Aerobic Conditions

在铜催化氧化体系下,以苯甲醇和2-氨基吡啶为反应原料,采用空气鼓泡法一步合成了N-(2-吡啶基)酰胺化合物.机理研究结果表明,苯甲醇在空气中氧化原位生成苯甲醛,将其作为偶联组分与氨基吡啶作用生成酰胺产物.生物活性测试结果显示,合成产物具有一定的抗菌活性.该反应高效、官能团兼容性好,反应中无需使用任何添加剂,并以空气中的氧气作为理想氧化剂,具备经济、绿色的优点.

N-(pyridine-2-yl)amides were synthesized in one step with benzyl alcohols and 2-aminopyridines in copper-catalyzed aerobic conditions by air bubbling method.The mechanism study demonstrated that benzaldehydes were formed in situ from benzyl alcohols under aerobic conditions and acted as coupling partners to react with 2-aminopyridines to synthesize amides.The bioactivity study showed that the synthesized products possessed certain antibacterial activity.This reaction features high efficiency and functional group tolerance.Moreover,no additives were used in the reaction and this method utilized oxygen from the air as an ideal oxidant with the virtue of economy and green.