Facile synthesis of aryl-substituted pyridines via Suzuki–Miyaura approach

摘要: Abstract A facile and efficient synthetic route to arylpyridines is reported. When heated with boronic acids in the presence of 5 mol % PdCl 2 (PPh 3 ) KHCO 4:1 DMF/H O solution at 110 °C, 5-iodopyridines have undergone Suzuki–Miyaura coupling reactions afford 5-aryl-substituted pyridines good excellent yields. The reaction has been found be general for a broad range iodopyridines acids, demonstrated tolerance variety aliphatic, aromatic, heteroaromatic ferrocenyl groups electron-withdrawing electron-donating substituents. This approach could accommodate various functional provide rapid access library functionalized pharmacological interest. starting prepared from α,β-alkynic ketones, involving conjugate addition propargylamine alkynones, followed by metal-catalyzed cross-coupling resulting N -propargylic β-enaminones aryl iodides electrophilic cyclization molecular iodine.