Background: Nitrogen containing heterocycle is one kind of the most important heterocycle. Among them, 1,2,4-triazolo[3,4-α]pyridine is a classic five member heterocycle fused six member heterocycle. 1,2,4-Triazolo-[3,4-α ]pyridine scaffold has been widely used in building blocks for drugs, pesticides and other fields. Keywords: 1, 2, 4-triazolo[3, 4-α]pyridine; synthesis; cyclization; biological activity; nitrogen heterocyclic; synthetic procedure.