The invention discloses a compounding method for a thioamide compound shown as formula (II). The compounding method comprises the following steps: by taking aldehyde and formyl aliphatic amine as reacting raw materials and taking Na2S.9H2O as a sulfuration reagent, reacting in a water phase under an effect of an oxidizing agent, thereby acquiring the thioamide compound. The compounding method provided by the invention has the advantages that the raw materials are low in cost and are easily acquired, the solvents are green and environment-friendly, the reaction operation is simple, the condition is mild, the substrate is wide in universality, the yield is higher, the functional group tolerance is excellent, the thioamide modification for natural aldehyde and biological active molecule is successively realized, and a method for efficiently constructing the thioamide compound is supplied to the medicinal chemical and biologic orthogonal chemical research.