The explosive growth of algae resulted from the eutrophication of water bodies occurs frequently around the coastal area in recent years, which severely damages the balance of ecosystems. The classical methods exhibit various restrictions during the prevention procedures under different algae density conditions in the water body at different periods, such as the remaining residues for chemical reagents, the high cost of manpower or big volume of equipment for physical patterns and the instability along with slow effectiveness for biological strategies. The application of new, efficient and safe algal bloom prevention under controlling is a hot and challenging topic currently. The extracellular protease and the secondary metabolite of marine bacteria were thus effectively investigated for the leading compounds with algicidal activity. Considering their low toxicity, high selectivity and environment-friendly properties, the use of natural bacillamides and their analogues as algicides has proven to be particularly attracting. The relating synthesis were carried out for the much lower contents from diversified natural resources. After summarizing the progress in synthesis of natural algicide bacillamides from 2005 to 2023, a new green technology was realized for biomimetic preparation of the key intermediate of thiazole units. The mechanism was discussed for this novel methodology with the potential for the industrial production in large scales.