4-Hydroxy-2-pyridones are embedded as common structural units of many natural products. They exhibited good or excellent biological activities such as antifungal, antibacterial, and cytototoxic activity and so on. The class of compounds has stimulated a great deal of interest on synthetic chemists due to their structural novelty, molecular diversity, and promising biological activities. In this article, the recent progress in the isolation, structural elucidation and total synthesis of 4-hydroxy-2-pyridone natural alkaloids have been reviewed, especially on total synthesis of ilicilolin H, tenellin and sambutaxin.

Key words: 4-hydroxy-2-pyridone, alkaloids, isolation, total synthesis