Disclosed are a chiral 3-hydroxypyrid-4-one derivative and a salt thereof. The compound is acquired by reacting methyl maltol or ethyl maltol with benzyl chloride to acquire a 3-benzyl protected maltol, then by reacting compound VII with different chiral amino alcohols to acquire 3-benzyloxypyrid-4-one, and finally by performing a palladium on carbon-catalyzed hydride reduction deprotection on compound IX. The compound of the present invention is capable of having iron ion chelating bioactivity, and is applicable in preparing an anti-iron overload medicament. The structure of the compound of the present invention is represented as formula (I).
