Techniques for the resolution by liquid chromatography of racemic compounds based upon diastereomer formation with a fluorescent chiral reagent are outlined in this review. The tagging reagents for various functional groups, i.e. amine, carboxyl, hydroxyl and thiol, are evaluated in terms of optical purity, handling, flexibility, stability, sensitivity and selectivity. The applicabilities of the reagents to drugs and biologically important substances are included in the text. This review is limited to reagents with fluorophores and reagents that exhibit fluorescence.