Introduction High−performance liquid chromatography (HPLC) coupled with various detection systems has been widely adopted for the analyses of various molecules in many research fields, such as biological, pharmaceutical, food, and environmental [1, 2] . The widening use of HPLC in the last four decades seems to be due to the advances in instrumentation, column resins, detection systems, and data processing. However, trace analysis of a target molecule in a sample containing multiple components

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... s not very easy. A selective and sensitive detection system is thus required for the analysis of small amounts of compounds in complex matrices such as biological samples. Among the various detection systems, fluorometry is one of the most reliable for the determination of trace quantities of biomolecules. However, almost all biomolecules do not fluoresce and require conversion to fluorescent molecules. For this purpose, many fluorescence tagging reagents have been developed and successively applied to the determination of various molecules, such as amines, amino acids, carboxylic acids, thiols, carbohydrates, lipids, and nucleic acids, in pre− and post−column derivatization methods. Several fluorogenic reagents having the benzofurazan (i. Abstract This review summarizes the synthesis, features and application of benzofurazan (i.e., 2,1,3−benzoxadiazole)−bearing fluorescence labeling re-