Abstract: The changes of metabolic profile are closely related to external stimulus, and the concentration of the metabolite can directly reflect the physiological or pathological states of organisms. Therefore, the quantitative detection of metabolites is necessary. However, traditional targeted metabolomic methods have such drawbacks as narrow coverage and low sensitivity. In recent years, derivatization techniques have developed rapidly in the field of metabolomics. Derivatization reagents for amine, hydroxyl, carboxyl, carbonyl, hydrosulphonyl and other groups have been used in metabolomics research. This paper introduces various derivatization reactions and their applications according to group classification and reviewes the characteristics of multi-group derivatization techniques, with a propect of their research directions and challenges.