Abstract: Metabolomics of biological sample has been a hot topic in the field of mass spectrometry in recent years. The components of biological samples are complex, among which alcohols are very important. Alcohol metabolites mainly include fatty alcohols, sugars, phenols, glycerides and sterols. These metabolites undertake crucial physiological functions in vivo. However, due to the low polarity of most alcohol metabolites and the lack of ionizable groups, their research is relatively less than other types of metabolites such as amines and acids in mass spectrometry field. Chemical derivatization is a powerful sample pretreatment technology, which through the design of organic chemical reagents targeting a functional group to react with the metabolites of interest in the sample, so as to load the derivatization reagent group into the molecular skeleton of the analyte. The addition of derivatization reagent group can change the physicochemical properties of the analyte, greatly improve its ionization efficiency in mass spectrometry. As a result, a rapid and sensitive method for the detection of metabolites can be established. The application of chemical derivatization technology in the detection and analysis of alcohol metabolites by mass spectrometry can greatly improve their mass spectrometry behavior, and offer help for the physiological and pathological research of alcohol metabolites. With the consistent efforts of researchers, mass spectrometry derivatization methods for alcohol metabolites are emerging, and these proposed methods have been applied into various types of mass spectrometry instruments, including gas chromatography-mass spectrometry (GC-MS), liquid chromatography-mass spectrometry (LC-MS), matrix assisted laser desorption mass spectrometry (MALDI-MS) and direct analysis mass spectrometry. The limit of detection (LOD) and limit of quantification (LOQ) of alcohol metabolites were also significantly reduced by the establishment of various mass spectrometry derivatization methods. In this paper, the chemical derivatization reactions for alcohol metabolites published in recent years were summarized, and the qualitative and quantitative methods and rapid screening methods for alcohol metabolites based on these derivatization reactions were briefly introduced.