Chlorogenic acid (CGA) is a type of water-soluble phenolic derivatives with a variety of physiological functions， but its low lipid solubility limit CGA's industrial applicability. Molecular modification is an effective approach to synthesize chlorogenic acid derivatives (CAD) which have higher liposolubility and comparable bioactivities to CGA. In this paper， the preparation of CAD using chemical methods including the acyl chloride method and enzymatic methods， such as esterification and ester exchange are reviewed. The typical approaches for the isolation and purification of CAD are discussed. Besides， the recent advances in chlorogenic acid derivatives' bioactivities including the antioxidant， antitumor and antifungal functions， lipid metabolism regulation properties are evaluated. Finally， the current issues in CAD study and potential applicability in future are summarized.