Abstract: The activities and synthesis of β-caryophyllene and its derivatives are summarized by reviewing the related literatures. In activities, β-caryophyllene has been used in cosmetic and food as a fragrance material. The pharmacological studies show that β-caryophyllene has the local anesthetic effect, and the effects of anti-inflammatory, repelling insects and treating general anxiety neurosis and depression. The β-caryophyllene alcohol is also applied in preparing medicament for codein and eliminating phlegm.Caryophyllene oxide has the effects of analgesic and anti-inflammatory, antifungal activities, cytotoxicity,etc. This paper also gives a brief introduction of the synthesis methods of β-caryophyllene and some of its derivatives.