This paper describes the preparation ofβ-elemene derivative of Re(C0)3 and[188Re]-1abelled radioactiveβ-elemene derivative of Re(CO)3.β-elemene derivative was synthesized by purifiedβ-elemene with di-(2-picoyl)amine.Radioactiveβ-elemene derivative of Re(CO)3 was synthesized byβ-elemene di-(2-picoyl)amine with fac-[188Re(CO)3(H20)3]+ and purified by C18 reverse phase HPLC.β-elemene derivative was synthesized at a yield of 64%.Radioactiveβ-elemene derivative of Re(CO)3 was prepared with a radiochemical yield of 40% and a radiochemical purity of greater than 95%.It is concluded that this process is economic and suited for preparing ra-dioactiveβ-elemene derivative of Re(CO)3 which may become a potential therapeutic radiopharmaceuticals in the fu-ture.