Abstract: OBJECTIVE To synthesize the title compound. METHODS Tripthiocyanatolide was semi-synthesized by triptolide, which was a convenient starting material, through the reaction of nucleophilic substitution. RESULTS The total yield was 79.5%. The target compound was identified by IR, 1H-NMR and MS. CONCLUSION It′s very important to develop a new product with high effect and low toxicity by making use of 2-step synthesis technology.