Incarvillateine[1],one of the novel monoterpene alkaloids,has been found to exhibit more potent antinociceptive activity comparable to that of morphine in a formalin-induced pain model in mice.The mechanism of action was also regarded to be different from that of morphine,[2]which makes incarvillateine to become an important potential lead compound for developing new nonopioid analgesic drugs.The total synthesis of incarvillateine has been completed by our group in 2009.[3] Recently,a new improved strategy has been designed to complete a series of analogues.