Objective To design and synthesize panaxadiol derivatives. Methods A series of panaxadiol derivatives have been synthesized with simple acylation of hydroxy group of panaxadiol. The chemical structures of these derivatives were identified by NMR. Results Five derivatives were obtained and four of them were new compounds. Conclusion These derivatives can be obtained readily， thus a large number of derivatives can be synthesized similarly for bioassay. This provides a new approach for the research and development of Panax notoginseng.