Objective To study the sulfonylation of panaxadiol from Panax notoginseng. Methods A series of panaxadiol derivatives have been synthesized by Sulfuryl chloride with 3-hydroxy group of panaxadiol. The chemical structures of these derivatives were identified by NMR. Results Four derivatives were obtained. Conclusion These four derivatives were new compounds and 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.