Natural spinasterol-glucose (3-O-β-D-glucopyanosylspinasterol), isolated from Stewartia koreana leaves, has been identified as a compound to exhibit a potent anti-inflammatory activity. Further biological investigations for spinasterol glycosides were needed, but due to the difficulty and inefficiency of isolation and synthesis of natural spinasterol and spinasterol glucose it has not been done. Therefore, we have designed and synthesized a new sterol, such as ergostenol((3β, 5α)-ergost-8(14)-en-3-ol), as the substitute for spinasterol. In present study, we will describe the synthesis and biological activities of ergostenol and its glycosides.