PURPOSE: A method for preparing tricyclo compound derivatives of a novel structure is provided to obtain glycosylated derivatives with immunosuppression and to improve superior solubility. CONSTITUTION: A glycosylated tricyclo compound derivative is denoted by a chemical formula 1. The tricyclo compound is tacrolimus, ascomycin, rapamycin, or meridamycin. A linker is a formyl group, an acetyl group, a propionyl group, a butyl group, an acryl group, an ethylsuccinyl group, a succinyl group, or an aminohexyl group. A method for preparing the derivative of chemical formula 1 comprises: a step of introducing a succinyl group at 1 -OH site using glucose and introducing a protection group to -OH residue a step of adding a macrolide compound to compound 25 and removing the R3 and R4 protection group from the compound 25.본 발명은 트리사이클로 화합물 구조에 당을 부착하여 신규 구조의 트리사이클로 화합물 유도체들을 만드는 기술 및 그 기술에 의해 합성되는 당화 유도체에 관한 것으로서, 면역억제 기능을 보유하며, 최대 10,000배 이상 수용성이 향상되었다.
