The present invention belongs to a field of pharmaceutical chemistry, which discloses rapamycin carbonate analog represented by the structural formula I or pharmaceutically acceptable salt, medicament composition, and preparation and application thereof. Compared with rapamycin, the rapamycin carbonate analog of the present invention causes the water solubility to be strengthened by introducing water-soluble, polar group, such as hydroxyl, and the like, thereby the pharmacologic and pharmacokinetic properties are improved. Biological test on different tumor cell lines indicates that the antitumor activity of the rapamycin carbonate analog is superior to that of rapamycin, compared with the rapamycin and listed rapamycin analog CCI-779, the compounds have better pharmacokinetic parameter, the medicament is absorbed and distributed more easily in the tumor tissue, systematic immunosuppression biological activity test indicates that the compounds have higher immunosuppression activity than that of the rapamycin. The rapamycin carbonate analog provided by the present invention has simple preparation method, strong maneuverability, higher yield, and better medicament development prospect.