The invention relates to a preparation method of a novel glycoside ceramide analogue with immunoregulation activity and an application thereof, and belongs to the technical field of chemistry and medicine. Based on the structural analysis of a receptor and combined with molecular docking and molecular dynamics simulation technologies, a category of compound with modified sugar ring (tryptophan, glutamic acid derivative or p-hydroxyphenylpropionic acid are introduced into R1 or R2 sites respectively) is designed and synthesized. Biological activity research shows that such compound has Th2 selectivity and has potential for use in pharmaceuticals. The novel compound has the following main synthetic characteristics: R1 is a hydroxyl group or a tryptophan derivative linked through an amide condensation reaction; R2 is a hydroxyl group or an L-glutamic acid derivative linked through amide condensation reaction, or p-hydroxybenzoic acid; R3 is -OBn, R4 is -N3;or R3 is -N3, R4 is -OBn;R5 maybe a substituent such as SEt, S-iPr, SPh, STOL, OC (NH) CCl3, and the like.