| 摘要 |
A process for preparing pegylated mycophenolic acid derivatives having improved water solubility and bioavailability is provided to simplify the preparation procedure, inhibit side reactions, and improve preparation yield by using non-harmful poly(ethylene glycol)(PEG). A process for preparing pegylated mycophenolic acid derivatives represented by the formula(7) comprises the steps of: dissolving MeO(methoxy)-PEG represented by the formula(4) in organic solvent, and pegylating with RX as reaction reagent in the presence of base to prepare compounds represented by the formula(8); dissolving the compounds represented by the formula(8) in organic solvent and reacting with R'X to prepare compounds represented by the formula(9); and dissolving the compounds represented by the formula(9) and mycophenolic acid derivatives in organic solvent and reacting with base, wherein R is methanesulfonyl, p-methylbenzenesulfonyl, benzenesulfonyl, p-toluenesulfonyl or trifluoro acetyl; R' is K(potassium), Na(sodium) or Li(lithium); X is halogen including chloro, bromo and iodo; and n is 38 to 46. |
