| 摘要 |
A process for the synthesis of mycophenolate mofetil of formula (I), which chemically is 2-(4-morpholinyl)ethyl ester of mycophenolic acid is disclosed, where R1 is 2-(-morpholinyl)ethyl and R2 is hydrogen atom, wherein the process includes a direct esterification reaction of mycophenolic acid with 4-(2-hydroxyethyl)morpholine in a suitable solvent such as an ether (particularly dibutylether) under azeotropic separation of water. Mycophenolate mofetil of formula (I)has cytostatic effect. It carries out inosine monophosphate dehydrogenase selective inhibition, wherein it also de novo synthesis pathway of guanosine nucleotides and their incorporation into DNK, such that the cytostatic effect to lymphocytes is higher that to other cells.
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