| 摘要 |
PURPOSE: A novel acetaminophen derivatives is provided, which shows good stability, and shows similar analgesic and antipyretic effect compared with existing acetaminophen preparations but gives less liver-toxicity, so can be used as analgesics and antipyretics. CONSTITUTION: A process for the preparation of acetaminophen-O-L-aspartate or acetaminophen-O-pyruvate(a kind of novel acetaminophen derivatives) comprises: dissolving acetaminophen, Boc-amino-L-aspartic acid or pyruvic acid, and DMAP(Dimethyl 4-amino pyridine) in organic solvent, desirably anhydrous ethylacetate; adding a mixed solution of DCC(Dicyclohexylcarbodiimide) in anhydrous ethylacetate, and reacting at room temperature for 2hrs; filtering and removing produced crystal, and removing solvent under decompression; separating with silica gel column chromatography; dissolving the product in tetrahydropurane, adding ether chlorite, and reacting at -20°C for 2hrs; filtering produced solid under decompression, and re-crystallizing to get the objective substances.
|
