| 摘要 |
NEW MATERIAL:The compound of formula (R<1> is H or 1-4C alkyl; R<2> and R<3> are H, alkyl, alkenyl, aryl or aralkyl). EXAMPLE:Ethyl 7-ethylcamptothecin-10-yl phosphate. USE:A carcinostatic agent having mitigated toxicity and soluble in water. PREPARATION:For example, a camptothecin derivative having a hydroxyl group at A-ring is made to react with 1-5 equivalent of phosphorus oxychloride in a solvent such as pyridine under ice cooling or at room temperature, reacting further with 1-5 equivalent of an alcohol of formula ROH (R is alkyl, alkenyl, aralkyl or aryl) and treating the reaction mixture with water.
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