| 摘要 |
NEW MATERIAL:A camptothecin derivative of the formula [R<1> is H, Cl, 1-4C alkyl; R<2> is -OCO-NR<3>R<4> (R<3>, R<4> are H, alkyl, or they incorporate to form a heterocyclic containing N atoms) which occupies 9-12 positions in the camptothecin skeleton] and its ammonium salt. EXAMPLE:9-[4-(isopropylcarbamoylmethyl)-1-piperazino]carbonyloxycamptothe cin-. USE:Antineoplastic: it has lower toxicity than camptothecin and higher antineoplastic action. PREPARATION:A comptothecin or 7-substituted camptothecin bearing hydroxyl on its A ring is allowed to react with carbamoyl phosgen which is the corre sponding side-chaine chloride and converted into the chlorocarbonyl derivative, then the product is allowed to react with a corresponding amine to give the compound of the formula. |
