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    • 19. 发明授权
    • Process for the preparation of 9-amino camptothecin
    • 制备9-氨基喜树碱的方法
    • US06403603B1
    • 2002-06-11
    • US08284129
    • 1994-08-02
    • Angelo BedeschiWalter CabriIlaria CandianiFranco Zarini
    • Angelo BedeschiWalter CabriIlaria CandianiFranco Zarini
    • C07D49122
    • C07D491/22
    • 9-Amino-20(S)-camptothecin (I) is prepared by reducing 12-nitro-20(S)-camptothecin (II); converting the resulting 12-amino-20(S)-camptothecin (III) into a compound of formula (IV) wherein X is a group which can be reductively removed; reacting the compound of formula (IV) with a nitrating agent, to obtain thereby the corresponding 9-nitro-20(S)-camptothecin compound of formula (V) substituted at the 12-position by the group X; reducing in a single step the compound of formula (V), so obtaining the 9-amino-20(S)-camptothecin of formula (I); or reducing the compound of formula (V), so obtaining the corresponding 9-amino-20(S)-camptothecin compound of formula (VI) substituted at the 12-position by the group X and reductively removing the X group from the compound of formula (VI), so obtaining 9-amino-20(S)-camptothecin.
    • 通过还原12-硝基-20(S) - 喜树碱(II)制备9-氨基-20(S) - 喜树碱(I) 将所得的12-氨基-20(S) - 喜树碱(III)转化成式(IV)的化合物,其中X是可被还原去除的基团; 使式(Ⅳ)化合物与硝化剂反应,由此获得在X-12位被12位取代的相应的9-硝基-20(S)喜树碱化合物。 在一步中还原式(Ⅴ)化合物,从而得到式(I)的9-氨基-20(S) - 喜树碱; 或降低式(Ⅴ)化合物,从而得到在X基上被12位取代的相应的式(Ⅵ)的9-氨基-20(S) - 喜树碱化合物,并将X基团从 式(VI),因此得到9-氨基-20(S) - 喜树碱。