Process for preparing Topotecan from 10-hydroxy-4-(S) camptothecin
    3.
    发明授权
    Process for preparing Topotecan from 10-hydroxy-4-(S) camptothecin 有权
    从10-羟基-4-(S)喜树碱制备拓扑替康的方法

    公开(公告)号:US06660861B1

    公开(公告)日:2003-12-09

    申请号:US10401119

    申请日:2003-03-27

    IPC分类号: C07D49114

    CPC分类号: C07D491/22

    摘要: The present invention relates to the use of dihalomethanes as reagents for the preparation of Topotecan{4-(S)-10(dimethylamino)-methyl-4-ethyl 4,9 dihydroxyl-H-pyrano[3′4′:6,7]indolizino-[1,2-b]quinoline-3,14(4H,12H)dione} from 10-hydroxycamptothecin. The invention discloses the rationale use of dichloromethane under solid-liquid phase transfer catalysis, which can behave both as solvent and a reactant when it serves as a source for C-1 unit for amino-alkylation of 10-hydroxy-4-(S)camptothecin.

    摘要翻译: 本发明涉及二卤代甲烷作为制备拓扑替康{4-(S)-10(二甲基氨基) - 甲基-4-乙基-4,9-二羟基-H-吡喃并[3'4':6,7 ]吲哚并[1,2-b]喹啉-3,14(4H,12H)二酮}。 本发明公开了在固 - 液相转移催化作用下二氯甲烷的理论应用,当其用作10-羟基-4-(S)氨基烷基化的C-1单元的来源时,其可以作为溶剂和反应物, 喜树碱