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    The synthesis of naturally occuring ecteinascidins and related compounds
    2.
    发明公开
    The synthesis of naturally occuring ecteinascidins and related compounds 有权
    Herstellung vonnatürlichvorkommenden Ecteinascidinen und verwandten Verbindungen

    公开(公告)号：EP2305689A1

    公开(公告)日：2011-04-06

    申请号：EP10181699.9

    申请日：2003-02-04

    申请人： Pharma Mar S.A.U.

    发明人： Menchaca, Roberto ,  Martinez, Valentin ,  Rodriguez, Alberto ,  Rodriguez, Natividad ,  Gallego, Pilar ,  Cuevas, Carmen ,  Munt, Simon ,  Manzanares, Ignacio

    IPC分类号： C07D515/22 ,  A61K31/50 ,  A61P35/00

    CPC分类号： C07D515/18 ,  C07D515/22

    摘要： The present invention provides compounds of formula:

    wherein
    R a and R b together with the carbon to which they are attached form a group of formula:

    where each X 1 is independently selected from hydrogen or substituted or unsubstituted R', OR', -(C=O)R', substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, and substituted or unsubstituted aralkyl; wherein R' is selected from the group consisting of H, OH, NO 2 NH 2 , SH, CN, halogen, C(=O)H, C(=O)CH 3 , CO 2 H, CO 2 CH 3 , C 1 -C 6 alkyl, alkenyl, alkynyl, aryl, aralkyl and heterocyclic;
    where R d is a substituted or unsubstituted R', OR',-(C=O)R', substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, or substituted or unsubstituted aralkyl; wherein R' is selected from the group consisting of OH, NO 2 , NH 2 , SH, CN, halogen, C(=O)H, C(=O)CH 3 , CO 2 H, CO 2 CH 3 , C 1 -C 6 alkyl, alkenyl, alkynyl, aryl, aralkyl and heterocyclic;
    R 7 is -OCH 3 and R 8 is -OH or R 7 and R 8 together form a group -O-CH 2 -O-;
    R 12a is hydrogen, acyl, alkenyl, or alkyl-O-CO-;
    R 21 is -H, OH or CN;
    X is -O- or -NH-;
    R 5 and R 18 are -OX 1 , wherein each X 1 is independently selected from hydrogen, substituted or unsubstituted C 1 -C 18 alkyl, substituted or unsubstituted C 2 -C 18 alkenyl, substituted or unsubstituted C 2 C 18 alkynyl, substituted or unsubstituted aryl, and -C(=O)R' wherein R' is selected from hydrogen, OH, NO 2 , NH 2 , SH, CN, halogen, C 1 -C 6 alkyl, alkenyl, alkynyl, aryl, aralkyl, and heterocyclic.

    摘要翻译： 本发明提供下式的化合物：其中R a和R b与它们所连接的碳一起形成下式：其中每个X 1独立地选自氢或取代或未取代的R'，OR'， - （ C = O）R'，取代或未取代的烷基，取代或未取代的烷氧基，取代或未取代的烯基，取代或未取代的炔基，取代或未取代的芳基和取代或未取代的芳烷基; 其中R'选自H，OH，NO 2 NH 2，SH，CN，卤素，C（= O）H，C（= O）CH 3，CO 2 H，CO 2 CH 3，C C 1 -C 6烷基，烯基，炔基，芳基，芳烷基和杂环基; 其中R d是取代或未取代的R'，OR'， - （C = O）R'，取代或未取代的烷基，取代或未取代的烷氧基，取代或未取代的烯基，取代或未取代的炔基，取代或未取代的芳基或取代的 或未取代的芳烷基; 其中R'选自OH，NO 2，NH 2，SH，CN，卤素，C（= O）H，C（= O）CH 3，CO 2 H，CO 2 CH 3，C 1 -C 6烷基，烯基，炔基，芳基，芳烷基和杂环基; R 7是-OCH 3，R 8是-OH或R 7和R 8一起形成-O-CH 2 -O-基团; R 12a是氢，酰基，烯基或烷基-O-CO-; R 21是-H，OH或CN; X是-O-或-NH-; R 5和R 18是-OX 1，其中每个X 1独立地选自氢，取代或未取代的C 1 -C 18烷基，取代或未取代的C 2 -C 18烯基，取代或未取代的C 2 C 18炔基，取代的 或未取代的芳基，和-C（= O）R'，其中R'选自氢，OH，NO 2，NH 2，SH，CN，卤素，C 1 -C 6烷基，烯基，炔基，芳基，芳烷基， 和杂环。