2,3'-Anhydro-2'-deoxy-5-fluorouridine derivatives with cytotoxic activity, a manufacturing process and application
    5.
    发明公开
    2,3'-Anhydro-2'-deoxy-5-fluorouridine derivatives with cytotoxic activity, a manufacturing process and application 审中-公开
    具有细胞毒活性的2,3'-脱氢-2'-脱氧-5-氟尿苷衍生物,生产方法和应用

    公开(公告)号:EP3172216A1

    公开(公告)日:2017-05-31

    申请号:EP14772458.7

    申请日:2014-08-22

    摘要: The subject matter of the invention is novel 2,3′-anhydro-2′-deoxy-5-fluorouridine derivatives of general formula 1 where R is a trifluoromethyl, 2,2,2-trifluoroethyl, difluoromethyl, perfluoroethyl, 1-fluoroethyl, 2-fluoroethyl, 1,1-difluoroethyl, 1,2-difluoroethyl, 2,2-difluoroethyl, 1,1,2-trifluoroethyl, 1,2,2-trifluoroethyl, 1,1,2,2-tetrafluoroethyl, 1,2,2,2-tetrafluoroethyl group. In a second aspect, the subject matter of the invention is a process for the manufacture of 2,3′-anhydro-2′-deoxy-5-fluorouridine derivatives of general formula 1. In a third aspect, the subject matter of the invention is an application of 2,3′-anhydro-2′-deoxy-5-fluorouridine derivatives of general formula 1 in the anticancer treatment of breast cancer, cervical cancer, lung cancer and nasopharynx cancer.

    摘要翻译: 本发明的主题是通式1的新的2,3'-脱水-2'-脱氧-5-氟尿苷衍生物,其中R是三氟甲基,2,2,2-三氟乙基,二氟甲基,全氟乙基,1-氟乙基, 2-氟乙基,1,1-二氟乙基,1,2-二氟乙基,2,2-二氟乙基,1,1,2-三氟乙基,1,2,2-三氟乙基,1,1,2,2-四氟乙基, 2,2,2-四氟乙基。 第二方面,本发明的主题是制备通式1的2,3'-脱水-2'-脱氧-5-氟尿苷衍生物的方法。在第三方面,本发明的主题 是通式1的2,3'-脱水-2'-脱氧-5-氟尿苷衍生物在乳腺癌,宫颈癌,肺癌和鼻咽癌的抗癌治疗中的应用。

    SYNTHESIS OF FLUOROCARBOFUNCTIONAL SILSESQUIOXANES
    8.
    发明公开
    SYNTHESIS OF FLUOROCARBOFUNCTIONAL SILSESQUIOXANES 有权
    合成FLUOR卡博功能倍半硅氧烷

    公开(公告)号:EP2473549A1

    公开(公告)日:2012-07-11

    申请号:EP10759741.1

    申请日:2010-08-16

    IPC分类号: C08G77/04

    摘要: The subject of the invention is the method of synthesis of fluoracarbofunctional cage silsesquioxanes of the general formula in which•R1 stands for HCF2(CF2)n(CH2)mO(CH2)3Si(CH3)2O or HCF2(CF2)n(CH2)mO(CH2)3 group in which n=1-12, m=1-4;•R2, R3, R4, R5, R6, R7, R8 can be the same as R1 or different from it and stand all either for the (C1-C25) alkyl group or any aryl group, based on hydrosilylation of fluoroalkyl-allyl ether with an appropriate hydrogen-silsesquioxane in the presence of siloxide rhodium complex [{Rh(OSiMe3)(cod)}2] as a catalyst.