ARYLOXIME LINKERS IN THE SOLID-PHASE SYNTHESIS OF 3-AMINOBENZISOXAZOLES
    2.
    发明申请
    ARYLOXIME LINKERS IN THE SOLID-PHASE SYNTHESIS OF 3-AMINOBENZISOXAZOLES 审中-公开
    在3-氨基苯甲酸的固相合成中的连接子

    公开(公告)号:WO00027627A1

    公开(公告)日:2000-05-18

    申请号:PCT/US1999/026803

    申请日:1999-11-12

    摘要: In its first aspect, the invention is directed to a solid support mediated method for the synthesis of diverse polycyclic heterocycles according to general formula (V). A second aspect of the invention is directed to a solid support bound intermediate compound that optionally can be derivatized before a cyclization and displacement procedure provides a product. The intermediate is preferably stable to a wide range of chemical conditions thus allowing, if desired, for the chemical derivatization of the intermediate. A third aspect of the invention is directed to a library of polycyclic heterocycle compounds where said library contains a plurality of diverse library compounds of general formula (V). A fourth aspect of the invention is directed to a method for the synthesis of a library of diverse polycyclic heterocycles by the general method described. A fifth aspect of the invention is directed to an assay kit for the identification of lead compounds of the library described therein.

    摘要翻译: 在其第一方面,本发明涉及用于合成根据通式(V)的多种多环杂环的固体支持介导的方法。 本发明的第二方面涉及固体支持物结合的中间体化合物,其可任选地在环化和置换程序提供产物之前衍生化。 中间体优选在宽范围的化学条件下是稳定的,因此如果需要,允许中间体的化学衍生化。 本发明的第三方面涉及多环杂环化合物文库,其中所述文库含有多种通式(Ⅴ)的多种文库化合物。 本发明的第四方面涉及通过所述一般方法合成不同多环杂环的文库的方法。 本发明的第五方面涉及用于鉴定其中所述文库的铅化合物的测定试剂盒。