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    Methods for making 4-tetrazolyl-4-phenylpiperidine compounds
    2.
    发明授权
    Methods for making 4-tetrazolyl-4-phenylpiperidine compounds 有权
    制备4-四唑基-4-苯基哌啶化合物的方法

    公开(公告)号：US08039636B2

    公开(公告)日：2011-10-18

    申请号：US12466797

    申请日：2009-05-15

    申请人： Kevin Brown ,  Timothy J. Doyle ,  John W. F. Whitehead

    发明人： Kevin Brown ,  Timothy J. Doyle ,  John W. F. Whitehead

    IPC分类号： C07D257/04 ,  C07D405/00

    CPC分类号： C07D211/64 ,  C07D257/04 ,  C07D307/22 ,  C07D401/04

    摘要： Methods, composition, and intermediates are disclosed that are useful for making 4-Tetrazolyl-4-phenylpiperidine Compounds according to Formula I, where Ar1 is —C3-C8 cycloalkyl, phenyl, naphthyl, anthryl, phenanthryl or -(5-7-membered) heteroaryl, each being unsubstituted or substituted with one or more R2 groups; Ar2 is phenyl, naphthyl, anthryl, phenanthryl or -(5-7-membered) heteroaryl, each being unsubstituted or substituted with one or more R2 groups; Z1 and Z2 are each independently a —(C1-C4 alkyl) group; R1 is —(CH2)nC(O)N(R3)(R4) where R3 and R4 are each independently H or —(C1-C4 alkyl); R2 is halogen, —C1-C3 alkyl, —O—(C1-C3 alkyl), —NH(C1-C3 alkyl) or —N(C1-C3 alkyl)2; n is an integer ranging from 1 to 4; m is an integer ranging from 0 to 4; and, in certain embodiments, the phenyl moiety attached to the 4-position of the piperidine ring of a compound according to Formula I can be optionally substituted with one or more R2 groups.

    摘要翻译： 公开了可用于制备根据式I的4-四唑基-4-苯基哌啶化合物的方法，组合物和中间体，其中Ar 1是-C 3 -C 8环烷基，苯基，萘基，蒽基，菲基或 - （5-7-元） ）杂芳基，各自为未取代的或被一个或多个R 2基团取代; Ar 2是苯基，萘基，蒽基，菲基或 - （5-7-元）杂芳基，各自是未取代的或被一个或多个R 2基团取代; Z 1和Z 2各自独立地为 - （C 1 -C 4烷基）基团; R1是 - （CH2）nC（O）N（R3）（R4）其中R3和R4各自独立地是H或 - （C1-C4烷基）; R2是卤素，-C1-C3烷基，-O-（C1-C3烷基），-NH（C1-C3烷基）或-N（C1-C3烷基）2; n为1〜4的整数; m为0〜4的整数; 并且在某些实施方案中，连接到根据式I的化合物的哌啶环的4-位的苯基部分可以任选地被一个或多个R 2基团取代。

    Methods for making 4-tetrazolyl-4-phenylpiperidine compounds
    4.
    发明授权
    Methods for making 4-tetrazolyl-4-phenylpiperidine compounds 有权
    制备4-四唑基-4-苯基哌啶化合物的方法

    公开(公告)号：US07557219B2

    公开(公告)日：2009-07-07

    申请号：US11495221

    申请日：2006-07-28

    申请人： Kevin Brown ,  Timothy J. Doyle ,  John W. F. Whitehead

    发明人： Kevin Brown ,  Timothy J. Doyle ,  John W. F. Whitehead

    IPC分类号： C07D257/04 ,  A61K31/445

    CPC分类号： C07D211/64 ,  C07D257/04 ,  C07D307/22 ,  C07D401/04

    摘要： Methods, composition, and intermediates are disclosed that are useful for making 4-Tetrazolyl-4-phenylpiperidine Compounds according to Formula I, where Ar1 is —C3-C8 cycloalkyl, phenyl, naphthyl, anthryl, phenanthryl or -(5-7-membered) heteroaryl, each being unsubstituted or substituted with one or more R2 groups; Ar2 is phenyl, naphthyl, anthryl, phenanthryl or -(5-7-membered) heteroaryl, each being unsubstituted or substituted with one or more R2 groups; Z1 and Z2 are each independently a —(C1-C4 alkyl) group; R1 is —(CH2)nC(O)N(R3)(R4) where R3 and R4 are each independently H or —(C1-C4 alkyl); R2 is halogen, —C1-C3 alkyl, —O—(C1-C3 alkyl), —NH(C1-C3 alkyl) or —N(C1-C3 alkyl)2; n is an integer ranging from 1 to 4; m is an integer ranging from 0 to 4; and, in certain embodiments, the phenyl moiety attached to the 4-position of the piperidine ring of a compound according to Formula I can be optionally substituted with one or more R2 groups.

    摘要翻译： 公开了可用于制备根据式I的4-四唑基-4-苯基哌啶化合物的方法，组合物和中间体，其中Ar 1是-C 3 -C 8环烷基，苯基，萘基，蒽基，菲基或 - （5-7-元） ）杂芳基，各自为未取代的或被一个或多个R 2基团取代; Ar 2是苯基，萘基，蒽基，菲基或 - （5-7-元）杂芳基，各自是未取代的或被一个或多个R 2基团取代; Z 1和Z 2各自独立地为 - （C 1 -C 4烷基）基团; R1是 - （CH2）nC（O）N（R3）（R4）其中R3和R4各自独立地是H或 - （C1-C4烷基）; R2是卤素，-C1-C3烷基，-O-（C1-C3烷基），-NH（C1-C3烷基）或-N（C1-C3烷基）2; n为1〜4的整数; m为0〜4的整数; 并且在某些实施方案中，连接到根据式I的化合物的哌啶环的4-位的苯基部分可以任选地被一个或多个R 2基团取代。