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    Method for preparing 4-amino-4-phenylpiperidines
    3.
    发明授权
    Method for preparing 4-amino-4-phenylpiperidines 失效
    制备4-氨基-4-苯基哌啶的方法

    公开(公告)号：US07045630B2

    公开(公告)日：2006-05-16

    申请号：US10483532

    申请日：2002-07-15

    申请人： Alain Alcade ,  Gilles Anne-Archard ,  Daniel Capraro

    发明人： Alain Alcade ,  Gilles Anne-Archard ,  Daniel Capraro

    IPC分类号： C07D211/56 ,  C07D211/98 ,  C07D211/08

    CPC分类号： C07D211/58 ,  C07D211/66 ,  Y02P20/55

    摘要： The invention relates to a process for preparing a 4-amino-4-phenylpiperidine (I): in which R is hydrogen or a (C1–C3)alkyl group, characterized in that a 1-protected 4-piperidone (II): in which Pr′ represents a removable N-protecting group, is treated sequentially first with an alkali metal cyanide and then with an amine ENHPr″ (III) in which E represents a group R′=(C1–C3)alkyl, or an N-protecting group and Pr″ is an N-protecting group, the protecting group(s) being removable under the same conditions as Pr′; then the compound thus obtained (IV) is subjected to a Grignard reaction with a phenylmagnesium halide, the two or three protecting groups are removed from the compound thus obtained (V) and compound (I) is isolated or in the form of the free base, which is converted into one of its salts.

    摘要翻译： 本发明涉及一种制备4-氨基-4-苯基哌啶（I）的方法：其中R是氢或（C 1 -C 3 -C 3）烷基 其特征在于，首先用碱金属氰化物，然后与胺ENHPr“（III）首先处理其中Pr'代表可去除的N-保护基团的1-保护的4-哌啶酮（II），其中E 表示基团R'=（C 1 -C 3）烷基或N-保护基，Pr“是N-保护基，保护基（ s）在与Pr'相同的条件下可拆卸; 然后将由此获得的化合物（IV）与卤化苯基镁进行格氏反应，从由此获得的化合物（V）中除去两个或三个保护基，并且化合物（I）被分离或以游离碱的形式 ，其被转化成其盐之一。