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    Process for preparation of n-heteroaryl-n-aryl-amine by reacting n-aryl carbamic acid ester with halo-heteroaryl and analogous process
    34.
    发明专利
    Process for preparation of n-heteroaryl-n-aryl-amine by reacting n-aryl carbamic acid ester with halo-heteroaryl and analogous process 审中-公开
    通过使用HALO-HETEROARYL和ANALOGOUS过程反应N-芳基碳酸酯来制备N-叔丁基-N-芳基胺的方法

    公开(公告)号：JP2011037909A

    公开(公告)日：2011-02-24

    申请号：JP2010264372

    申请日：2010-11-26

    申请人： Vertex Pharmaceuticals Inc ,  バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated

    发明人： SNOONIAN JOHN R ,  OLIVER-SHAFFER PATRICA-ANN

    IPC分类号： A61K31/44 ,  A61P7/02 ,  A61P19/10 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P37/08 ,  A61P43/00 ,  C07D213/56 ,  C07D213/75 ,  C07D213/79 ,  C07D213/80 ,  C07D213/803 ,  C07D213/82

    CPC分类号： C07D213/75 ,  C07D213/56 ,  C07D213/80 ,  C07D213/803 ,  C07D213/82

    摘要： PROBLEM TO BE SOLVED: To provide a process for the preparation of a diaryl amine compound or a salt thereof.
    SOLUTION: The invention relates to processes for producing a diaryl amine compound of formula (I), or a salt thereof. The process comprises a step of coupling a compound of formula (II) with an amine of formula (III) in the presence of an alkali metal salt or a transition metal catalyst, wherein, Ar
    1 and Ar
    2 are independently Q, wherein each Q is an aryl or heteroaryl ring system optionally fused to a saturated or unsaturated 5-8 membered ring having 0-4 heteroatoms, wherein Q is optionally substituted as defined by a specific group, wherein: X is a leaving group, and Y is -C(O)-O-Z, and Z is selected from 1-6C aliphatic, benzyl, Fmoc, -SO
    2 R' and Q, provided that Q is not substituted with X or alkyne, wherein R' is selected from hydrogen, 1-6C aliphatic, halo, 1-6C alkoxy, cyano, nitro, amino, hydroxy, and a 5-6 membered carbocyclic or heterocyclic ring system optionally substituted with 1 to 3 substituents independently selected from 1-6C aliphatic group.
    COPYRIGHT: (C)2011,JPO&INPIT

    摘要翻译： 待解决的问题：提供二芳基胺化合物或其盐的制备方法。 解决方案：本发明涉及制备式（I）的二芳基胺化合物或其盐的方法。 该方法包括在碱金属盐或过渡金属催化剂存在下将式（II）的化合物与式（III）的胺偶联的步骤，其中Ar 1， SB> 2 独立地是Q，其中每个Q是芳基或杂芳基环系统，任选地与具有0-4个杂原子的饱和或不饱和5-8元环稠合，其中Q任选地被特定基团 ，其中：X是离去基团，Y是-C（O）-OZ，Z选自1-6C脂族基，苄基，Fmoc，-SOS2R，R'和Q，提供 该Q不被X或炔取代，其中R'选自氢，1-6C脂族，卤素，1-6C烷氧基，氰基，硝基，氨基，羟基和5-6元碳环或杂环系统 被1至3个独立地选自1-6C脂族基团的取代基取代。 版权所有（C）2011，JPO＆INPIT