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    PROCESS FOR THE PRODUCTION OF 4-AMINO-2,5-BISHETEROCYCLYLQUINAZOLINES
    18.
    发明授权
    PROCESS FOR THE PRODUCTION OF 4-AMINO-2,5-BISHETEROCYCLYLQUINAZOLINES 有权
    生产4-氨基-2,5-二（新）苄基喹唑啉的方法

    公开(公告)号：EP1412331B1

    公开(公告)日：2006-04-19

    申请号：EP02745749.8

    申请日：2002-07-19

    申请人： Pfizer Limited ,  PFIZER INC.

    发明人： BOULTON, Lee, Terence, c/o Pfizer Limited ,  CROOK, Robert, James, c/o Pfizer Global Res.& Dev. ,  PETTMAN, Alan, John, c/o Pfizer Global Res. & Dev. ,  WALTON, Robert, c/o Pfizer Global Res. & Dev.

    IPC分类号： C07D213/57 ,  C07D217/06 ,  C07D401/14

    CPC分类号： C07D401/04 ,  C07D213/57

    摘要： The invention provides a process for the production of a compound of formula (A), or a pharmaceutically acceptable salt or solvate thereof, wherein R1 represents C¿1-4? alkoxy optionally substituted by one or more fluorine atoms; R?2¿ represents H or C¿1-6? alkoxy optionally substituted by one or more fluorine atoms; R?3¿ represents a 5- or 6-membered heterocyclic ring which is optionally substituted; R4 is a 4-, 5-, 6- or 7-membered heterocyclic ring which is optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring, the ring system as a whole being optionally substituted; the process comprising condensing a compound of formula (B), wherein R1 to R3 are as defined above; with a compound of formula (C), wherein R?5 and R6¿ taken together with the N atom to which they are attached represent a 4-, 5-, 6-, or 7-membered N-containing heterocyclic ring, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring, the ring system as a whole being optionally substituted.

    摘要翻译： 本发明提供了制备式（A）化合物或其药学上可接受的盐或溶剂合物的方法，其中R 1代表C 1-4 - 任选被一个或多个氟原子取代的烷氧基; R 2代表H或C 1 -6？ 任选被一个或多个氟原子取代的烷氧基; R 3'代表任选被取代的5或6元杂环; R4是任选地与苯环或5或6元杂环稠合的4-，5-，6-或7-元杂环，所述环体系作为整体任选被取代; 该方法包括缩合式（B）的化合物，其中R 1至R 3如上所定义; 与式（C）的化合物反应，其中R 5和R 6与它们所连接的N原子一起代表4-，5-，6-或7-元含N杂环，该环 任选与苯环或5-或6-元杂环稠合，所述环体系作为整体任选被取代。