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    PROCESS FOR THE SYNTHESIS OF GLYT-1 INHIBITORS
    4.
    发明公开
    PROCESS FOR THE SYNTHESIS OF GLYT-1 INHIBITORS 有权
    方法合成GLYT-1抑制剂的

    公开(公告)号：EP2131843A2

    公开(公告)日：2009-12-16

    申请号：EP08709206.0

    申请日：2008-02-25

    申请人： F. Hoffmann-La Roche AG

    发明人： PFLEGER, Christophe ,  WALDMEIER, Pius ,  WANG, Shaoning

    IPC分类号： A61K31/497 ,  A61P25/00 ,  C07D213/74

    CPC分类号： C07D213/74 ,  C07D295/18

    摘要： Process for preparation of a compound of formula (I) wherein Het is a 6-membered heteroaryl group, containing one, two or three nitrogen atoms; R1 is (C1-C6)-alkyl, (C3-C6)-cycloalkyl, NR4R5 or (C1-C6)-alkyl subtituted by halogen; R2 is hydroxy, halogen, NO2, CN, (C1-C6)-alkyl, (C3-C6)-cycloalkyl, (C1-C6)-alkyl substituted by halogen, (C1-C6)-alkyl substituted by hydroxy, (CH2)o-(C1-C6)-alkoxy, (C1-C6)-alkoxy substituted by halogen, NR4R5, C(O)R6 or SO2 R7; R3 is (C1-C6)-alkyl, (C3-C6)-cycloalkyl or (C1-C6)-alkyl subtituted by halogen; R4 and R5 independently from each other are hydrogen or (C1-C6)-alkyl; R6 is hydrogen, (C1-C6)-alkyl, (C1-C6)-alkoxy or NR4R5; R7 is (C1-C6)-alkyl, (C1-C6)-alkyl optionally subtituted by halogen, (CH2)o-(C3-C6)-cycloalkyl, (CH2)o-(C3-C6)-alkoxy or NR4R5; n is 0, 1, 2 or 3; o is 0, 1 or 2; and pharmaceutically acceptable acid addition salts thereof, characterized in that it comprises the steps of a) reacting a compound of formula (21) with a compound of formula: R3 OH 8 to a compound of formula (11) and b) coupling the compound of formula (11) in the presence of a coupling reagent or the corresponding acid halogenide with a compound of formula (15) to obtain a compound of formula (I).

    PROCESS FOR THE SYNTHESIS OF GLYT-1 INHIBITORS
    7.
    发明授权
    PROCESS FOR THE SYNTHESIS OF GLYT-1 INHIBITORS 有权
    方法合成GLYT-1抑制剂的

    公开(公告)号：EP2131843B1

    公开(公告)日：2011-11-09

    申请号：EP08709206.0

    申请日：2008-02-25

    申请人： F. Hoffmann-La Roche AG

    发明人： PFLEGER, Christophe ,  WALDMEIER, Pius ,  WANG, Shaoning

    IPC分类号： A61K31/497 ,  A61P25/00 ,  C07D213/74

    CPC分类号： C07D213/74 ,  C07D295/18

    摘要： Process for preparation of a compound of formula (I) wherein Het is a 6-membered heteroaryl group, containing one, two or three nitrogen atoms; R1 is (C1-C6)-alkyl, (C3-C6)-cycloalkyl, NR4R5 or (C1-C6)-alkyl subtituted by halogen; R2 is hydroxy, halogen, NO2, CN, (C1-C6)-alkyl, (C3-C6)-cycloalkyl, (C1-C6)-alkyl substituted by halogen, (C1-C6)-alkyl substituted by hydroxy, (CH2)o-(C1-C6)-alkoxy, (C1-C6)-alkoxy substituted by halogen, NR4R5, C(O)R6 or SO2 R7; R3 is (C1-C6)-alkyl, (C3-C6)-cycloalkyl or (C1-C6)-alkyl subtituted by halogen; R4 and R5 independently from each other are hydrogen or (C1-C6)-alkyl; R6 is hydrogen, (C1-C6)-alkyl, (C1-C6)-alkoxy or NR4R5; R7 is (C1-C6)-alkyl, (C1-C6)-alkyl optionally subtituted by halogen, (CH2)o-(C3-C6)-cycloalkyl, (CH2)o-(C3-C6)-alkoxy or NR4R5; n is 0, 1, 2 or 3; o is 0, 1 or 2; and pharmaceutically acceptable acid addition salts thereof, characterized in that it comprises the steps of a) reacting a compound of formula (21) with a compound of formula: R3 OH 8 to a compound of formula (11) and b) coupling the compound of formula (11) in the presence of a coupling reagent or the corresponding acid halogenide with a compound of formula (15) to obtain a compound of formula (I).