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    METHOD FOR THE PREPARATION OF INTERMEDIATES USEFUL FOR THE SYNTHESIS OF [1,2,4]-TRIAZOLO[4,3-A]PYRIDINES
    75.
    发明公开
    METHOD FOR THE PREPARATION OF INTERMEDIATES USEFUL FOR THE SYNTHESIS OF [1,2,4]-TRIAZOLO[4,3-A]PYRIDINES 审中-公开

    公开(公告)号：EP3567040A1

    公开(公告)日：2019-11-13

    申请号：EP19181689.1

    申请日：2014-06-24

    申请人： Amgen, Inc

    发明人： Bio, Matthew ,  Fang, Eric ,  Milne, Jacqueline E. ,  Wiedemann, Sean ,  Wilsily, Ash

    IPC分类号： C07D471/04

    摘要： The present application discloses a method comprising: (A)
    (i) admixing a methylnicotinate of Formula (I):

    wherein R3 is Cl, Br, or I, and R4 is alkyl;
    with 1,3,5-triazine, and a base, under conditions sufficient to form a naphthyridinone of Formula (II):

    (ii) admixing the naphthyridinone of Formula (II) with methoxyethanol, a base, and a copper (I) catalyst, under conditions sufficient to form 3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one ("NAPH"):

    or (B):
    (i) admixing protected 2-alkoxypyridin-4-ylamine with a lithium reagent, under conditions sufficient to form the protected N-(3-formyl-4-amino-2-alkoxy)pyridine:

    wherein PG is a protecting group
    wherein R 8 is an alkyl group;
    (ii) admixing the protected N-(3-formyl-4-amino-2-alkoxy)pyridine with 1-hydroxy-2-(2-methoxyethoxy)ethane-1 -sulfonate:

    and base, under conditions sufficient to form a naphthyridine of Formula (III):

    ; and
    (iii) acidifying the naphthyridine of Formula (III), under conditions sufficient to form 3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one ("NAPH"):