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    PROCESS FOR THE PREPARATION OF MORPHINAN-6-ONE COMPOUNDS
    1.
    发明公开
    PROCESS FOR THE PREPARATION OF MORPHINAN-6-ONE COMPOUNDS 审中-公开

    公开(公告)号：EP4174072A2

    公开(公告)日：2023-05-03

    申请号：EP22204999.1

    申请日：2014-02-05

    申请人： Macfarlan Smith Limited

    发明人： ARCHER, Nicolas ,  DAVIES, Timothy ,  PRICE, Amy ,  YOUNG, Maureen

    IPC分类号： C07D489/08

    摘要： The present provides a process for preparing a compound of formula (3), the process comprising the steps of:
    (a) providing an aqueous acidic solution comprising a compound of formula (1) and, as an impurity, a compound of formula (2); and
    (b) treating the aqueous acidic solution of step (a) such that the compound of formula (2) dehydrates to form a compound of formula (1) and the compound of formula (1) is reduced to form an aqueous acidic solution of the compound of formula (3),


    wherein:
    the treating of step (b) is carried out at one or more temperatures greater than ambient in the presence of a hydrogenation catalyst and hydrogen gas; and
    wherein for the compounds of formulae (1), (2) and (3):
    i) R 1 is -OH, R 2 is -OH and R 3 -H; or
    ii) R 1 is -OCH 3 , R 2 is -H and R 3 -CH 3 ; or
    iii) R 1 is -OH, R 2 is -H and R 3 -CH 3 ; or
    iv) R 1 is -OCH 3 , R 2 is -H and R 3 -H; or
    v) R 1 is -OH, R 2 is -H and R 3 -H; or
    vi) R 1 is -OCH 3 , R 2 is -OH and R 3 -H.

    CRYSTALLINE 6,7-UNSATURATED-7-CARBAMOYL MORPHINANE DERIVATIVE, AND METHOD FOR PRODUCING SAME
    3.
    发明公开
    CRYSTALLINE 6,7-UNSATURATED-7-CARBAMOYL MORPHINANE DERIVATIVE, AND METHOD FOR PRODUCING SAME 审中-公开

    公开(公告)号：EP3560929A2

    公开(公告)日：2019-10-30

    申请号：EP19162034.3

    申请日：2011-11-11

    申请人： Shionogi & Co., Ltd

    发明人： TAMURA, Yoshinori

    IPC分类号： C07D489/08 ,  A61K31/485 ,  A61P1/08 ,  A61P1/10 ,  B01J27/10 ,  C07D271/06

    摘要： The present invention relates to a process for preparing a compound of the formula (II):

    wherein R 1b is a hydroxy-protecting group, R 2 is optionally substituted lower alkyl, and R 3 is optionally substituted lower alkyl, optionally substituted cycloalkyl, substituted or non-substituted aryl or substituted or non-substituted heteroaryl, characterized by reacting a compound of the formula (III):

    wherein R 1b and R 2 are the same as defined above, in the presence or absence of an acid with a compound of the formula: R 3 -N=C=O , wherein R 3 is the same as defined above, or with a compound of the formula: R 3 -NH-C(=O)-X, wherein R 3 is the same as defined above and X is a leaving group.