Process for the preparation of adapalene
    1.
    发明授权
    Process for the preparation of adapalene 失效
    阿达帕林制备方法

    公开(公告)号:US07345189B2

    公开(公告)日:2008-03-18

    申请号:US11392909

    申请日:2006-03-30

    IPC分类号: C07C69/76

    摘要: A process for the preparation of a compound of formula (I), or a salt thereof wherein R is H, C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; comprising the reaction between a compound of formula (II) wherein R1 and R2 are independently hydrogen, C1-C8 alkyl, aryl, aryl-C1-C8 alkyl, or R1 and R2, taken together, form a —(CH2)m—V—(CH2)n— group, in which V is NR3 or C(R3)2 wherein R3 is hydrogen, C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; and m and n, which can be the same or different, are 1 or 2; with a compound of formula (III) in which R4 and R5 are independently C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; in the presence of a Ni (II) salt, an organic ligand and a basic agent, to obtain a compound of formula (I) wherein R is C1-C8 alkyl, aryl or aryl-C1-C8 alkyl and, if desired, its conversion to a compound of formula (I) wherein R is hydrogen or to a salt thereof.

    摘要翻译: 制备式(I)化合物或其盐的方法,其中R为H,C 1 -C 8烷基,芳基或芳基-C C 1 -C 8烷基; 包括其中R 1和R 2独立地是氢,C 1 -C 8的式(II)化合物之间的反应 烷基,芳基,芳基-C 1 -C 8烷基或R 1和R 2

    Process for the preparation of adapalene
    2.
    发明申请
    Process for the preparation of adapalene 失效
    阿达帕林制备方法

    公开(公告)号:US20060229465A1

    公开(公告)日:2006-10-12

    申请号:US11392909

    申请日:2006-03-30

    IPC分类号: C07C69/76

    摘要: A process for the preparation of a compound of formula (I), or a salt thereof wherein R is H, C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; comprising the reaction between a compound of formula (II) wherein R1 and R2 are independently hydrogen, C1-C8 alkyl, aryl, aryl-C1-C8 alkyl, or R1 and R2, taken together, form a —(CH2)m—V—(CH2)n— group, in which V is NR3 or C(R3)2 wherein R3 is hydrogen, C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; and m and n, which can be the same or different, are 1 or 2; with a compound of formula (III) in which R4 and R5 are independently C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; in the presence of a Ni (II) salt, an organic ligand and a basic agent, to obtain a compound of formula (I) wherein R is C1-C8 alkyl, aryl or aryl-C1-C8 alkyl and, if desired, its conversion to a compound of formula (I) wherein R is hydrogen or to a salt thereof.

    摘要翻译: 制备式(I)化合物或其盐的方法,其中R为H,C 1 -C 8烷基,芳基或芳基-C C 1 -C 8烷基; 包括其中R 1和R 2独立地是氢,C 1 -C 8的式(II)化合物之间的反应 烷基,芳基,芳基-C 1 -C 8烷基或R 1和R 2