Process for the preparation of naproxene nitroxyalkylesters
    44.
    发明申请
    Process for the preparation of naproxene nitroxyalkylesters 有权
    制备萘普生硝基烷基酯的方法

    公开(公告)号:US20050119339A1

    公开(公告)日:2005-06-02

    申请号:US10625558

    申请日:2003-07-24

    CPC分类号: C07C201/02 C07C203/04

    摘要: A process for obtaining nitroxyalklesters of the 2(S)(6-methoxy-2-naphthyl)-propanoic acid having an enantiomeric excess higher than or equal to 95%, preferably higher than or equal to 98%, characterized in that an halide of the 2-(S)-(6 methoxy-2-naphthyl)propanoic acid of formula A-Hal, wherein A is the acid acyl residue, is reacted in an inert orgariic solvent with an aliphatic nitroxyalkanol HO—Y—ONO2, wherein Y is a C2-C20 alkylene or a cycloalkylene from 3 to 8 carbon atoms, or an alkylene as defined containing a cycloalkylene as defined, in the presence of an inorganic base.

    摘要翻译: 一种获得具有高于或等于95%,优选高于或等于98%的对映异构体过量的2(S)(6-甲氧基-2-萘基) - 丙酸的硝基螺旋体的方法,其特征在于, 其中A是酸酰基残基的式A-Hal的2-(S) - (6-甲氧基-2-萘基)丙酸在惰性溶剂中与脂族硝基链烷醇HO-Y-ONO 2,其中Y是C 2 -C 20亚烷基或3至8个碳原子的亚环烷基,或如所定义的含有如所定义的亚环烷基的亚烷基 在无机碱存在下进行。

    Process for the preparation of adapalene
    50.
    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