PURIFICATION OF POSACONAZOLE AND OF POSACONAZOLE INTERMEDIATES
    1.
    发明申请
    PURIFICATION OF POSACONAZOLE AND OF POSACONAZOLE INTERMEDIATES 有权
    噻苯并噻唑和噻唑烷中间体的纯化

    公开(公告)号:US20130211086A1

    公开(公告)日:2013-08-15

    申请号:US13697803

    申请日:2011-05-18

    IPC分类号: C07D307/12 C07D405/12

    摘要: The present invention relates to a process for the preparation of a hydrogen chloride (HCl) salt of a compound of formula (I) wherein Y1 and Y2 are independently F or Cl, preferably F, said compound of formula (I) containing the cis-isomer and the trans-isomer, wherein the process comprises (1) providing the compound of formula (I) comprised in a first suitable solvent; and (2) treating the compound of formula (I) comprised in the first suitable solvent with HCl comprised in a second suitable solvent to obtain the HCl salt of the compound of formula (I).

    摘要翻译: 本发明涉及一种制备式(I)化合物的氯化氢(HCl)盐的方法,其中Y1和Y2独立地是F或Cl,优选F,所述式(I)化合物含有顺式 - 异构体和反式异构体,其中所述方法包括(1)提供包含在第一合适溶剂中的式(I)化合物; 和(2)用包含在第二合适溶剂中的HCl处理包含在第一合适溶剂中的式(I)化合物,得到式(I)化合物的HCl盐。

    Purification of posaconazole and of posaconazole intermediates
    4.
    发明授权
    Purification of posaconazole and of posaconazole intermediates 有权
    泊沙康唑和泊沙康唑中间体的纯化

    公开(公告)号:US09206146B2

    公开(公告)日:2015-12-08

    申请号:US13697803

    申请日:2011-05-18

    摘要: The present invention relates to a process for the preparation of a hydrogen chloride (HCl) salt of a compound of formula (I) wherein Y1 and Y2 are independently F or Cl, preferably F, said compound of formula (I) containing the cis-isomer and the trans-isomer, wherein the process comprises (1) providing the compound of formula (I) comprised in a first suitable solvent; and (2) treating the compound of formula (I) comprised in the first suitable solvent with HCl comprised in a second suitable solvent to obtain the HCl salt of the compound of formula (I).

    摘要翻译: 本发明涉及一种制备式(I)化合物的氯化氢(HCl)盐的方法,其中Y1和Y2独立地为F或Cl,优选为F,所述式(I)化合物含有顺式 - 异构体和反式异构体,其中所述方法包括(1)提供包含在第一合适溶剂中的式(I)化合物; 和(2)用包含在第二合适溶剂中的HCl处理包含在第一合适溶剂中的式(I)化合物,得到式(I)化合物的HCl盐。

    PROCESS FOR THE PREPARATION OF A CHIRAL COMPOUND
    5.
    发明申请
    PROCESS FOR THE PREPARATION OF A CHIRAL COMPOUND 有权
    制备化合物的方法

    公开(公告)号:US20140303184A1

    公开(公告)日:2014-10-09

    申请号:US14125341

    申请日:2012-06-14

    IPC分类号: C07D249/12 A61K31/496

    摘要: The present invention relates to a process for the preparation of a compound of formula (V), in particular posaconazole, wherein said process comprises the steps of (1) providing a mixture comprising a compound of formula (IV), a protic solvent system, and a suitable base; and (2) heating the mixture of (1) to obtain a mixture comprising the compound of formula (V).

    摘要翻译: 本发明涉及一种制备式(V)化合物,特别是泊沙康唑的方法,其中所述方法包括以下步骤:(1)提供包含式(IV)化合物,质子溶剂体系, 和一个合适的基地; 和(2)加热(1)的混合物以获得包含式(V)化合物的混合物。