Process for the preparation of pyridine compounds
    25.
    发明授权
    Process for the preparation of pyridine compounds 失效
    吡啶化合物的制备方法

    公开(公告)号:US07605268B2

    公开(公告)日:2009-10-20

    申请号:US11737852

    申请日:2007-04-20

    IPC分类号: C07D401/12

    CPC分类号: C07D471/04 C07D401/12

    摘要: A process for preparation of a compound of formula (I), both as the isomeric mixture and individual isomers, wherein Q is ═CR8— or ═N—; each R1, R2, R3, R4 is independently selected from hydrogen, halogen, hydroxy; nitro; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen or C1-C6 alkoxy; phenyl-C1-C6 alkyl; phenyl-C1-C6 alkoxy; and —N(RaRb) wherein each Ra and Rb is independently hydrogen or C1-C6 alkyl or Ra and Rb, taken together with the nitrogen atom they are linked to, form a saturated heterocyclic ring; and each R5, R6, R7, R8 is independently selected from hydrogen, halogen, hydroxy; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen; C1-C6 alkyl-carbonyl, C1-C6 alkoxy-carbonyl, and oxazol-2-yl; comprising converting a compound of formula (IV), to said compound of formula (I), in the presence of a catalyst, if necessary in an organic solvent.

    摘要翻译: 制备式(I)化合物的方法,均为异构体混合物和各异构体,其中Q为-CR8-或-N-; 每个R 1,R 2,R 3,R 4独立地选自氢,卤素,羟基; 硝基 任选被羟基取代的C 1 -C 6烷基; 烷硫基C1-C6; 任选被卤素或C 1 -C 6烷氧基取代的C 1 -C 6烷氧基; 苯基-C 1 -C 6烷基; 苯基-C 1 -C 6烷氧基; 和-N(RaRb),其中每个R a和R b独立地是氢或C 1 -C 6烷基或R a和R b与它们连接的氮原子一起形成饱和杂环; 并且每个R 5,R 6,R 7,R 8独立地选自氢,卤素,羟基; 任选被羟基取代的C 1 -C 6烷基; 烷硫基C1-C6; 任选被卤素取代的C 1 -C 6烷氧基; C 1 -C 6烷基 - 羰基,C 1 -C 6烷氧羰基和恶唑-2-基; 包括在催化剂存在下,如果需要在有机溶剂中将式(Ⅳ)化合物转化为所述式(Ⅳ)化合物。

    Process for the preparation of adapalene
    26.
    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
    28.
    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

    PROCESS FOR THE PREPARATION OF ZILEUTON
    30.
    发明申请
    PROCESS FOR THE PREPARATION OF ZILEUTON 审中-公开
    制备ZILEUTON的方法

    公开(公告)号:US20090286996A1

    公开(公告)日:2009-11-19

    申请号:US12423122

    申请日:2009-04-14

    摘要: Process for preparing a compound of formula (I), or a salt thereof, comprising reacting of a compound of formula (II) wherein X and R are as herein defined; with a compound of formula (III) NH2OZ  (III) wherein Z is a hydroxy protecting group, in presence of a catalyst, to obtain a compound of formula (IV), or a salt thereof, removing the hydroxyl protecting group to obtain a compound of formula (V), or a salt thereof; converting a compound of formula (V), or a salt thereof, into a compound of formula (I), or a salt thereof; and, if desired, converting a compound of formula (I) into a salt thereof, or vice versa.

    摘要翻译: 制备式(I)化合物或其盐的方法,包括其中X和R如本文所定义的式(II)化合物的反应; 与式(III)化合物(其中Z为羟基保护基)在催化剂存在下反应,得到式(Ⅳ)化合物或其盐,除去羟基保护基,得到化合物 式(Ⅴ)化合物或其盐; 将式(Ⅴ)化合物或其盐转化为式(I)化合物或其盐; 如果需要,将式(I)化合物转化为其盐,反之亦然。