OPTICALLY ACTIVE METHYLHYDROXYLAMINOPROPANOL DERIVATIVE AND ITS USE AS INTERMEDIATE FOR PREPARATION OF (S)-(-)-3-METHYLAMINO-1-(2-THIENYL)PROPAN-1-OL
    1.
    发明申请
    OPTICALLY ACTIVE METHYLHYDROXYLAMINOPROPANOL DERIVATIVE AND ITS USE AS INTERMEDIATE FOR PREPARATION OF (S)-(-)-3-METHYLAMINO-1-(2-THIENYL)PROPAN-1-OL 有权
    (S) - ( - ) - 3-甲基氨基-1-(2-噻吩基)丙烷-1-醇的光学活性甲基羟基氨基丙酸衍生物及其用作中间体

    公开(公告)号:US20090112001A1

    公开(公告)日:2009-04-30

    申请号:US12120748

    申请日:2008-05-15

    IPC分类号: C07D333/20

    CPC分类号: C07D333/20

    摘要: The present invention provides an (S)-methylhydroxylaminopropanol derivative and the (S)-methylhydroxylaminopropanol derivative of the present invention is used as an intermediate for preparation of (S)-(−)-3-methylamino-1-(2-thienyl)propan-1-ol, which is an intermediate for preparation of (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine oxalate. The present invention also provides a process for preparing (S)-(−)-3-methylamino-1-(2-thienyl)propan-1-ol with higher yield and lower cost, wherein the (S)-methylhydroxylaminopropanol derivative is used as an intermediate.

    摘要翻译: 本发明提供(S) - 甲基羟基氨基丙醇衍生物,本发明的(S) - 甲基羟基氨基丙醇衍生物用作制备(S) - ( - ) - 3-甲基氨基-1-(2-噻吩基) 丙烷-1-醇,其是制备(S) - (+) - N-甲基-3-甲基-3-(1-萘氧基)-3-(2-噻吩基)丙胺草酸盐的中间体。 本发明还提供了一种制备(S) - ( - ) - 3-甲基氨基-1-(2-噻吩基)丙-1-醇的方法,其产率更高,成本更低,其中使用(S) - 甲基羟基氨基丙醇衍生物 作为中间体。

    OPTICALLY ACTIVE METHYLHYDROXYLAMINOPROPANOL DERIVATIVE AND ITS USE AS INTERMEDIATE FOR PREPARATION OF (S)-(-)-3-METHYLAMINO-1-(-2-THIENYL)PROPAN-1-OL
    2.
    发明申请
    OPTICALLY ACTIVE METHYLHYDROXYLAMINOPROPANOL DERIVATIVE AND ITS USE AS INTERMEDIATE FOR PREPARATION OF (S)-(-)-3-METHYLAMINO-1-(-2-THIENYL)PROPAN-1-OL 有权
    (S) - ( - ) - 3-甲基氨基-1-(2-噻吩基)丙烷-1-醇的光学活性甲基羟基氨基丙酰胺衍生物及其用作中间体

    公开(公告)号:US20120190869A1

    公开(公告)日:2012-07-26

    申请号:US13436253

    申请日:2012-03-30

    IPC分类号: C07D333/20

    CPC分类号: C07D333/20

    摘要: The present invention provides an (S)-methylhydroxylaminopropanol compound and the (S)-methylhydroxylaminopropanol compound of the present invention is used as an intermediate for preparation of (S)-(−)-3-methylamino-1-(2-thienyl)propan-1-ol, which is an intermediate for preparation of (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine oxalate. The present invention also provides a process for preparing (S)-(+3-methylamino-1-(2-thienyl)propan-1-ol with higher yield and lower cost, wherein the (S)-methylhydroxylaminopropanol compound is used as an intermediate.

    摘要翻译: 本发明提供(S) - 甲基羟基氨基丙醇化合物,本发明的(S) - 甲基羟基氨基丙醇化合物用作制备(S) - ( - ) - 3-甲基氨基-1-(2-噻吩基) 丙烷-1-醇,其是制备(S) - (+) - N-甲基-3-甲基-3-(1-萘氧基)-3-(2-噻吩基)丙胺草酸盐的中间体。 本发明还提供了一种制备(S) - (+ 3-甲基氨基-1-(2-噻吩基)丙-1-醇的方法,其产率高,成本较低,其中(S) - 甲基羟基氨基丙醇化合物用作 中间。

    METHOD FOR TREATING HEPATITIS B
    3.
    发明申请
    METHOD FOR TREATING HEPATITIS B 审中-公开
    治疗乙型肝炎的方法B

    公开(公告)号:US20130123204A1

    公开(公告)日:2013-05-16

    申请号:US13735620

    申请日:2013-01-07

    IPC分类号: A61K31/352

    摘要: The disclosure provides a method for treating hepatitis B, including: administering an effective amount of proanthocyanidins wherein the formula of a monomer of the proanthocyanidins is shown as Formula (I): wherein R1 is OCH3, R2 is OH and R3 is H, or R1 is OH and R2 and R3 both are H, or R1 and R2 both are OH and R3 is H, or R1, R2 and R3 all are OH, and R4 is 3-(α)-OH, 3-(β)-OH, 3-(α)-O-sugar or 3-(β)-O-sugar. Bonding between adjacent monomers take place at C4, C8 Carbon-carbon bond or C2, C7 oxygen bond of A type or C4, C8 or C4, C6 Carbon-carbon bond of B type or C type of proanthocyanidins. And the polymerized number is from 2 to 30.

    摘要翻译: 本发明提供了一种治疗乙型肝炎的方法,包括:给予有效量的原花青素,其中原花青素单体的式如式(I)所示:其中R1是OCH3,R2是OH,R3是H,或R1 是OH,R 2和R 2都是H,或者R 1和R 2都是OH,R 3是H,或者R 1,R 2和R 3都是OH,R 4是3-(α)-OH,3-(β)-OH ,3-(α)-O-糖或3-(β)-O-糖。 相邻单体之间的键合发生在C4,C8碳 - 碳键或A型的C2,C7氧键或C4,C8或C4,C6B型或C型原花色素的碳 - 碳键。 聚合数为2〜30。