Carvedilol phosphate sesquihydrate
    2.
    发明授权
    Carvedilol phosphate sesquihydrate 有权
    卡维地洛磷酸倍半水合物

    公开(公告)号:US08344159B2

    公开(公告)日:2013-01-01

    申请号:US12304645

    申请日:2007-06-11

    IPC分类号: C07D209/88

    CPC分类号: C07D209/88

    摘要: The present invention relates a novel crystalline 1-(Carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol phosphate sesquihydrate (Carvedilol dihydrogenphosphate sesquihydrate), methods of preparing the sesquihydrate by adding phosphoric acid to a suspension of Carvedilol in water, water miscible solvents or a mixture of water and water miscible organic solvent followed by isolating the product directly or by adding solvent.

    摘要翻译: 本发明涉及一种新的1-(恶唑-4-基氧基-3 - [[2-(邻甲氧基苯氧基)乙基]氨基] -2-丙醇磷酸倍半水合物(卡维地洛二氢磷酸倍半水合物)的结晶,通过加入制备倍半水合物的方法 磷酸与卡维地洛在水中的混悬液,水溶性溶剂或水与水混溶的有机溶剂的混合物,然后直接或通过加入溶剂分离产物。

    CARVEDILOL PHOSPHATE SESQUIHYDRATE
    4.
    发明申请
    CARVEDILOL PHOSPHATE SESQUIHYDRATE 有权
    CARVEDILOL磷酸盐水溶液

    公开(公告)号:US20090259051A1

    公开(公告)日:2009-10-15

    申请号:US12304645

    申请日:2007-06-11

    IPC分类号: C07D209/82 A61P9/12

    CPC分类号: C07D209/88

    摘要: The present invention relates a novel crystalline 1-(Carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy) ethyl]amino]-2-propanol phosphate sesquihydrate (Carvedilol dihydrogenphosphate sesquihydrate), methods of preparing the sesquihydrate by adding phosphoric acid to a suspension of Carvedilol in water, water miscible solvents or a mixture of water and water miscible organic solvent followed by isolating the product directly or by adding solvent.

    摘要翻译: 本发明涉及一种新的1-(恶唑-4-基氧基-3 - [[2-(邻甲氧基苯氧基)乙基]氨基] -2-丙醇磷酸倍半水合物(卡维地洛二氢磷酸倍半水合物)的结晶,通过加入制备倍半水合物的方法 磷酸与卡维地洛在水中的混悬液,水溶性溶剂或水与水混溶的有机溶剂的混合物,然后直接或通过加入溶剂分离产物。

    Process for the Large Scale Production of Rizatriptan Benzoate
    7.
    发明申请
    Process for the Large Scale Production of Rizatriptan Benzoate 审中-公开
    大量生产利萨曲曲苯甲酸酯的工艺

    公开(公告)号:US20090062550A1

    公开(公告)日:2009-03-05

    申请号:US12093683

    申请日:2006-11-14

    IPC分类号: C07D249/08

    CPC分类号: C07D403/06

    摘要: The present invention provides a method for preparing pure Rizatriptan benzoate having purity more than 99.5% and dimer impurity less than 0.1% comprises, i) Condensation of 1,2,4-Triazole with 4-Nitro benzyl bromide to yield 1-(4-nitrophenyl)methyl-1,2,4-triazole ii) Reducing the 1-(4-nitrophenyl)methyl-1,2,4-triazole to give 1-(4-aminophenyl)methyl-1,2,4-triazole iii) Converting 1-(4-aminophenyl)methyl-1,2,4-triazole to 1-(4-hydrazinophenyl)methyl-1,2,4-triazole hydrochloride iv) Condensing the hydrazine derivative with 4-(Dimethylamino) butanal diethylacetal to get Rizatriptan and v) Salification of Rizatriptan to Rizatriptan benzoate.

    摘要翻译: 本发明提供一种制备纯度大于99.5%,二聚体杂质小于0.1%的纯粹利扎曲普坦苯甲酸酯的方法,包括:i)1,2,4-三唑与4-硝基苄基溴的缩合,得到1-(4- 硝基苯基)甲基-1,2,4-三唑ii)还原1-(4-硝基苯基)甲基-1,2,4-三唑,得到1-(4-氨基苯基)甲基-1,2,4-三唑iii )将1-(4-氨基苯基)甲基-1,2,4-三唑转化为1-(4-肼基苯基)甲基-1,2,4-三唑盐酸盐iv)将肼衍生物与4-(二甲基氨基)丁醛二乙缩醛缩合 获得利扎曲坦和v)利扎曲坦对盐酸利扎曲坦的盐化。