CARVEDILOL PHOSPHATE SESQUIHYDRATE
    2.
    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。

    Carvedilol phosphate sesquihydrate
    4.
    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。

    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。

    Process for the preparation of Telmisartan
    8.
    发明授权
    Process for the preparation of Telmisartan 有权
    制备替米沙坦的方法

    公开(公告)号:US07884214B2

    公开(公告)日:2011-02-08

    申请号:US12064150

    申请日:2006-07-19

    IPC分类号: C07D403/02

    CPC分类号: C07D235/20

    摘要: The present invention encompasses a method for the preparation of Telmisartan comprises, through Telmisartan dihydrochloride comprises i) Condensing 4-Methyl-2-n-propyl-1H-benzimidazole-6-carboxylic acid with N-Methyl-O-phenylenediamine dihydrochloride to yields 4-methyl-6 (1-methyl benzimidazol-2-yl)-2-n-propyl 1H-benzimidazole ii) Treating 4-methyl-6-(1-methylbenzimidazol-2-yl)-2-n-propyl-1H-benzimidazole with 4′-(bromomethyl)-2-biphenyl-2-carboxylate in presence of a base in an organic solvent and isolating the ester as acid addition salt iii) Converting ester acid addition salt to Telmisartan dihydrochloride and iv) Converting Telmisartan dihydrochloride to Telmisartan.

    摘要翻译: 本发明包括用于制备替米沙坦的方法,其包括通过替米沙坦二盐酸盐包括i)使4-甲基-2-正丙基-1H-苯并咪唑-6-羧酸与N-甲基-O-苯二胺二盐酸盐冷凝,得到4 - 甲基-6(1-甲基苯并咪唑-2-基)-2-正丙基1H-苯并咪唑ii)处理4-甲基-6-(1-甲基苯并咪唑-2-基)-2-正丙基-1H- 苯并咪唑与4' - (溴甲基)-2-联苯基-2-羧酸叔丁酯在碱的存在下在有机溶剂中反应,并将酯分离为酸加成盐iii)将酯酸加成盐转化为替米沙坦二盐酸盐,和iv)将替米沙坦二盐酸盐转化为 替米沙坦

    Process for the Large Scale Production of Stavudine
    9.
    发明申请
    Process for the Large Scale Production of Stavudine 有权
    司他夫定大规模生产工艺

    公开(公告)号:US20080312428A1

    公开(公告)日:2008-12-18

    申请号:US12094586

    申请日:2006-11-17

    IPC分类号: C07H19/06

    CPC分类号: C07H19/06 C07D405/04

    摘要: The present invention provides a method for preparing pure Stavudine having purity more than 99.5% comprises: i) Converting 3′,5′-anhydrothymidine to crude Stavudine, ii) Converting crude Stavudine to stable solvates of Stavudine, iii) Desolvation of the solvates to give pure Stavudine. The present invention also disclosed novel solvates of Stavudine and conversion of novel Stavudine solvates to Stavudine.

    摘要翻译: 本发明提供了一种制备纯度大于99.5%的纯度司他夫定的方法,包括:i)将3',5'-脱水胸苷转化为粗制司他夫定,ii)将粗制司他夫定转化为司他夫定的稳定溶剂化物,iii)溶剂化物的去溶剂化 给予纯粹的司他夫定。 本发明还公开了新的司他夫定溶剂化物,并将新的司他夫定溶剂化物转化为司他夫定。