IMPROVED PROCESS FOR PREPARING MONTELUKAST AND SALTS THEREOF
    7.
    发明申请
    IMPROVED PROCESS FOR PREPARING MONTELUKAST AND SALTS THEREOF 有权
    改进方法制备MONTELUKAST及其销售费用

    公开(公告)号:US20110112300A1

    公开(公告)日:2011-05-12

    申请号:US12673916

    申请日:2009-05-25

    IPC分类号: C07D215/14

    CPC分类号: C07D215/18

    摘要: A method for the preparation of montelukast and salts thereof has been described. The method comprises of following steps: (a) (S)-1-(3-((E)-2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-isopropenylphenyljpropyl methane sulphonate (styrene mesylate salt) (b) coupling with 1-(mercapto methyl)cyclopropane acetic acid followed by salification with an amine gives styrene amine salt (c) Converting styrene amine salt to Montelukast amine salt (d) Converting Montelukast amine salt to Montelukast free acid and or its required alkali/alkaline salt.

    摘要翻译: 已经描述了制备孟鲁司特及其盐的方法。 该方法包括以下步骤:(a)(S)-1-(3 - ((E)-2-(7-氯喹啉-2-基)乙烯基)苯基)-3-(2-异丙烯基苯基丙基甲磺酸酯 甲磺酸盐)(b)与1-(巯基甲基)环丙烷乙酸偶联,然后用胺成盐,得到苯乙烯胺盐(c)将苯乙烯胺盐转化为孟鲁司特胺盐(d)将蒙特鲁卡斯特胺盐转化为蒙特鲁卡斯特游离酸和 或其所需的碱/碱盐。

    Process for preparing Montelukast and salts thereof
    8.
    发明授权
    Process for preparing Montelukast and salts thereof 有权
    制备孟鲁司特及其盐的方法

    公开(公告)号:US08367834B2

    公开(公告)日:2013-02-05

    申请号:US13474135

    申请日:2012-05-17

    IPC分类号: C07D215/18

    CPC分类号: C07D215/18

    摘要: A method for the preparation of montelukast and salts thereof has been described. The method comprises of following steps: (a) (S)-1-(3-((E)-2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-isopropenylphenyljpropyl methane sulphonate (styrene mesylate salt) (b) coupling with 1-(mercaptomethyl)cyclopropane acetic acid followed by salification with an amine gives styrene amine salt (c) Converting styrene amine salt to Montelukast amine salt (d) Converting Montelukast amine salt to Montelukast free acid and or its required alkali/alkaline salt.

    摘要翻译: 已经描述了制备孟鲁司特及其盐的方法。 该方法包括以下步骤:(a)(S)-1-(3 - ((E)-2-(7-氯喹啉-2-基)乙烯基)苯基)-3-(2-异丙烯基苯基丙基甲磺酸酯 甲磺酸盐)(b)与1-(巯基甲基)环丙烷乙酸偶联,然后用胺成盐,得到苯乙烯胺盐(c)将苯乙烯胺盐转化为蒙特鲁卡斯特胺盐(d)将蒙特卡斯特胺盐转化为蒙特鲁卡斯特游离酸和/ 其所需的碱/碱盐。

    Process for preparing montelukast and salts thereof
    9.
    发明授权
    Process for preparing montelukast and salts thereof 有权
    孟鲁司特及其盐的制备方法

    公开(公告)号:US08207343B2

    公开(公告)日:2012-06-26

    申请号:US12673916

    申请日:2009-05-25

    IPC分类号: C07D215/18

    CPC分类号: C07D215/18

    摘要: A method for the preparation of montelukast and salts thereof has been described. The method comprises of following steps: (a) (S)-1-(3-((E)-2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-isopropenylphenyl)propyl methane sulphonate (styrene mesylate salt) (b) coupling with 1-(mercapto methyl)cyclopropane acetic acid followed by salification with an amine gives styrene amine salt (c) Converting styrene amine salt to Montelukast amine salt (d) Converting Montelukast amine salt to Montelukast free acid and or its required alkali/alkaline salt.

    摘要翻译: 已经描述了制备孟鲁司特及其盐的方法。 该方法包括以下步骤:(a)(S)-1-(3 - ((E)-2-(7-氯喹啉-2-基)乙烯基)苯基)-3-(2-异丙烯基苯基)丙基甲磺酸盐 (苯乙烯甲磺酸盐)(b)与1-(巯基甲基)环丙烷乙酸偶联,然后与胺成盐,得到苯乙烯胺盐(c)将苯乙烯胺盐转化为蒙特鲁卡斯特胺盐(d)将Montelukast胺盐转化为Montelukast 酸和/或其所需的碱/碱盐。

    Process for the preparation of Telmisartan
    10.
    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