利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

5 条记录 (耗时 0.034 秒)

    Process for the preparation of biologically active tetrahydrobenzthiazole derivative
    4.
    发明申请
    Process for the preparation of biologically active tetrahydrobenzthiazole derivative 审中-公开

    公开(公告)号：US20070123573A1

    公开(公告)日：2007-05-31

    申请号：US10588564

    申请日：2005-04-25

    申请人： Dhiren Mistry ,  Kamlesh Soni ,  Sanjay Vasoya ,  Vinod Kansal

    发明人： Dhiren Mistry ,  Kamlesh Soni ,  Sanjay Vasoya ,  Vinod Kansal

    IPC分类号： A61K31/428 ,  C07D277/82

    CPC分类号： C07D277/82

    摘要： Improved process for the preparation of the intermediate compound of formula II for formation of biological active tetrahydrobenzothiazole compound of formula (I) as well as the biological active tetrahydrobenzothiazole compound of formula (I) and/or its pharmaceutically acceptable salts or solvates. The process comprises reacting 4-amino cyclohexanol of formula (III) or its acid addition salts with phthalic anhydride in presence of acid catalyst and their salts, in polar aprotic solvent or its mixture with organic solvent, capable of removing water azeotropically to give 4-(phthalimido)-cyclohexanol of formula (IV); oxidizing 4-(phthalimido)-cyclohexanol of formula (IV) to give 4-(phthalimido)-cyclohexanone of formula (V); brominating 4-(phthalimido)-cyclohexanone of formula (V) with brominating agent in organic solvent in presence of Lewis acid catalyst to prepare 2-bromo-4-(phthalimido)-cyclohexanone of formula (VI); treating 2-bromo-4-(phthalimido)-cyclohexanone of formula (VI) with thiourea in organic solvent in presence of base to give 2-amino-6-phthalimido-4,5,6,7-tetrahydro benzothiazol of formula (VII); reacting compound of formula (VII) with hydrazine hydrate and base in polar solvent to give racemic 2,6-diamino-4,5,6,7-tetrahydro-1,3-benzothiazole of formula (VIII); resolving racemic 2,6-diamino-4,5,6,7-tetrahydro-1,3-benzothiazole of formula (VIII) to prepare (6S)-2,6-diamino-4,5,6,7-tetrahydro-1,3-benzothiazole of formula (II). To form the compound of Formula I and if desired its salts/solvates the above process is carried out with further steps of coupling (6S)-2,6-dimino-4,5,6,7-tetrahydro-1,3-benzothiazole of formula (II) with propionaldehyde in presence of mineral acid in polar organic solvent and reducing agent to prepare (S)-(−)-2-Amino-6-(n-propylamino)-4,5,6,7-tetrahydrobenzothiazole of formula (I);and if desired converting (S)-(−)-2-Amino-6-(propylamino)-4,5,6,7-tetrahydrobenzothiazole to its pharmaceutically acceptable salts or solvates.

    Process for preparing Valsartan
    5.
    发明申请
    Process for preparing Valsartan 失效
    缬沙坦制备方法

    公开(公告)号：US20060258878A1

    公开(公告)日：2006-11-16

    申请号：US11491638

    申请日：2006-07-24

    申请人： Rohit Soni ,  Sanjay Vasoya ,  Ravindra Ghotikar ,  Anand Pandey ,  Hetal Shah

    发明人： Rohit Soni ,  Sanjay Vasoya ,  Ravindra Ghotikar ,  Anand Pandey ,  Hetal Shah

    IPC分类号： C07C255/49

    CPC分类号： C07D257/04 ,  C07C255/58

    摘要： The invention relates to novel compound of formula (IV), which is an organic acid salt of N-[(2′-cyanobiphenyl-4-yl)methyl]-(L)-valine ester. This compound is an useful intermediate for process of preparation of Valsartan of formula (I), chemically known as (S)—N-(1-Carboxy-2-methylprop-1-yl)-N-pentanoyl-N-[2′-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]amine. This invention also relates to a process for preparing Valsartan using novel intermediate of formula (IV).

    摘要翻译： 本发明涉及新的式（Ⅳ）化合物，它是N - [（2'-氰基联苯-4-基）甲基] - （L） - 缬氨酸酯的有机酸盐。 该化合物是制备式（I）的缬沙坦的方法的有用的中间体，化学上称为（S）-N-（1-羧基-2-甲基丙-1-基）-N-戊酰基-N- [2' - （1H-四唑-5-基）联苯-4-基甲基]胺。 本发明还涉及使用式（IV）的新型中间体制备缬沙坦的方法。