PROCESS FOR PREPARING IRBESARTAN
    3.
    发明申请
    PROCESS FOR PREPARING IRBESARTAN 审中-公开
    制备IRBESARTAN的方法

    公开(公告)号:US20090286990A1

    公开(公告)日:2009-11-19

    申请号:US11569380

    申请日:2005-05-20

    IPC分类号: C07D487/10 C07C237/20

    CPC分类号: C07D403/10

    摘要: A process for preparing irbesartan comprises pentanoylation of cycloleucine in the presence of sodium hydroxide to form n-pentanoyl cycloleucine, condensing this product with 2-(4-aminomethyl phenyl) benzonitrile using dicyclohexyl carbodiimide and 1-hydroxy benzotriazole as a catalyst to form the 4-(&quest-N-pentanoyl amino) cyclopentamido methyl-2′-cyano biphenyl compound, and then cyclizing using trifluoroacetic acid in the presence of an aromatic solvent to form cyano irbesartan. Cyano irbesartan is converted to irbesartan by reaction with tributyltin chloride and sodium azide in the presence of an aromatic solvent.

    摘要翻译: 制备厄贝沙坦的方法包括在氢氧化钠存在下对环己基氨基甲酸进行戊酰化以形成正戊基环己烯,使用二环己基碳二亚胺和1-羟基苯并三唑作为催化剂将该产物与2-(4-氨基甲基苯基)苄腈缩合形成4 - (&N-N-戊酰基氨基)环戊酰氨基甲基-2'-氰基联苯化合物,然后在芳族溶剂存在下使用三氟乙酸环化形成氰基厄贝沙坦。 在芳香族溶剂存在下,通过与三丁基氯化锡和叠氮化钠反应将氰基厄贝沙坦转化成厄贝沙坦。

    Methods for the preparation of polymorphs of doxazosin mesylate
    4.
    发明授权
    Methods for the preparation of polymorphs of doxazosin mesylate 有权
    制备甲磺酸多沙唑嗪多晶型物的方法

    公开(公告)号:US06399775B1

    公开(公告)日:2002-06-04

    申请号:US09615241

    申请日:2000-07-13

    IPC分类号: C07D40514

    CPC分类号: C07D405/12

    摘要: Form D of doxazosin mesylate and a process for preparing Form D of doxazosin mesylate is described. The process is (a) dissolving doxazosin base and methane sulfonic acid in an alcohol having 1 to 8 carbon atoms; (b) precipitating Form D of doxazosin mesylate from the resulting solution; and (c) separating the Form D of doxazosin mesylate.

    摘要翻译: 描述了甲磺酸多沙唑嗪的D型和制备甲磺酸多沙唑嗪的D型的方法。 该方法是(a)将多沙唑嗪碱和甲磺酸溶解在具有1-8个碳原子的醇中; (b)从所得溶液中沉淀甲磺酸多沙唑嗪的D型; 和(c)分离甲磺酸多沙唑嗪的D型。