Method for reducing residual alcohols in crystalline valacyclovir hydrochloride
    4.
    发明申请
    Method for reducing residual alcohols in crystalline valacyclovir hydrochloride 审中-公开
    降低结晶盐酸伐昔洛韦中残留醇的方法

    公开(公告)号:US20050070711A1

    公开(公告)日:2005-03-31

    申请号:US10688538

    申请日:2003-10-16

    IPC分类号: C07D473/00 C07D473/10

    CPC分类号: C07D473/00

    摘要: Provided is a method of reducing excess residual process solvents, especially excess residual process alcohol (e.g. isopropanol), in valacyclovir hydrochloride to about 1000 ppm (weight) or less by contacting valacyclovir hydrochloride having excess residual process alcohol with moist gas.

    摘要翻译: 提供了通过使具有多余残余工艺醇的伐昔洛韦盐酸盐与湿气接触来将过量的残余工艺溶剂,特别是过量的残余工艺醇(例如异丙醇)在盐酸伐昔洛韦中减少至约1000ppm(重量)或更低的方法。

    Crystalline forms of carvedilol and processes for their preparation
    7.
    发明申请
    Crystalline forms of carvedilol and processes for their preparation 审中-公开
    卡维地洛的结晶形式及其制备方法

    公开(公告)号:US20070043099A1

    公开(公告)日:2007-02-22

    申请号:US11450699

    申请日:2006-06-09

    IPC分类号: A61K31/403 C07D209/82

    CPC分类号: C07D209/88

    摘要: This invention relates to a novel crystalline form of carvedilol, to processes for its preparation, to compositions containing it and to its use in medicine. This invention further relates to a novel process for preparing crystalline carvedilol Form II.

    摘要翻译: 本发明涉及一种新颖的卡维地洛结晶形式,其制备方法,含有它的组合物及其在药物中的用途。 本发明还涉及制备结晶卡维地洛II型的新方法。

    Processes for preparing clarithromycin and clarithromycin intermediate, essentially oxime-free clarithromycin, and pharmaceutical composition comprising the same

    公开(公告)号:US20060205683A1

    公开(公告)日:2006-09-14

    申请号:US11432983

    申请日:2006-05-11

    IPC分类号: A61K31/7048 C07H17/08

    CPC分类号: C07H17/08 C07F7/1892

    摘要: The present invention relates to processes for preparing protected silylated clarithromycin oxime, preferably 6-O-methyl-2′, 4″-bis(trimethylsilyl)-erythromycin A 9-O-(2-methoxyprop-2-yl)oxime (“S-MOP oxime”), and for converting protected silylated clarithromycin oxime, preferably S-MOP oxime, to clarithromycin. Processes for preparing protected silylated clarithromycin oxime according to the present invention, include reacting a silyl oxime derivative with methylating agent in the presence of at least one solvent and a base, where the solvent comprises methyl tertbutyl ether. Processes for converting protected silylated clarithromycin oxime to clarithromycin according to the present invention, include reacting protected silylated clarithromycin oxime with ethanol and water at an ethanol to water ratio of about 1:1, in the presence of an acid and a deoximating agent and cooling the reaction mixture prior to adding sodium hydroxide, where the process takes place without any additional water addition. Further processes for converting protected silylated clarithromycin oxime to clarithromycin, include heating a mixture of protected silylated clarithromycin oxime, acid, and deoximating agent in an ethanol/water solvent to reflux for more than 4 hours, with a two-fold addition of deoximating agent to produce essentially oxime-free clarithromycin.

    Risedronate sodium having a very low content of iron
    9.
    发明授权
    Risedronate sodium having a very low content of iron 失效
    利塞膦酸钠具有非常低的铁含量

    公开(公告)号:US07358360B2

    公开(公告)日:2008-04-15

    申请号:US10759919

    申请日:2004-01-16

    IPC分类号: C07F9/28

    CPC分类号: C07F9/59

    摘要: The present invention relates to a method of making risedronate sodium substantially free of iron including the steps of refluxing, especially with mechanical agitation, a combination of risedronic acid, a sodium base, especially sodium hydroxide, and an iron-reducing amount of EDTA in a liquid that is water, a lower alkanol, or, especially, a mixture of a lower alkanol and water; and isolating risedronate sodium substantially free of iron from the combination.

    摘要翻译: 本发明涉及一种制备基本上不含铁的利塞膦酸钠的方法,包括以下步骤:特别是机械搅拌下,将利塞膦酸,钠碱,特别是氢氧化钠和减铁量的EDTA的组合在 液体是水,低级链烷醇,或特别是低级链烷醇和水的混合物; 并从该组合中分离出基本上不含铁的利塞膦酸钠。

    Processes for preparing clarithromycin and clarithromycin intermediate, essentially oxime-free clarithromycin, and pharmaceutical composition comprising the same
    10.
    发明授权
    Processes for preparing clarithromycin and clarithromycin intermediate, essentially oxime-free clarithromycin, and pharmaceutical composition comprising the same 失效
    用于制备克拉霉素和克拉霉素中间体,基本上不含肟的克拉霉素的方法和包含其的药物组合物

    公开(公告)号:US06617436B2

    公开(公告)日:2003-09-09

    申请号:US09736447

    申请日:2000-12-15

    IPC分类号: C07H100

    CPC分类号: C07H17/08 C07F7/1892

    摘要: The present invention relates to processes for preparing protected silylated clarithromycin oxime, preferably 6-O-methyl-2′, 4″-bis(trimethylsilyl)-erythromycin A 9-O-(2-methoxyprop-2-yl)oxime (“S-MOP oxime”), and for converting protected silylated clarithromycin oxime, preferably S-MOP oxime, to clarithromycin. Processes for preparing protected silylated clarithromycin oxime according to the present invention, include reacting a silyl oxime derivative with methylating agent in the presence of at least one solvent and a base, where the solvent comprises methyl tertbutyl ether. Processes for converting protected silylated clarithromycin oxime to clarithromycin according to the present invention, include reacting protected silylated clarithromycin oxime with ethanol and water at an ethanol to water ratio of about 1:1, in the presence of an acid and a deoximating agent and cooling the reaction mixture prior to adding sodium hydroxide, where the process takes place without any additional water addition. Further processes for converting protected silylated clarithromycin oxime to clarithromycin, include heating a mixture of protected silylated clarithromycin oxime, acid, and deoximating agent in an ethanol/water solvent to reflux for more than 4 hours, with a two-fold addition of deoximating agent to produce essentially oxime-free clarithromycin.

    摘要翻译: 本发明涉及制备受保护的甲硅烷基化克拉霉素肟,优选6-O-甲基-2',4“ - 双(三甲基甲硅烷基) - 红霉素A 9-O-(2-甲氧基丙-2-基)肟(” S-MOP肟“),并将保护的甲硅烷基化克拉霉素肟(优选S-MOP肟)转化为克拉霉素。 根据本发明的制备受保护的甲硅烷基化克拉霉素肟的方法包括使甲硅烷基肟衍生物与甲基化剂在至少一种溶剂和碱的存在下反应,其中溶剂包括甲基叔丁基醚。 将受保护的甲硅烷基化克拉霉素肟转化为克拉霉素的方法包括在酸和脱肟剂的存在下,将保护的甲硅烷基化克拉霉素肟与乙醇和水以约1:1的乙醇与水反应并冷却 在加入氢氧化钠之前的反应混合物,其中该方法进行而没有任何额外的水添加。 将受保护的甲硅烷基化克拉霉素肟转化为克拉霉素的其它方法包括在乙醇/水溶剂中将受保护的甲硅烷基化克拉霉素肟,酸和脱肟剂的混合物加热回流4小时以上,加入二肟剂至 产生基本上无肟的克拉霉素。