NEW SYNTHESIS PROCESS OF ANTIPARASITIC DRUG SELAMECTIN
    6.
    发明公开
    NEW SYNTHESIS PROCESS OF ANTIPARASITIC DRUG SELAMECTIN 有权
    消除合成蛋白抗菌素抗生素

    公开(公告)号:EP2835376A1

    公开(公告)日:2015-02-11

    申请号:EP13773160.0

    申请日:2013-04-02

    IPC分类号: C07H17/08

    CPC分类号: C07H1/00 C07H17/08

    摘要: Provided in the present invention are novel key intermediates of selamectin and the preparation method thereof. Also provided is a new synthesis process, using doramectin as a starting material, and obtaining selamectin via hydrogenation, oxidation, oximation and desugaring. The new process of the present invention has few steps, and is simple to operate, high in yield, low in cost and causes little pollution, and is more suitable for large scale industrial production.

    摘要翻译: 本发明提供了新颖的新颖的关键中间体及其制备方法。 还提供了一种新的合成方法,使用多拉菌素作为起始原料,并通过氢化,氧化,肟化和脱除得到selamectin。 本发明的新工艺步骤很少,操作简单,产量高,成本低,污染少,更适合大规模工业化生产。

    METHOD FOR PREPARING SOFOSBUVIR CRYSTAL FORM-6
    7.
    发明公开
    METHOD FOR PREPARING SOFOSBUVIR CRYSTAL FORM-6 审中-公开
    制备SOFOSBUVIR晶体形式-6的方法

    公开(公告)号:EP3241837A1

    公开(公告)日:2017-11-08

    申请号:EP15874972.1

    申请日:2015-11-11

    CPC分类号: C07H1/06 C07H19/06 C07H19/10

    摘要: The present invention relates to a method for preparing Sofosbuvir crystal form-6. The method is simple in operation, stable in process condition, good in reproducibility, high in yield rate and high in purity, viscous gel-type products are not formed during the process, the problem of blocking of a discharge port is solved, and the method is suitable for mass industrial production and has high economic value.

    摘要翻译: Sofosbuvir晶形-6的制备方法技术领域本发明涉及Sofosbuvir晶形-6的制备方法。 该方法操作简单,工艺条件稳定,重复性好,收率高,纯度高,在工艺过程中不形成粘性凝胶型产品,解决了出料口堵塞问题, 方法适用于大量工业生产,具有较高的经济价值。

    CRYSTAL FORM OF DABIGATRAN ETEXILATE MESYLATE AND PREPARATION METHOD AND USE THEREOF
    8.
    发明公开
    CRYSTAL FORM OF DABIGATRAN ETEXILATE MESYLATE AND PREPARATION METHOD AND USE THEREOF 审中-公开
    侠盗猎车手侠盗猎车手

    公开(公告)号:EP3115360A1

    公开(公告)日:2017-01-11

    申请号:EP15759282.5

    申请日:2015-03-04

    摘要: The present invention relates to novel crystal forms M and N of dabigatran etexilate mesylate and preparation method and uses thereof, wherein the X-Ray powder diffractogram of the crystal form M has characteristic peaks at the following 2θ diffraction angles: 5.7±0.2°, 6.2±0.2°, 11.2±0.2°, 12.4±0.2°, 18.2±0.2°, 21.4±0.2°, 21.8±0.2° and 23.6±0.2°; and the X-Ray powder diffractogram of the crystal form N has characteristic peaks at the following 2θ diffraction angles: 6.0±0.2°, 11.8±0.2°, 18.2±0.2°, 21.6±0.2°, 24.4±0.2°, 27.7±0.2° and 29.7±0.2°. The crystal forms of the present invention have excellent properties in the aspects of leaching time, biological release, chemical stability and processing adaptability.

    摘要翻译: 本发明涉及甲磺酸达比加群酯的新型结晶形式M和N及其制备方法和用途,其中晶型M的X射线粉末衍射图在以下2θ衍射角为5.7±0.2°处具有特征峰, 6.2±0.2°,11.2±0.2°,12.4±0.2°,18.2±0.2°,21.4±0.2°,21.8±0.2°和23.6±0.2°; 晶体形式N的X射线粉末衍射图在以下2θ衍射角处具有特征峰:6.0±0.2°,11.8±0.2°,18.2±0.2°,21.6±0.2°,24.4±0.2°,27.7± 0.2°和29.7±0.2°。 本发明的结晶形式在浸出时间,生物释放,化学稳定性和加工适应性方面具有优异的性能。