PROCESS FOR REGORAFENIB
    1.
    发明申请
    PROCESS FOR REGORAFENIB 有权
    REGORAFIBIB的过程

    公开(公告)号:US20160251313A1

    公开(公告)日:2016-09-01

    申请号:US15026694

    申请日:2014-09-29

    IPC分类号: C07D213/81

    CPC分类号: C07D213/81 C07B2200/13

    摘要: The present invention provides processes for the preparation of i) Regorafenib (4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide, BAY 73-4506, Stivarga®) and its pharmaceutically acceptable salt thereof; ii) a crystalline solid of Regorafenib tosylate; iii) Regorafenib Polymorph I from Regorafenib tosylate, and iv) a pure 4-(4-amino-3-fluorophenoxy)-N-methylpicolinamide from 4-amino-3-fluorophenol and 4-chloro-N-methylpicolinamide in the presence of potassium tert-butoxide.

    摘要翻译: 本发明提供了制备i)雷卡非尼(4- [4 - ({[4-氯-3-(三氟甲基)苯基]氨基甲酰基}氨基)-3-氟苯氧基] -N-甲基吡啶-2-甲酰胺的方法, BAY 73-4506,Stivarga?)及其药学上可接受的盐; ii)瑞波非尼甲苯磺酸盐的结晶固体; iii)从罗非拉布甲苯磺酸盐获得的瑞考非非多晶型I,和iv)在钾存在下,由4-氨基-3-氟苯酚和4-氯-N-甲基吡啶酰胺制得纯的4-(4-氨基-3-氟苯氧基)-N-甲基吡啶酰胺 叔丁醇盐。

    PROCESS FOR THE RESOLUTION OF OMEPRAZOLE
    2.
    发明申请
    PROCESS FOR THE RESOLUTION OF OMEPRAZOLE 有权
    奥美拉唑分解方法

    公开(公告)号:US20140235859A1

    公开(公告)日:2014-08-21

    申请号:US14264450

    申请日:2014-04-29

    IPC分类号: C07D401/12

    CPC分类号: C07D401/12 C07D401/14

    摘要: The present invention relates to process for the resolution of omeprazole. The present invention further provides a novel compound of enantiomers of omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a solid of (R)- or (S)-omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a process for the preparation of esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention also provides a process for the preparation of recovery of chiral BINOL.

    摘要翻译: 本发明涉及奥美拉唑的分辨方法。 本发明还提供了奥美拉唑环胺盐的新型对映体化合物及其制备方法。 本发明还提供(R) - 或(S) - 奥美拉唑环胺盐的固体及其制备方法。 本发明还提供了制备基本上不含其三水合物形式的艾美拉唑镁二水合物的方法。 本发明还提供了制备手性BINOL回收的方法。