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96 条记录 (耗时 0.031 秒)

    AN IMPROVED PROCESS FOR THE PREPARATION OF FOSAPREPITANT HAVING IMPROVED PURITY
    8.
    发明申请
    AN IMPROVED PROCESS FOR THE PREPARATION OF FOSAPREPITANT HAVING IMPROVED PURITY 审中-公开
    制备具有提高纯度的复方的改进方法

    公开(公告)号：WO2015083033A1

    公开(公告)日：2015-06-11

    申请号：PCT/IB2014/066279

    申请日：2014-11-24

    申请人： PIRAMAL ENTERPRISES LIMITED

    发明人： KRISHNAMURTHY, Dhileepkumar ,  MORTHALA, Raghavendar Rao ,  JAGTAP, Ashutosh ,  LADKAT, Prashant ,  KUMBHAR, Ajay

    IPC分类号： C07F9/6558

    CPC分类号： C07F9/65583

    摘要： The present invention relates to an improved process for the preparation of [3-{[(2 R ,3 S )-2- [(1 R )-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4- yl]methyl}-5-oxo-2 H -1,2,4-triazol-1-yl]phosphonic acid (Fosaprepitant or the compound of formula I) or its pharmaceutically acceptable salt, having palladium (Pd) content less than 1 ppm comprising catalytic hydrogenation of the compound of formula II with Pd catalyst optionally in the presence of base, to give the compound of formula I or the pharmaceutically acceptable salt thereof, optionally isolating the compound of formula I or the pharmaceutically acceptable salt and treating the compound of formula I or the pharmaceutically acceptable salt thereof twice with the metal scavenger to obtain the compound of formula I or the pharmaceutically acceptable salt thereof having Pd content less than 1 ppm.

    摘要翻译： 本发明涉及制备[3 - {[（2R，3S）-2 - [（1R）-1- [3,5-双（三氟甲基）苯基]乙氧基] -3-（4 - 氟苯基）吗啉-4-基]甲基} -5-氧代-2H-1,2,4-三唑-1-基]膦酸（Fosaprepitant或式I化合物）或其药学上可接受的盐，其具有钯（ Pd）含量小于1ppm，包括式Pd化合物与Pd催化剂任选在碱存在下的催化氢化，得到式I化合物或其药学上可接受的盐，任选分离式I化合物或其药学上可接受的盐 可接受的盐，并且用金属清除剂将式I化合物或其药学上可接受的盐进行两次处理，得到具有Pd含量小于1ppm的式I化合物或其药学上可接受的盐。

    AN IMPROVED PROCESS FOR PREPARATION OF AN INTERMEDIATE OF THE PYRROLIDINE SUBSTITUTED FLAVONES
    10.
    发明申请
    AN IMPROVED PROCESS FOR PREPARATION OF AN INTERMEDIATE OF THE PYRROLIDINE SUBSTITUTED FLAVONES 审中-公开
    制备吡咯烷酮取代的氟的中间体的改进方法

    公开(公告)号：WO2014128524A1

    公开(公告)日：2014-08-28

    申请号：PCT/IB2013/051334

    申请日：2013-02-19

    申请人： PIRAMAL ENTERPRISES LIMITED

    发明人： CHENNAMSETTY, Suneelmanoharbabu ,  PATIL, Rajendra ,  HAREL, Prashant ,  HARIHARAN, Sivaramakrishnan

    IPC分类号： C07D207/08 ,  C07D405/04 ,  A61K31/4025 ,  A61P35/00

    CPC分类号： C07B57/00

    摘要： The present invention relates to a process for the preparation of a key intermediate (as described herein) used in the synthesis of (+)- trans enantiomer of pyrrolidine substituted flavones, represented by the compounds of formula (1) or pharmaceutically acceptable salts thereof; which are inhibitors of cyclin dependant kinases (CDKs) and can be used in the treatment of proliferative disorders such as cancer. Formula (1) wherein R 1 has the meaning as indicated in the claims. The process of the present invention has advantages of higher yield and purity, lower reaction temperature, is consistent and involves the use of non toxic solvents. The process of the present invention allows efficient large-scale synthesis and purity of the product obtained is greater than 97 %.

    摘要翻译： 本发明涉及用于合成由式（1）化合物或其药学上可接受的盐表示的吡咯烷取代的黄酮的（+） - 反式对映异构体中使用的关键中间体（如本文所述）的方法。 其是细胞周期蛋白依赖性激酶（CDK）的抑制剂，并且可以用于治疗增殖性疾病如癌症。 式（1）其中R1具有如权利要求中所示的含义。 本发明的方法具有产率高，纯度高，反应温度低的优点，是一致的，涉及无毒溶剂的使用。 本发明的方法允许有效的大规模合成和获得的产物的纯度大于97％。