PROCESS FOR THE PREPARATION OF TRAVOPROST
    8.
    发明公开
    PROCESS FOR THE PREPARATION OF TRAVOPROST 审中-公开
    VERFAHREN ZUR HERSTELLUNG VON TRAVOPROST

    公开(公告)号:EP2925720A1

    公开(公告)日:2015-10-07

    申请号:EP13811611.6

    申请日:2013-11-26

    IPC分类号: C07C405/00

    摘要: The subject of the invention is process the preparation of travoprost of formula (I) characterized by that the free acid of formula (II) is a.) activated with 2-chloro-1,3-dimethyl-imidazolinium chloride (DMC) and the resulting activated carboxylic acid intermediate is reacted with isopropyl alcohol, or b.) reacted with alkyl haloformate and the resulting mixed anhydride is reacted with isopropyl alcohol, or c.) activated with a straight or branched C1-8 dialkyl dicarbonate and reacted with isopropanol in the presence of water-free magnesium salt.

    摘要翻译: 本发明的主题是制备式(I)的曲伏前列素,其特征在于式(II)的游离酸是用2-氯-1,3-二甲基 - 咪唑啉氯化物(DMC)活化的, 使活化的羧酸中间体与异丙醇反应,或b。)与卤代甲酸烷基酯反应,并将得到的混合酸酐与异丙醇反应,或c。用直链或支链C 1-8二烷基二碳酸酯活化并与异丙醇反应 存在无水镁盐。

    Processes for the preparation of isomer free prostaglandins
    9.
    发明公开
    Processes for the preparation of isomer free prostaglandins 审中-公开
    前列腺素(Verfahren zur Herstellung Isomeren-freier Prostaglandine)

    公开(公告)号:EP2837621A1

    公开(公告)日:2015-02-18

    申请号:EP14180866.7

    申请日:2014-08-13

    IPC分类号: C07C405/00 C07D313/00

    摘要: Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6- trans isomer:

    wherein

    R 2 , R 3 and R 4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer free Prostaglandins and derivatives thereof are also provided.

    摘要翻译: 制备基本上不含5,6-反式异构体的式I-2化合物的新方法:其中R 2,R 3和R 4如说明书中所定义。 还提供了用于制备不含异构体的前列腺素及其衍生物的新型中间体。