Preparation of Amides of Retinoic Acid Via Mixed Anhydride and Mixed Carbonate Intermediates
    9.
    发明申请
    Preparation of Amides of Retinoic Acid Via Mixed Anhydride and Mixed Carbonate Intermediates 审中-公开
    通过混合酸酐和混合碳酸酯中间体制备视黄酸酰胺

    公开(公告)号:US20080221349A1

    公开(公告)日:2008-09-11

    申请号:US11968252

    申请日:2008-01-02

    IPC分类号: C07C69/618

    摘要: Processes for preparing amides of retinoic acid are disclosed. Intermediates useful in the preparation of amides of retinoic acid are also disclosed. In one version of the invention, fenretinide is produced via activation of retinoic acid (tretinoin) via its corresponding mixed anhydride or mixed carbonate followed by reaction of the activated intermediate with 4-aminophenol. Other amides of retinoic acid and isomers of retinoic acid, such as the 9-cis-form or 13-cis-form can also be made by this invention.

    摘要翻译: 公开了制备视黄酸酰胺的方法。 还公开了可用于制备视黄酸酰胺的中间体。 在本发明的一个方案中,通过其相应的混合酸酐或混合碳酸酯活化视黄酸(维A酸),然后将活化的中间体与4-氨基苯酚反应,产生芬维A胺。 视黄酸的其它酰胺和视黄酸的异构体如9-顺式或13-顺式也可以通过本发明制备。