POLYMORPHS OF DARUNAVIR
    14.
    发明申请
    POLYMORPHS OF DARUNAVIR 有权
    DARUNAVIR的POLYMORPHS

    公开(公告)号:US20140200356A1

    公开(公告)日:2014-07-17

    申请号:US14047243

    申请日:2013-10-07

    IPC分类号: C07D493/04

    摘要: The present invention provides novel solvated forms of darunavir and processes for their preparation. The present invention also provides novel processes for the preparation of darunavir amorphous form and pharmaceutical compositions comprising it. Thus, for example, darunavir 2-methyl-2-butanol solvate was dissolved in methylene dichloride, distilled under vacuum at 45° C. to obtain a residue, cyclohexane was added to the residue and stirred for 30 hours at 20 to 25° C., and the separated solid was filtered, washed with cyclohexane and dried under vacuum at 50° C. for 12 hours to yield darunavir amorphous form.

    摘要翻译: 本发明提供了地瑞那韦的新型溶剂化形式及其制备方法。 本发明还提供了制备地瑞那韦非晶形式的新方法和包含它的药物组合物。 因此,例如,将地瑞那韦2-甲基-2-丁醇溶剂合物溶解在二氯甲烷中,在45℃下真空蒸馏,得到残留物,将环己烷加入残留物中,在20〜25℃下搅拌30小时 将分离出的固体过滤,用环己烷洗涤,在50℃下真空干燥12小时,得到地瑞那韦非晶形式。