Process for the preparation of cyclo(Asp-DPhe-NMeVal-Arg-Gly)
    4.
    发明授权
    Process for the preparation of cyclo(Asp-DPhe-NMeVal-Arg-Gly) 失效
    制备环(Asp-DPhe-NMeVal-Arg-Gly)的方法

    公开(公告)号:US06822074B1

    公开(公告)日:2004-11-23

    申请号:US09936230

    申请日:2001-09-12

    IPC分类号: A61K3800

    摘要: Process for the preparation of the cyclic pentapeptide cyclo(Arg-Gly-Asp-DPhe-NMeVal) by cyclization of a linear pentapeptide selected from the group consisting of H-Arg(Pbf)-Gly-Asp(OBzl)-DPhe-NMeVal-OH, H-Gly-Asp(OBzl)-DPhe-NMeVal-Arg(Pbf)-OH, H-Asp(OBzl)-DPhe-NMeVal-Arg(Pbf)-Gly-OH, H-DPhe-NMeVal-Arg(Pbf)-Gly-Asp(OBzl)-OH or H-NMeVal-Arg(Pbf)-Gly-Asp (OBzl)-DPhe-OH, subsequent protective group removal and, if appropriate, further conversion into its physiologically acceptable salts.

    摘要翻译: 通过环化选自H-Arg(Pbf)-Gly-Asp(OBz1)-DPhe-NMeVal-OH,H-Arg(Pbf)-Gly-Asp(OBz1)-DPhe-NMeVal-OH)的线性五肽制备环状五肽环(Arg-Gly-Asp-DPhe-NMeVal) H-Gly-Asp(OBz1)-DPhe-NMeVal-Arg(Pbf)-OH,H-Asp(OBz1)-DPhe-NMeVal-Arg(Pbf)-Gly-OH,H-DPhe-NMeVal-Arg(Pbf) -Gly-Asp(OBzl)-OH或H-NMeVal-Arg(Pbf)-Gly-Asp(OBzl)-DPhe-OH,随后保护基团去除,并且如果合适,进一步转化成其生理上可接受的盐。