PROCESS FOR PREPARING CASPOFUNGIN AND NOVEL INTERMEDIATES THEREOF
    7.
    发明申请
    PROCESS FOR PREPARING CASPOFUNGIN AND NOVEL INTERMEDIATES THEREOF 有权
    制备CASPOFUNGIN及其新型中间体的方法

    公开(公告)号:US20130261286A1

    公开(公告)日:2013-10-03

    申请号:US13881204

    申请日:2011-01-12

    IPC分类号: C07K7/56

    CPC分类号: C07K7/56 C07D487/14

    摘要: The present invention relates to a novel process for preparing the aza cyclohexapeptide compound 1-[(4R,5S)-5-[(2-aminoethyl)amino]-N2-(10,12-dimethyl-1-oxotetradecyl)-4-hydroxy-L-ornithine]-5-[(3R)-3-hydroxy-L-ornithine]-pneumocandin B0 (caspofungin) represented by the following formula 1, which can improve the problem due to a pungent odor and toxicity during the process and can prepare caspofungin as a final product at high yield compared to conventional processes, and to novel intermediates which are used in the preparation process:

    摘要翻译: 本发明涉及一种制备氮杂环己肽化合物1 - [(4R,5S)-5 - [(2-氨基乙基)氨基] -N2-(10,12-二甲基-1-氧代十四烷基)-4- 羟基-L-鸟氨酸] -5 - [(3R)-3-羟基-L-鸟氨酸] - 肺炎球菌素B0(卡泊芬净),其可改善由于过程中刺激性气味和毒性引起的问题 并且与常规方法相比,可以以高产率制备卡泊芬净作为最终产物,以及用于制备过程中的新型中间体: