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    Preparation of leurosidine and novel leurosidine 4'-ethers and esters
    4.
    发明授权
    Preparation of leurosidine and novel leurosidine 4'-ethers and esters 失效
    制备leurosidine和新型leurosidine 4 {40-醚和酯

    公开(公告)号：US4075214A

    公开(公告)日：1978-02-21

    申请号：US687274

    申请日：1976-05-17

    申请人： Allen S. Katner ,  Gerald E. Gutowski ,  Jean C. Miller

    发明人： Allen S. Katner ,  Gerald E. Gutowski ,  Jean C. Miller

    IPC分类号： C07D519/04 ,  C07D471/18

    CPC分类号： C07D519/04

    摘要： Vincaleukoblastine (VLB, vinblastine) is converted to leurosidine, its 4' epimer, by reaction with thionyl chloride to form a bis-sulfite ester followed by treatment of the bis-sulfite ester with silver perchlorate. The bis-sulfite ester is covertible to novel 4' ethers by treatment with a lower alkanol or 4' esters of leurosidine perchlorate with acetic anhydride.

    摘要翻译： 通过与亚硫酰氯反应将成纤维细胞生长素（VLB，长春花碱）转化为左啡肽，其4'差向异构体，形成双亚硫酸酯，随后用高氯酸银处理双亚硫酸酯。 双亚硫酸酯可以通过用低级链烷醇或用乙酸酐的高氯酸列萘硫代酯的4'酯处理来形成新的4'醚。

    Acylation of pyrazofurin
    9.
    发明授权
    Acylation of pyrazofurin 失效
    吡哆醛的酰化

    公开(公告)号：US4053698A

    公开(公告)日：1977-10-11

    申请号：US660208

    申请日：1976-02-23

    申请人： Gerald E. Gutowski

    发明人： Gerald E. Gutowski

    IPC分类号： C07D407/04 ,  C07D231/38 ,  C07D231/40 ,  C07H7/06 ,  C07H13/02

    CPC分类号： C07D407/04

    摘要： A process for preparing new compounds which are N- and O-acylates of pyrazofurin comprises first selective mono-N-acylation under non-basic conditions in an organic solvent. The mono-N-acylate so formed is further acylated under mild basic conditions to provide a tetra-acylated or penta-acylated pyrazofurin derivative, depending upon the duration of reaction. Mild solvolysis of either a tetra-acylate or a penta-acylate provides a tri-acylated pyrazofurin derivative. In the presence of a strong base, the mono-N-acylate is further acylated to provide different tetra-acylates or penta-acylates of pyrazofurin, again depending upon the duration of reaction. Pyrazofurin acylates are useful as antiviral, antipsoriatic, and antifungal agents, as well as intermediates for new C-nucleosides.

    Acylated derivatives of pyrazofurin and process for their preparation
    10.
    发明授权
    Acylated derivatives of pyrazofurin and process for their preparation 失效
    吡呋喃的酰化衍生物及其制备方法

    公开(公告)号：US3960836A

    公开(公告)日：1976-06-01

    申请号：US490627

    申请日：1974-07-22

    申请人： Gerald E. Gutowski

    发明人： Gerald E. Gutowski

    IPC分类号： C07D405/04 ,  C07D407/04 ,  C07H7/06

    CPC分类号： C07D407/04

    摘要： A process for preparing new compounds which are N- and O-acylates of pyrazofurin comprises first selective mono-N-acylation under non-basic conditions in an organic solvent. The mono-N-acylate so formed is further acylated under mild basic conditions to provide a tetra-acylated or penta-acylated pyrazofurin derivative, depending upon the duration of reaction. Mild solvolysis of either a tetra-acylate or a penta-acylate provides a tri-acylated pyrazofurin derivative. In the presence of a strong base, the mono-N-acylate is further acylated to provide different tetra-acylates or penta-acylates of pyrazofurin, again depending upon the duration of reaction. Pyrazofurin acylates are useful as antiviral, antipsoriatic, and antifungal agents, as well as intermediates for new C-nucleosides.

    摘要翻译： 制备吡唑啉的N-和O-酰化物的新化合物的方法包括在非碱性条件下在有机溶剂中的第一选择性单-N-酰化反应。 如此形成的单-N-酰化物在温和的碱性条件下进一步酰化，以提供四酰化或五酰基化的吡呋烯衍生物，这取决于反应的持续时间。 四酰基化物或五酰基化物的轻度溶剂分解提供三酰化的吡呋烯衍生物。 在强碱存在下，再次依赖于反应的持续时间，将单-N-酰化物进一步酰化以提供不同的吡咯呋喃的四酰化物或五酰基化物。 吡佐灵素酰化物可用作抗病毒，抗牛皮癣和抗真菌剂，以及新的C-核苷的中间体。