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39 条记录 (耗时 0.035 秒)

    Preparation of 5-deazariboflavins
    13.
    发明授权
    Preparation of 5-deazariboflavins 失效
    5-deazariboflavins的制备

    公开(公告)号：US4277603A

    公开(公告)日：1981-07-07

    申请号：US19986

    申请日：1979-03-12

    申请人： Richard L. Tolman ,  Wallace T. Ashton ,  Ronald D. Brown

    发明人： Richard L. Tolman ,  Wallace T. Ashton ,  Ronald D. Brown

    IPC分类号： C07D239/54 ,  C07D239/545 ,  C07D471/04 ,  C07H15/18

    CPC分类号： C07D239/545 ,  C07D471/04 ,  C07H15/18

    摘要： This invention relates generally to a novel process for preparing 5-deazariboflavins by the cyclization of the corresponding 6-(N-substituted arylamino)uracils with trialkylorthoformate in the presence of a strong acid catalyst. An improved process for preparing the uracil intermediate is also disclosed. More particularly, it is concerned with the process for preparing 5-deazariboflavin by cyclizing 6-[3,4-dimethyl-N-(D-ribityl)anilino[uracil with trialkylorthoformate in the presence of a strong acid catalyst and hydrolyzing the resulting alkoxymethylene derivative. The corresponding uracil intermediate is prepared by reacting 6-chlorouracil with N-D-ribityl-3,4-xylidine.5-Deazariboflavins having the general Formula (I) herein below: ##STR1## wherein R.sub.7 is hydrogen or methyl, R.sub.8 is methyl, hydroxy or acyloxy and R.sub.10 is a ribityl group and the corresponding acyl and alkoxymethylene derivatives are useful as riboflavin antagonists with particular utility for the chemotherapy of coccidiosis in chickens or as intermediates for the preparation of said antagonists. The bis(alkoxymethylene) derivatives described herein are useful as prodrug forms of 5-deazariboflavins.When used for the treatment of coccidiosis, such compounds are administered to the animals by way of the feed and are effective in preventing coccidiosis when administered at levels of from about 0.0005% to about 0.05% by weight of the total feed consumed, the amount required for optimum prevention or control of the disease varying with the particular compound employed.

    摘要翻译： 本发明一般涉及在强酸催化剂存在下，通过使相应的6-（N-取代的芳基氨基）尿嘧啶与三烷基原甲酸酯环化制备5-脱氮黄素的新方法。 还公开了一种制备尿嘧啶中间体的改进方法。 更具体地说，它涉及通过在强酸催化剂存在下使6- [3,4-二甲基-N-（D-核糖基）苯胺基[尿嘧啶与三烷基原甲酸酯]环化来制备5-脱氮黄素的方法，并水解得到的烷氧基亚甲基 衍生物。 通过6-氯尿嘧啶与N-D-核糖基-3,4-二甲苯胺反应制备相应的尿嘧啶中间体。 具有下述通式（I）的5-脱氮维生素：其中R 7是氢或甲基，R 8是甲基，羟基或酰氧基，R 10是ribityl基团，并且相应的酰基和烷氧基亚甲基衍生物可用作特定的核黄素拮抗剂 用于鸡的球虫病化疗或用作制备所述拮抗剂的中间体的效用。 本文所述的双（烷氧基亚甲基）衍生物可用作5-脱氮白蛋白的前药形式。 当用于治疗球虫病时，通过饲料将这些化合物施用于动物，并且当以所消耗的总饲料的约0.0005重量％至约0.05重量％的水平施用量时，有效地预防球虫病，所需量 用于最佳预防或控制随所用特定化合物变化的疾病。

    Antifungal 1-substituted benzimidazoles
    19.
    发明授权
    Antifungal 1-substituted benzimidazoles 失效
    抗真菌剂1-取代苯并咪唑

    公开(公告)号：US4017503A

    公开(公告)日：1977-04-12

    申请号：US586438

    申请日：1975-06-12

    申请人： Wallace T. Ashton ,  Edward F. Rogers

    发明人： Wallace T. Ashton ,  Edward F. Rogers

    IPC分类号： C07D417/04 ,  A01N20060101 ,  A01N47/16 ,  A61K31/425 ,  C07C68/02 ,  C07D20060101 ,  C07D277/20 ,  C07D417/00

    CPC分类号： C07C68/02

    摘要： New benzimidazoles substituted at the 1-position with carbonyl substituents and at the 2-position with a 4-thiazolyl group are effective fungicides and anthelmintics exhibiting particularly useful hydrophilic and lypophilic effects. The compounds as well as processes for their preparation are described along with antifungal and anthelmintic compositions for their use. The 1-position substituent is a loweralkoxy or phenylloweralkoxy substituted ethoxy or polyethoxy carbonyl group of a chain with up to 4 ethoxy groups connected to the carbonyl. The compounds are generally prepared by contacting a 1-unsubstituted benzimidazole with a loweralkoxy or phenylloweralkoxy substituted ethoxy or polyethoxy chloroformate.

    摘要翻译： 在1-位被羰基取代基取代的2-苯并咪唑和2-噻唑基的2-位是有效的杀真菌剂和驱虫剂，其表现出特别有用的亲水性和溶血性作用。 该化合物及其制备方法与抗真菌和驱虫剂组合物一起使用。 1-位取代基是具有与羰基连接的多达4个乙氧基的链的低级烷氧基或苯基低级烷氧基取代的乙氧基或聚乙氧基羰基。 通常通过使1-未取代的苯并咪唑与低级烷氧基或苯基低级烷氧基取代的乙氧基或聚乙氧基氯甲酸酯接触来制备化合物。