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    Process for the synthesis of 4,5,6,7-tetrachloro-3′,6′-dihydroxy-2′,4′,5′,7′-tetraiodo-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (rose bengal) and related xanthenes
    4.
    发明授权
    Process for the synthesis of 4,5,6,7-tetrachloro-3′,6′-dihydroxy-2′,4′,5′,7′-tetraiodo-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (rose bengal) and related xanthenes 有权
    合成4,5,6,7-四氯-3'，6'-二羟基-2'，4'，5'，7'-四碘-3H-螺[异苯并呋喃-1,9'-呫吨] -3-one（玫瑰红）和相关的呫吨

    公开(公告)号：US08530675B2

    公开(公告)日：2013-09-10

    申请号：US12884833

    申请日：2010-09-17

    申请人： Jamie Singer ,  Eric A. Wachter ,  Timothy Scott ,  Marlon Lutz ,  Kevin Babiak

    发明人： Jamie Singer ,  Eric A. Wachter ,  Timothy Scott ,  Marlon Lutz ,  Kevin Babiak

    IPC分类号： C07D311/82

    CPC分类号： C07D311/82 ,  C07D493/10

    摘要： A new process for the manufacture of iodinated xanthenes in high purity includes a cyclization step followed by an iodination step. No extraction, chromatographic or solvent concentration steps are required, and the intermediate as well as final compounds are isolated via filtration or similar means. The process requires a single organic solvent, and the steps are completed at temperatures below 100° C. The exclusion of chloride ions, of chloride free-radicals, hypochlorite ions, or hypochlorous acid as reagents or from reagents that may generate these species in situ in the presence of oxidants, prevents undesirable impurity formation. Several new compounds have been conceived and isolated using these methods. These new compounds are also formed into new medicaments.

    摘要翻译： 用于制造高纯度碘化呫吨的新方法包括环化步骤，然后进行碘化步骤。 不需要提取，色谱或溶剂浓缩步骤，通过过滤或类似方法分离中间体和最终化合物。 该过程需要单一的有机溶剂，并且步骤在低于100℃的温度下完成。排除氯离子，氯化物自由基，次氯酸根离子或次氯酸作为试剂或从原位产生这些物质的试剂 在存在氧化剂的情况下，可防止不希望有的杂质形成。 已经使用这些方法构思和分离了几种新化合物。 这些新化合物也形成新的药物。