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    Compounds and Methods for Catalytic Directed ortho Substitution of Aromatic Amides and Esters
    7.
    发明申请
    Compounds and Methods for Catalytic Directed ortho Substitution of Aromatic Amides and Esters 审中-公开
    用于催化定向邻位取代芳族酰胺和酯的化合物和方法

    公开(公告)号：US20150166500A1

    公开(公告)日：2015-06-18

    申请号：US14541297

    申请日：2014-11-14

    申请人： Queen's University at Kingston

    发明人： Yigang Zhao ,  Victor A. Snieckus

    IPC分类号： C07D307/68 ,  C07C63/36 ,  C07C233/65

    CPC分类号： C07D307/68 ,  C07C63/36 ,  C07C67/343 ,  C07C69/76 ,  C07C69/94 ,  C07C231/12 ,  C07C233/65 ,  C07C2601/02 ,  C07D209/42 ,  C07D213/81 ,  C07D241/24 ,  C07D307/81 ,  C07D333/38 ,  C07D409/04 ,  C07C235/66 ,  C07C237/48

    摘要： Methods are described for efficient and regioselective reactions that are Ru-catalyzed and either (i) amide-directed C—H, C—N, C—O activation/C—C bond forming reactions, (ii) ester-directed C—O and C—N activation/C—C bond forming reactions, or (iii) amide-directed C—O activation/hydrodemethoxylation reactions. All of these reactions of directed C—H, C—N, C—O activation/coupling reactions establish a catalytic base-free DoM-cross coupling process at non-cryogenic temperature. High regioselectivity, yields, operational simplicity, low cost, and convenient scale-up make these reactions suitable for industrial applications. Many previously unknown amide-substituted or ester-substituted aryl and heteroaryl compounds are presented with synthetic details also provided.

    摘要翻译： 描述了Ru催化的有效和区域选择性反应的方法，和（i）酰胺指导的C-H，C-N，C-O活化/ C-C键形成反应，（ii）酯指导的C-O 和C-N活化/ C-C键形成反应，或（iii）酰胺指导的C-O活化/加氢脱甲氧基化反应。 所有这些直接C-H，C-N，C-O活化/偶联反应的反应在非低温温度下建立了催化无碱的DoM交叉偶联过程。 高的区域选择性，产率，操作简单性，低成本和方便的放大使这些反应适用于工业应用。 许多以前未知的酰胺取代或酯取代的芳基和杂芳基化合物也提供了合成细节。