Rh(I)-catalyzed alkylation of quinolines and pyridines via C-H bond activation
Rh(I)-catalyzed alkylation of quinolines and pyridines via C-H bond activation
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DOI：
10.1021/ja070388z
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发表时间：
2007-05-02
影响因子：
15
通讯作者：
Ellman, Jonathan A.
中科院分区：
文献类型：
--
作者：
Lewis, Jared C.;Bergman, Robert G.;Ellman, Jonathan A.
杂环邻位烷基化的范围已经大大扩大，包括药用上重要的吡啶和喹啉，它们只含有一个氮。这些反应在高浓度(0.8M)下进行，催化剂负载量低至1%Rh。杂环氮的邻位取代是有效的烷基化反应所必需的，并且与类似于我们早期工作中提出的Rh-卡宾中间体的中间体是一致的。
The scope of heterocycle ortho-alkylation has been dramatically expanded to include pharmaceutically important pyridines and quinolines, which contain only a single nitrogen. The reactions, which are conducted at a high concentration (0.8 M), can be performed with catalyst loadings as low as 1% Rh. Substitution ortho to the heterocycle ring nitrogen is required for efficient alkylation and is consistent with the intermediacy of a Rh-carbene intermediate similar to those proposed in our earlier work.