Ruthenium-Catalyzed N-Alkylation of Amines and Sulfonamides Using Borrowing Hydrogen Methodology
Ruthenium-Catalyzed N-Alkylation of Amines and Sulfonamides Using Borrowing Hydrogen Methodology
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DOI：
10.1021/ja807323a
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发表时间：
2009-02-11
影响因子：
15
通讯作者：
Williams, Jonathan M. J.
中科院分区：
文献类型：
--
作者：
Hamid, M. Haniti S. A.;Allen, C. Liana;Williams, Jonathan M. J.
用0.5mol%[Ru（p-cymene）Cl-2]（2）与双齿膦dppf或DPEphos作催化剂，实现了胺与醇的烷基化反应。伯胺被转化为仲胺，仲胺被转化为叔胺，包括吡贝地尔、曲吡那明和氯苯那敏的合成。报道了伯胺的N-杂环化反应，以及伯磺酰胺的烷基化反应。仲醇比伯醇需要更多的强制条件，但在该催化剂存在下仍然是有效的烷基化剂。
The alkylation of amines by alcohols has been achieved using 0.5 mol % [Ru(p-cymene)Cl-2](2) with the bidentate phosphines dppf or DPEphos as the catalyst. Primary amines have been converted into secondary amines, and secondary amines into tertiary amines, including the syntheses of Piribedil, Tripelennamine, and Chlorpheniramine. N-Heterocyclization reactions of primary amines are reported, as well as alkylation reactions of primary sulfonamides. Secondary alcohols require more forcing conditions than primary alcohols but are still effective alkylating agents in the presence of this catalyst.