Ruiz-Castillo Paula, Blackmond Donna G, Buchwald Stephen L
Department of Chemistry, Massachusetts Institute of Technology , Cambridge, Massachusetts 02139, United States.
J Am Chem Soc. 2015 Mar 4;137(8):3085-92. doi: 10.1021/ja512903g. Epub 2015 Feb 18.
We report the Pd-catalyzed arylation of very hindered α,α,α-trisubstituted primary amines. Kinetics-based mechanistic analysis and rational design have led to the development of two biarylphosphine ligands that allow the transformation to proceed with excellent efficiency. The process was effective in coupling a wide range of functionalized aryl and heteroaryl halides under mild conditions.
我们报道了钯催化的位阻极大的α,α,α-三取代伯胺的芳基化反应。基于动力学的机理分析和合理设计促成了两种联芳基膦配体的开发，这些配体可使转化反应高效进行。该过程能够在温和条件下有效地偶联多种官能化芳基卤化物和杂芳基卤化物。
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