Rational ligand design for the arylation of hindered primary amines guided by reaction progress kinetic analysis

Academic Article
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publication date

  • 2015

abstract

  • 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.