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CuI-Catalyzed Coupling Reaction of β-Amino Acids or Esters with Aryl Halides at Temperature Lower Than That Employed in the Normal Ullmann Reaction. Facile Synthesis of SB-214857

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journal contribution
posted on 14.07.2001, 00:00 by Dawei Ma, Chengfeng Xia
The CuI-catalyzed coupling reaction of aryl halides with β-amino acids or β-amino esters is completed at 100 °C in 48 h, which indicates that the structure of the β-amino acid has an accelerating effect for the Ullmann-type aryl amination reaction. This coupling reaction can be used to prepare enantiopure N-aryl β-amino acids. An efficient synthetic route to SB214857, a potent GPIIb/IIIa receptor antagonist, is developed using this method.