Cul-catalyzed coupling reaction of beta-amino acids or esters with aryl halides at temperature lower than that employed in the normal Ullmann reaction. Facile synthesis of SB-214857

[GRAPHICS] The Cul-catalyzed coupling reaction of aryl halides with beta -amino acids or beta -amino esters is completed at 100 degreesC in 48 h, which indicates that the structure of the,beta -amino acid has an accelerating effect for the Ullmann-type aryl amination reaction. This coupling reaction can be use d to prepare enantiopure N-aryl beta -amino acids. An efficient synthetic r oute to SB214857, a potent GPIIb/IIIa receptor antagonist, is developed usi ng this method.