Highly Efficient Enantiospecific Synthesis of Imidazoline-Containing Amino Acids Using Bis(triphenyl)oxodiphosphonium Trifluoromethanesulfonate

A highly efficient enantiospecific synthesis of imidazoline-based amino acids is reported from dipeptides composed of a C-terminal beta-amino-alpha-amino acid residue using bis(triphenyl) oxodiphosphonium trifluoromethanesulfonate. These imidazolines were easily converted to imidazoles and incorporated into macrolactam analogues of bistratamide H without loss of stereochemical integrity.