[摘要]:Novel racemic and enantiomerically enriched unsatd. tryprostatin B analogs were synthesized by an enaminone-based strategy. The synthesis also features a novel copper(I)-catalyzed dipeptide formation. In addn., the enantiomeric purity of an enantiomerically enriched analog I was detd. by 1H NMR spectroscopy by use of our own chiral solvating agent.