Abstract In this work we present new, fully synthetic phenylglycine-derived primary amine organocatalysts useful for the one-step preparation of optically active warfarin, an important anticoagulant. Both enantiomeric forms of the catalysts are equally available and can be prepared by robust procedures without recourse to chromatographic purification. Together with a co-catalyst, particularly acetic acid or 2, 4-dinitrophenol, they can furnish warfarin in ...