Polymer-assisted solution-phase (PASP) library synthesis of α-ketoamides

A parallel solution‐phase library synthesis of α‐ketoamides is described. The two‐step library synthesis is accomplished using polymer‐assisted solution‐phase (PASP) synthesis techniques. This high‐yielding, multi‐step sequence utilizes sequestering resins for the removal of reactants, reactant by‐products, and tagged reagents. The first step of the library synthesis utilizes PASP resins to mediate the amide coupling of an α‐hydroxy acid with an amine. The second step uses PASP resins for the periodinane oxidation of the α‐hydroxy acid to an α‐ketoamide leaving highly pure products after simple filtration and evaporation. © 2000 John Wiley & Sons, Inc. Biotechnol Bioeng (Comb Chem) 71:51–57, 2000.