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

Authors
South, MS Dice, TA Parlow, JJ
Citation
Ms. South et al., Polymer-assisted solution-phase (PASP) library synthesis of alpha-ketoamides, BIOTECH BIO, 71(1), 2000, pp. 51-57
Citations number
58
Categorie Soggetti
Biotecnology & Applied Microbiology",Microbiology
Journal title
BIOTECHNOLOGY AND BIOENGINEERING
ISSN journal
00063592 → ACNP
Volume
71
Issue
1
Year of publication
2000
Pages
51 - 57
Database
ISI
SICI code
0006-3592(200024)71:1<51:PS(LSO>2.0.ZU;2-4
Abstract
A parallel solution-phase library synthesis of alpha-ketoamides is describe d. The two-step library synthesis is accomplished using polymer-assisted so lution-phase (PASP) synthesis techniques. This high-yielding, multi-step se quence utilizes sequestering resins for the removal of reactants, reactant by-products, and tagged reagents. The first step of the library synthesis u tilizes PASP resins to mediate the amide coupling of an alpha-hydroxy acid with an amine. The second step uses PASP resins for the periodinane oxidati on of the oi-hydroxy acid to an alpha-ketoamide leaving highly pure product s after simple filtration and evaporation. (C) 2000 John Wiley & Sons, Inc.