title: Combinatorial approaches to harmacophoric heterocycles: A solid-phase synthesis of 3,1-benzoxazine-4-ones
abstract: An efficient solid-phase synthesis of 3,1-benzoxazine-4-ones is described. Immobilized amino acid based functionalized urea derivatives 2 undergo a high yielding heterocyclization under mild conditions in presence of coupling reagents (DIC, TsCl/Py, or Ac2O) to afford 3,1-benzoxazine-4-ones 6. The method offers broad scope for structural and chemical diversity, and is amenable for combinatorial synthesis of 3,1-benzoxazine-4-ones libraries with potential for discovery of novel serine protease inhibitors. Copyright 1998 John Wiley & Sons, Inc.
authors: Versicor, Inc., Ardenwood Business Park, 34790 Ardentech Court, Fremont, California 94555, USA.
authors: MF
authors: Gordeev