ISSN:
0006-3592
Keywords:
solid-phase synthesis
;
3,1-benzoxazine-4-ones
;
serine protease inhibitor
;
heterocyclic acylating agents
;
Chemistry
;
Biochemistry and Biotechnology
Source:
Wiley InterScience Backfile Collection 1832-2000
Topics:
Biology
,
Process Engineering, Biotechnology, Nutrition Technology
Notes:
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. © 1998 John Wiley & Sons, Inc. Biotechnol Bioeng (Comb Chem) 61:13-16, 1998.
Additional Material:
3 Ill.
Type of Medium:
Electronic Resource
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