Title:
【発明の名称】α-ヒドロキシ-β-アミノ酸およびアミド誘導体の合成のための方法
Document Type and Number:
Japanese Patent JP2002532466
Kind Code:
A
Abstract:
Methods for the synthesis of alpha-hydroxy-beta-amino acid and amide derivatives and alpha-ketoamide derivatives and novel derivatives made by these methods are provided. These methods involve reacting a N-terminally blocked (protected) aminoaldehyde with an isonitrile and a carboxylic acid to give an amino-alpha-acyloxy carboxamide. The acyloxy group may be removed to give the derivative. Alternatively the protecting group is removed and acyl shift occurs to give the derivative. These derivatives are useful in the synthesis of compounds such as peptidyl alpha-ketoamides and alpha-hydroxy-beta-carboxylic acid and amide derivatives. Certain of these compounds have been reported to have activity as inhibitors of proteases, such as serine proteases and cysteine proteases.
Inventors:
Semple, Joseph E.
Levy, O'Dill E.
Levy, O'Dill E.
Application Number:
JP2000588130A
Publication Date:
October 02, 2002
Filing Date:
December 16, 1999
Export Citation:
Assignee:
Corbus International, Incorporated
International Classes:
C07C231/00; C07C237/06; C07C277/08; C07C279/36; C07C281/10; C07C231/12; (IPC1-7): C07C231/12; C07C237/06; C07C277/08; C07C279/36; C07C281/10
Attorney, Agent or Firm:
Shusaku Yamamoto