| 摘要 |
PROBLEM TO BE SOLVED: To provide a method for obtaining trandolapril by simple reaction operation in relation to two steps just before the final in a long process for producing the trandolapril starting from a commercially available raw material compound. SOLUTION: The method for producing the trandolapril is carried out as follows. A salt of benzyl (2S,3aR,7aS)-hexahydro-2-indolinecarboxylate with an optically active 10-camphor-sulfonic acid is reacted with N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanyl N-carboxy anhydride or N-[1(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine in a solvent containing a tertiary amine to provide benzyl (2S,3aR,7aS)-1-[(S)-N-[(S)-1-ethoxycarbonyl-3-phenylpropyl]alanyl]hexahydro-2-indolinecarboxylate. The resultant ester is then reduced with hydrogen. COPYRIGHT: (C)2005,JPO&NCIPI
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