| abstract |
The invention provides intermediates from which α-keto amide compounds having protease inhibiting activity can be prepared extremely economically and stereoselectively. Specifically, epoxycarboxylic acid amides, azides and amino alcohols represented by the general formulae (I), (VI) and (IX) respectively, and processes for preparing α-keto amide compounds by using the amides, the azides or the alcohols are provided wherein R?1 and R2¿ are each alkyl, alkenyl, an aromatic hydrocarbon group, or a heterocyclic group; R3 is alkyl, alkenyl, an aromatic hydrocarbon group, a heterocyclic group, R6-O-, or R7-N(R8)- (wherein R6 is alkyl, alkenyl, an aromatic hydrocarbon group, or a heterocyclic group; and R?7 and R8¿ are each hydrogen, alkyl, alkenyl, an aromatic hydrocarbon group, or a heterocyclic group); R?4 and R5¿ are each a group selected from among those defined above for R?7 and R8¿, or alternatively R?4 and R5¿ together with the carbon atom to which they are bonded may form a ring; and X is O- or N(R9)- (wherein R9 is hydrogen or alkyl, or R9 may unite with R4 or R5 to form a ring). |