To provide a new α-ketoamide derivative composed of a non-peptide α-ketoamide derivative, having excellent chymase inhibiting action and useful as an agent for the prevention and treatment of cardiovascular diseases, etc., of warm-blooded animals.
The objective compound is expressed by formula I [A is a substituted lower alkyl, a lower alkoxy or an aromatic ring; R1 and R2 are each H, a (substituted)alkyl or the like], e.g. N-[2,5-bis(N-benzylcarbamoyl) phenyl]-2-oxo-3-phenylpropanamide. The compound of formula I can be produced by reacting an α-keto-acid halide derivative of formula A-COCO-X (X is a halogen) with an aniline derivative of formula II preferably in a reaction solvent (e.g. tetrahydrofuran) in the presence of an organic base (e.g. 4- dimethylaminopyridine). The amount of the organic base is preferably 0.05-1.0 mol based on 1 mol of the aniline derivative and the reaction temperature is preferably 0-30°C.
SAKAI YUSUKE
INOUE ATSUSHI
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