abstract |
PURPOSE: To provide the novel compd. which has an effect of increasing secretion of a CGMP, i.e., a specific marker for the secretion of sodium and ANP system activation and is useful for the treatment of a blood pressure, cardiac failure, renal failure, cirrhosis, lung edema, etc. n CONSTITUTION: The recemic bodies of formula I (R 1 is 1 to 6C alkyl which may be substd. with phenoxy, cyclohexyl, H, trifluoromethyl; R 2 is 1 to 4C alkyl which may be substd. with cyano, hydroxyl, etc.; R 3 is 1 to 5C alkyl, 3 to 5C cycloalkyl) and the compd. in the form of their optical antipodes. For example, the compd. of formula II. The compd. of the formula I is obtd. by bringing, for example, the aldehyde of formula III into reaction with the β- ketocarboxyalate of formula IV, β-ketocarboxyamide of formula V and ammonia preferably at 20 to 100°C in a solvent, such as water. n COPYRIGHT: (C)1992,JPO |