PURPOSE: To obtain aryl and heterocyclic substituted propenamide derivs. useful for the treatment of ischemic conditions and arrhythmia and having potassium channel-activating action.
CONSTITUTION: The aryl and heterocyclic substituted propenamide derivs. are compds. of formula I (where X is O or SiR1; R1 is aryl or heterocyclic; R2 is H, hydroxyl or the like; R3 and R4 are each H, alkyl, arylalkyl or carbocyclic; R5 is H, alkyl, alkenyl or the like; R6-R4 are each H, alkyl or the like; and Y is a single bond, -O-, -S- or the like), e.g. [3S-[3α,4β(Z)]]-N-(6-cyano-3,4- dihydro-3-hydroxy-2,2-dimethyl-2H-1-benzopyran-4-yl)-3-phenyl-2-propenamide. The compds. of the formula I are obtd. by reacting compds. of formula II with amines of formula III in a solvent such as THF. The compds. of the formula I are also useful for the treatment of other cardiovascular disturbances such as congestive heart failure and myocardial infarction and central nervous system injuries such as Parkinsonism and epilepsy.
SHIETSUDO ZETSUTO AAMETSUDO
DEINOSU PII SANTAFUIANOSU