abstract |
PURPOSE: To produce a new benzopyran derivative having potassium channel activating function, which is useful as cardiovascular medicines such as antiarrythmic drug and drug for ischemic heart disease. n CONSTITUTION: Formula I (A is CH 2 , O, NR 9 , S, SO, SO 2 ; R 9 is H, 1-4C alkyl; X is O, S; Y is NR 8 , O, S, formula II; R 1 is aryl, arylalkyl, heterocyclic group, (heterocyclic) alkyl; R 2 is H, OH, formula III; R 10 is H, OH, alkyl, etc.; R 3 -R 8 are each H, alkyl, arylalkyl, CR 3 R 4 is 5-7 membered carbocyclic group; R 1 and R 7 , R 1 and R 8 , or R 7 and R 8 are 5-7 membered unsaturated or saturated ring, and R 5 is CN, NO 2 , etc.) shows the compound, e.g. (trans)-1-(6-cyano-3,4- dihydro-3-hydroxy-2,2-dimethyl-2H-1-benzopyran-4-yl)-3-phenyl urea. This compound, in which A=X=O and Y=NR 8 , is obtained by treating the compound of formula IV with chloroformic acid-4-nytrophenyl and then by allowing the reaction product of formula V to react with the compound of formula VI in an organic solvent. n COPYRIGHT: (C)1992,JPO |