BICYCLO (3.1.0) HEXYL-SUBSTITUTED CARBONYLAMINOPHENOXY CARDIOVASCULAR

摘要

l-Alkylamino-3-(4-(endobicyclo3.1.0!hex-6-yl)alkyl-ureido)-phenoxy)-2- propanol and substituted derivatives thereof; alkylamino-3-(4-(endobicyclo(3.1.0! hex6-yl)-alkylcarbonylamino!-l-phenoxy)-2-propanol and substituted derivatives thereof; as well as methods for preparing such compounds are disclosed. 5-(4(Endobi-cyclo(3.1.0!hex-6-yl)alkylureido!-l-phenoxy)methyl-3-alkyl -2-optionally substituted oxazolidine and derivatives thereof; 5-(4-(endobicyclo3.l.0!hex-6-yl)alkyl-carbonylamino!-1-phenoxy)methyl- 3-alkyl-2-optionally substituted oxazolidine and derivatives thereof; and methods for preparing these compounds are also disclosed. These compounds exhibit cardiovascular activity and are useful in the treatment of abnormal heart conditions as well as hypertension in mammals. The bicyclo2-propanols are prepared by treatment of the corresponding 1,2-epoxy-3-(4-{(endobicyclo3.1.0!hex-6-yl) alkylureido-, or alkylcarbonylamino-1-phenoxypropane, with the desired alkylamine or by base or acid hydrolysis of the corresponding 5-(4-(endobicyclo3.1.0!-hex-6-yl)-alkylureido-, or alkylcarbonylamino!-1-phenoxy) methyloxazolidines. The latter compounds are prepared from the corresponding 1-alkylamino-3-(4-(endobicyclo-3.1.0!hex-6-yl)alkylureido-, or alkylcarbonylamino!-1-phenoxy)-2-propanol by treatment with an optionally substituted aldehyde.