| 摘要 |
NEW MATERIAL:A 3-propionylsalicyclic acid derivative of formula I [R is H, lower alkyl or formula II (R<1> and R<2> are lower alkyl or R<1> and R<2> together with the nitrogen atom to which they are linked through or not through a hetero atom may form a heterocyclic ring; n is an integer 1-4); X is H or halogen, provided that R represents formula II when X is H atom]. EXAMPLE:Ethyl-5-chloro-3-propionylsalicylate. USE:Useful as a remedy for preventing the fit of angina pectoris and cardiac infraction, etc. and a remedy for increasing the discharge capacity of the urinary bladder, disappearance of subjective symptom of thamuria, etc. having coronary arterial vasodilator action and coronary blood stream increasing action, and further useful as a synthetic intermediate for compounds useful as a diuretic having the remissive action, e.g. smooth muscle spasm in the lower urinary tract. PROCESS:A compound of formula III (X' is halogen) is reacted with a propionyl halide by the Friedel-Crafts reaction to give the aimed compound of formula I . |
