CARBOSTYRIL DERIVATIVE

摘要

NEW MATERIAL:A carbostyril derivative of formula I (R<1> is H or phenyl; R<2> is H, phenyl or lower alkyl; R<3> is lower alkyl, lower alkoxy, halogen or cyano; A is lower alkylene; n is 0-3; the bond between the 3-and the 4-carbon atoms of the carbostyril skeleton is single or double bond) and its salt. EXAMPLE:3-Phenyl-1-[ 3-( 4-phenyl-1-piperazinyl )propyl ]-3, 4-dihydrocarbostyril. 1-oxalate. USE:Antihistaminic agent for the remedy and prophylaxis of allergosis of respiratory tracts such as sneeze, snivels, etc. and acute uriticaria, etc. Also useful as a central nervous system depressant such as central muscle relaxant, preoperative medicine, etc. It is low toxic and has no side effects. PROCESS:The compound of formula I is prepared, e.g. by reacting a compound of formula V with a compound of formula IV obtained by reacting a compound of formula II with compound of formual III in an inert solent in the presence of a dehydro-halogenating agent.