| abstract |
NEW MATERIAL:A carbostyril derivative of formula I (R 1 is H or lower alkyl; R 2 is halogen-substituted lower alkanoyl or halogen-substituted lower alkyl; the bond between the 3- and the 4-carbon atoms in the carbostyril skeleton is single or double bond.) and its salt. n EXAMPLE: 6-(β-Chloropropionylamino)carbostyril. n USE: A phosphodiesterase inhibitor, a blood platelet coagulation inhibiting agent, (antithrombic agent), antibacterial agent, and intermediaters of central nervous system depressants (some of which are novel) and antihistaminic agents. n PROCESS: The compound of formula I is prepared by reacting a compound of formula II with a compound of formula R 2 ' -X 1 (X is halogen; R 2 ' is halogen-substituted lower alkyl) or formula R 2 "-OH(R 2 " is halogen-substotituted lower alkanoyl). A compound of formula III (A is CO; l is 0 or 1; Y is lower alkylene; X 2 is halogen) which is one of the compounds of formula I, can be converted to a novel compound of formula VI (R 3 is halogen, etc.; n is 0W3) useful as a central nervous system depressant, etc. n COPYRIGHT: (C)1981,JPO&Japio |