still for framstellning of new isoindolinderivat

摘要

1498348 Naphthyridine derivatives RHONEPOULENC SA 17 Sept 1976 [22 Sept 1975] 38671/76 Addition to 1417935 Heading C2C Novel compounds II in which Y is H, halogen, C 1-4 alkyl, C 1-4 alkoxy, CN or NO 2 and R is H, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, C 1-4 hydroxyalkyl or phenyl, and acid addition salts thereof, are prepared by (a) reacting a compound IV with a 1-R-2-chlorocarbonyl-piperazine, or (b) reacting a mixed carbonate of a compound IV with a 1-R-piperazine. Compounds IV are prepared by partial reduction of corresponding imides which are themselves prepared by reacting a trifluoromethyl-substituted anhydride with a 2-amino- 7-Y-naphthyridine. 4 - Trifluoromethyl - phthalic anhydride is prepared by converting 2-amino-4-trifluoromethylbenzoic acid to the methyl ester, diazotizing the ester and reacting the diazo compound with KCN to form methyl 2-cyano-4-trifluoromethylbenzoate, hydrolysing this to form 4-trifluoromethyl-phthalic acid and cyclizing this to form the desired anhydride. Pharmaceutical compositions useful as tranquillizers and anticonvulsants comprise a compound II or a non-toxic acid addition salt thereof, together with a pharmaceutical carrier. The compositions may be in a form suitable for oral, parenteral, rectal or topical administration.