Method for preparing Derivatives of (naftiridina - 1.8 - 2 (IL - 2) - 1 piperazinil carbonyloxy) - 1 and - 3 isoindolinona counterparts (mono and diazotados naftiridina - 18 - 2 (IL) - 6 - 1 - piperazinil carbonyloxy) - 7 - (naftiridina1,8 pirrolpiridinas oxo 5 and IL - 2), 6 (1 piperazinil carbonyloxy) pirrolpirazinas oxo - 7 5

摘要

1417935 Naphthyridine derivatives RHONEPOULENC SA 13 May 1974 [15 May 1973 14 March 1974 (2)] 21081/74 Heading C2C Novel compounds I (in which one symbol X is =N-and the others are all -CY=; Y is H, halo, 1-4 C alkyl or alkoxy, CN or NO 2 ; A is =CH- and A 1 is =CH- or =N- or A is =N- and A 1 is =N-; Z is H, halo, 1-4 C alkyl or alkoxy or NO 2 ; m is 0 or 1-4; and (i) n is O or R is H, 1-4 C alkyl, 2-4 C alkenyl or alkynyl, 1-4 C hydroxyalkyl or phenyl or (ii) n is 1 and R is 1-4 C alkyl or hydroxyalkyl or phenyl) and acid addition salts thereof are prepared by (i) reaction of a piperazine II with a naphthyridine III or an alkali metal derivative thereof; (ii) reaction of a piperazine VIII with a mixed carbonate IX (in which Ar is phenyl which may be substituted by 1-4 C alkyl or NO 2 ) or (iii) oxidation of a compound I in which n is 0 to give a compound in which n is 1. Compounds III may be prepared by reaction of a compound V with a compound VI to give a compound VII cyclization of the compound VII to give an imide IV which is then partially reduced. Compounds VIII in which n is 1 may be prepared by oxidation of those in which n is 0. Compounds IX may be prepared by reaction of a chloroformate CICOOAr with a compound III. 2 - Amino - 7 - methoxy - 1,8 - naphthyridine is prepared by reaction of sodium methoxide with 2 - acetamido - 7 - chloro - 1,8 - naphthyridine. Pharmaceutical compositions useful as anticonvulsants and tranquillizers comprise a compound I or a suitable salt thereof in combination with a carrier or diluent.