| 摘要 |
1432443 2 - Quinoxaline - carboxamide - 1,4- dioxides PFIZER Inc 26 March 1973 [1 May 1972] 14518/73 Heading C2C Compounds I: in which one of X 1 and X 2 is hydrogen, chloro, fluoro, bromo, methyl, methoxy, trifluoromethyl or -SO 2 -NR 3 R 4 (where R 3 and R 4 are hydrogen or methyl) and the other is hydrogen, chloro, bromo, methyl or methoxy with the proviso that when one of X 1 and X 2 is SO 2 -NR 3 R 4 , the other is hydrogen, R 1 is hydrogen, alkyl, cycloalkyl, hydroxyalkyl, phenyl or allyl, R 2 is hydrogen, allyl cycloalkyl, benzyl, alkyl (optionally substituted by amino, mono- or di-(C 1-4 alkyl)amino, pyrrolo, piperazino, pyrrolidino, piperidino, morpholino, piperazino (optionally N-substituted by hydroxy-C 1-4 alkyl, C 1-4 alkanoyl, C 1-4 alkyl or (C 1-4 alkoxy) carbonyl), imidazoldino, hydroxy, C 1-4 alkoxy, carboxy, (C 1-4 alkoxy) carbonyl, carbamoyl, mono- or di-(C 1-4 alkyl) carbamyl, C 1-4 alkanoyloxy or C 1-4 alkanoylamino) or phenyl (optionally substituted by C 1-4 alkyl, C 1-4 alkoxy, amino, mono- or di-(C 1-4 alkyl) amino, carboxy, (C 1-4 alkoxy) carbonyl, hydroxy, carbamoyl; or trifluoromethyl) or NR 1 R 2 represents pyrrolo, pyrrolidino, piperidino, morpholino, piperazino (optionally, N-substituted by C 1-4 alkyl, hydroxy C 1-4 alkyl, C 1-4 alkanoyl or (C 1-4 alkoxy) carbonyl) are prepared by reacting a benzofuroxan II: with an amine HNR 1 R 2 and a pyruvic acid ester CH 3 -CO-CO-OR in which R is an ester forming group preferably C 1-6 alkyl, phenyl (optionally substituted by methyl, methoxy or chloro), benzyl (optionally substituted by methoxy or bromo), phenethyl, chloroethyl, hydroxyethyl, dimethylaminopropyl, methoxyethyl or cyclohexyl. Compound II (X 1 =CF 3 , X 2 =H) is prepared from 2 - nitro - 4 - trifluoromethylaniline with NaNO 2 and cone. H 2 SO 4 to form an azide which cyclizes on reflux. Compounds II (X 1 = SO 2 NR 3 R 4 , X 2 =H; X 1 =OMe, X 2 =Me; X 1 = Cl, X 2 =Me or MeO) are prepared by reacting an X 1 , X 2 substituted 2-nitroaniline with NaOCl solution. |
