首页> 外国专利> 7-(1-Pyrrolidinyl)-3-quinolone-and -naphthyridone-carboxylic acid derivatives processes for their preparation and substituted mono- and bicyclic pyrrolidine derivatives as intermediate products for their preparation and antibacterial agents and feed additives containing them

7-(1-Pyrrolidinyl)-3-quinolone-and -naphthyridone-carboxylic acid derivatives processes for their preparation and substituted mono- and bicyclic pyrrolidine derivatives as intermediate products for their preparation and antibacterial agents and feed additives containing them

机译:7-(1-吡咯烷基)-3-喹诺酮和萘啶酮-羧酸衍生物的制备方法以及取代的单环和双环吡咯烷衍生物作为其制备的中间产物以及抗菌剂和含有它们的饲料添加剂

摘要

7-(1-Pyrrolidinyl)-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid and 7-(1-pyrrolidinyl)-1,4-dihydro-4-oxo-1,8-naphthyridin-3-carboxylic derivs. of formula (I), their hydrates, acid addition salts, as well as their alkali metal, alkaline earth, silver and guanidinium salts are new; X1 = halo; X2 = H, NH2, 1-4C alkylamino, di(1-3C alkyl)amino, OH, 1-4C alkoxy, SH, 1-4C alkylthio, arylthio or halo; R1 = 1-4C alkyl, 2-4C alkenyl, 3-6C cycloalkyl, 2-hydroxyethyl, 2-fluoroethyl, OMe, NH2, MeNH, EtNH or Me2N; or is Ph (opt. mono- or disubstd. by F); R2 = H, 1-4C alkyl or (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl; R3 = a gp. of formula (a): R4 = 1-4C alkyl, aryl or 1-4C acyl; R5 = H, 1-4C alkyl, OH or OMe; R6 = H, 1-4C alkyl (opt. substd. by OH), aryl, heteroaryl, benzyl, 1-4C alkoxycarbonyl, 1-4C acyl, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl or 3-6C cycloalkyl; R7 = H or 1-4C alkyl; R',R'' = H, Me or Ph; R''' = H or Me; Y = O, CH2, CH2CH2 or CH2O (where the bond to N may be via C as well as O); (Note: Y is not otherwise defined in claim 1). Z = O or S; A = N or CR8; R8 = H, halo, Me, CN, NO2 or OH, or R8+R1 = a bridge of type (b)-(d): Cpds. of formula (e) are excluded; R1 = 1-4C alkyl; R2,R3 = H or 1-4C alkyl; R4 = cyclopropyl, Ph, halophenyl, thienyl, opt. substd. by 1-4C alkyl or halo; R5 = halo. Also claimed is the S,S-configuration of a cpd. of formula (f) and its salts:A = CCl, CF or COMe.
机译:7-(1-吡咯烷基)-1,4-二氢-4-氧-3-喹啉羧酸和7-(1-吡咯烷基)-1,4-二氢-4-氧-1,8-萘啶-3 -羧基衍生物。在式(Ⅰ)中,它们的水合物,酸加成盐以及它们的碱金属,碱土金属,银和胍盐是新的; X <1> =卤素; X 2 = H,NH 2,1-4C烷基氨基,二(1-3C烷基)氨基,OH,1-4C烷氧基,SH,1-4C烷硫基,芳硫基或卤素; R 1 = 1-4C烷基,2-4C烯基,3-6C环烷基,2-羟乙基,2-氟乙基,OMe,NH 2,MeNH,EtNH或Me 2 N;或是Ph(被F独断或质疑); R 2 = H,1-4C烷基或(5-甲基-2-氧代-1,3-二氧杂-4-基)甲基; R 3 = gp。式(a)的通式:R 4 = 1-4C烷基,芳基或1-4C酰基。 R 5 = H,1-4C烷基,OH或OMe; R 6 = H,1-4C烷基(被OH取代),芳基,杂芳基,苄基,1-4C烷氧羰基,1-4C酰基,(5-甲基-2-氧代-1,3-二氧戊环-4-基)甲基或3-6C环烷基; R 7 = H或1-4C烷基; R',R''= H,Me或Ph; R'''= H或Me; Y = O,CH 2,CH 2 CH 2或CH 2 O(其中与N的键可以通过C以及O键); (注意:在权利要求1中未另行定义Y)。 Z = O或S; A = N或CR 8; R 8 = H,卤素,Me,CN,NO 2或OH,或R 8 + R 1 =(b)-(d)类型的桥:Cpds。式(e)中的不包括在内; R1 = 1-4C烷基; R2,R3 = H或1-4C烷基; R4 =环丙基,Ph,卤代苯基,噻吩基,最佳。取代通过1-4C烷基或卤素; R5 =卤素。还要求保护的是cpd的S,S-配置。式(f)的盐及其盐:A = CCl,CF或COMe。

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