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2-bromo-5-fluoro 4-methylaniline 2-chloro-4-fluoro-5-methylbenzoic acid 2-chloro-4-fluoro-5-methylbenzonitrile 📜,亚硝酸丁酯,2-溴-5-氟-4-甲基苯胺,,盐酸置于乙醚,Magnesium Sulfate,正己烷体系中,用 乙腈 用作溶剂,化学反应 0.67H,以obtaining The Title Compound (5.6 G) As A Pale Yellow Oil的收率获得5-溴-4-氯-2-氟甲苯
参考文献:Pyridonecarboxylic Acid Derivatives Or Salts Thereof And Drugs
标题:Pyridonecarboxylic Acid Derivatives Or Salts Thereof And Drugs
摘要:本发明涉及一种以一般式(1)表示的吡啶酮羧酸衍生物:##str1##其中,R.Sup.1为--Oh,羧保护基或(烷基)氨基,R.Sup.2为h或--No.Sub.2,(保护的)氨基,(保护的)羟基,低级烷基或低级烷氧基,R.Sup.3为卤素原子,H或--No.Sub.2,低级烷基,低级烷氧基或氨基,R.Sup.4为偶氮基,(取代的)肼基,(取代的)氨基,低级烷氧基或羟基,R.Sup.5,R.Sup.6和r.Sup.7独立地为h,--No.Sub.2,卤素原子或低级烷基,R.Sup.8为--No.Sub.2,(取代的)氨基,--Oh或低级烷氧基,A为n或c--R.Sup.12,其中r.Sup.12为h,卤素原子或(取代的)低级烷基,低级烯基,低级炔基,低级烷氧基,低级烷硫基或硝基,B为n或c--R.Sup.13,其中r.Sup.13为h或卤素原子,或其盐,以及包含此类化合物作为活性成分的药物.该衍生物或其盐表现出优异的抗菌作用和口服吸收性,几乎不引起副作用,并且易于合成.
专利信息
专利号:US-6136823-A
优先权日:1996-11-28
标题 :Pyridonecarboxylic acid derivatives or salts thereof and drugs containing the same as the active ingredient
发明人:SAKAE NOBUYA; YAZAKI AKIRA; KURAMOTO YASUHIRO; YOSHIDA JIRO; NIINO YOSHIKO; OHSHITA YOSHIHIRO; HIRAO YUZO; HAYASHI NORIHIRO; AMANO HIROTAKA
权利人:WAKUNAGA PHARMA CO LTD
摘要:PCT No. PCT/JP97/04326 Sec. 371 Date May 28, 1999 Sec. 102(e) Date May 28, 1999 PCT Filed Nov. 27, 1997 PCT Pub. No. WO98/23592 PCT Pub. Date Jun. 4, 1998The invention relates to pyridonecarboxylic acid derivatives represented by the general formula (1): wherein R1 is -OH, a carboxy-protecting group or (alkyl)amino group, R2 is H, or -NO2, (protected) amino, (protected) hydroxyl, lower alkyl or lower alkoxyl group, R3 is a halogen atom, H, or -NO2, lower alkyl, lower alkoxyl or amino group, R4 is an azido, (substituted) hydrazino, (substituted) amino, lower alkoxyl or hydroxyl group, R5, R6 and R7 are independently H, -NO2, halogen atom or lower alkyl group, R8 is a -NO2, (substituted) amino, -OH or lower alkoxyl group, A is N or C-R12, in which R12 is H, halogen atom, or (substituted) lower alkyl, lower alkenyl, lower alkynyl, lower alkoxyl, lower alkylthio or nitro group, and B is N or C-R13, in which R13 is H or halogen atom, or salts thereof, and medicine comprising such a compound as an active ingredient. The derivatives or the salts thereof exhibit excellent antibacterial action and peroral absorbability, scarcely cause side effects, and are easy of synthesis.