CAS: 111542-93-9; Sparfloxacin

上下游产品

5-Amino-1-cyclopropyl-6,7,8-trifluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid 3,5-dimethylpiperazine 2,3,4,5-tetrafluorobenzoic acid 2,3,4,5-tetrafluoro-6-nitrobenzoic acid

1-环丙基-5-酰胺-6,7,8-三氟-1,4-二氢-4-氧代-3-喹啉羧酸乙酯置于盐酸,三乙胺体系中,用 吡啶 用作溶剂,化学反应 2.0H,反应生成司氟沙星
参考文献:Synthesis And Biological Activity Of 5-Amino-And 5-Hydroxyquinolones,And The Overwhelming Influence Of The Remote N1-Substituent In Determining The Structure-Activity Relationship
标题:Synthesis And Biological Activity Of 5-Amino-And 5-Hydroxyquinolones,And The Overwhelming Influence Of The Remote N1-Substituent In Determining The Structure-Activity Relationship
摘要:A Series Of 5-Amino-And 5-Hydroxyquinolone Antibacterials Substituted At C7 With A Select Group Of Common Piperazinyl And 3-Aminopyrrolidinyl Side Chains Was Prepared. These 5-Substituted Derivatives Were Compared To The Analogous 5-Hydrogen Compounds For Antiinfective Activity By Using Dna Gyrase Inhibition,Minimum Inhibitory Concentrations Against A Variety Of Bacteria,And In Vivo Efficacy In The Mouse Infection Model. The Influence On The Structure-Activity Relationships Of Varied Substituents At C8 (H,F,Cl) And Ni (Ethyl,Cyclopropyl,Difluorophenyl) Was Also Studied. The Results Showed That Several Of The Structure-Activity Conclusions Regarding Side-Chain Bulk At C7,The Effect Of Halogen At C8,And The Effect Of The C5-Amino Group Were Greatly Influenced By The Choice Of The N1-Substituent. Several Outstanding Broad Spectrum Quinolones Were Identified In This Work. In Particular,The Spectrum And Potency Of The 7-Piperazinyl Quinolones Could Be Greatly Enhanced By The Judicious Choice Of C5-,C8-,And N1-Substitutents.
Doi:10.1021/jm00107A039

专利信息

专利号:US-8093381-B2
优先权日:2007-05-24
标题:Method of synthesis of fluoroquinolones
发明人：BERTHON-CEDILLE LAURENCE; LEGUERN MARIE-EMMANUELLE; RENAUD GILLES; TOMBRET FRANCIS
权利人:BERTHON-CEDILLE LAURENCE; LEGUERN MARIE-EMMANUELLE; RENAUD GILLES; TOMBRET FRANCIS; BIOCODEX
摘要:The invention relates to a method of preparation of fluoroquinolones of formula (I) from compounds of formula (II): n nin which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and X are as defined in Claim 1.

专利号:US-2009054643-A1
优先权日:2007-05-24
标 题:Novel method of synthesis of fluoroquinolones