2,4-二氯-5-氟-β-氧代苯丙酸乙酯置于sodium Hydroxide,乙酸酐,Sodium Hydride体系中,用 四氢呋喃,乙二醇二甲醚,二氯甲烷 作为反应溶剂,化学反应 7.0H,反应生成 7-氯-6-氟-1-对氟苯基-1,4-二氢-4-氧代-3-喹啉羧酸
参考文献:Synthesis And Structure-Activity Relationships Of Novel Arylfluoroquinolone Antibacterial Agents
标题:Synthesis And Structure-Activity Relationships Of Novel Arylfluoroquinolone Antibacterial Agents
摘要:A Series Of Novel Arylfluoroquinolones Has Been Prepared. These Derivatives Are Characterized By Having A Fluorine Atom At The 6-Position,Substituted Amino Groups At The 7-Position,And Substituted Phenyl Groups At The 1-Position. Structure-Activity Relationship (Sar) Studies Indicate That The In Vitro Antibacterial Potency Is Greatest When The 1-Substituent Is Either P-Fluorophenyl Or P-Hydroxyphenyl And The 7-Substituent Is Either 1-Piperazinyl,4-Methyl-1-Piperazinyl,Or 3-Amino-1-Pyrrolidinyl. The Electronic And Spatial Properties Of The 1-Substituent,As Well As The Steric Bulk,Play Important Roles In The Antimicrobial Potency In This Class Of Antibacterials. As A Result Of This Study,Compounds 45 And 41 Were Found To Possess Excellent In Vitro Potency And In Vivo Efficacy.
DOI:10.1021/jm00149A003