Ciprofloxacin C3 amide derivative, preparation method thereof and application

• Main Authors: LIU BIN, WANG XIN, LIU BINGMI, DONG BOYANG, LIU CHANGZHI, JING JIAOJIAO
• Format: Patent
• Language: Chinese; English
• Published: 22.02.2017
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention discloses a ciprofloxacin C3 amide derivative, a preparation method thereof and an application. The ciprofloxacin C3 amide derivative is provided with a structure as shown in a formula (I). Ciprofloxacin hydrochloride is added into excessive methylene dichloride, triethylamine is dripped to adjust the pH (potential of hydrogen) of reaction liquid to be 7.5-8.5, an appropriate amount of ethyl chloroformate is added, the reaction liquid is subjected to return flow agitation at the temperature of 20 DEG C and is clear, triethylamine is dripped into the reaction liquid so that the pH of the reaction liquid is 7.5-8.5, arylamine is added, return flow is continued for 1-2 hours, and the reaction liquid is cooled, reduced pressure distillation and concentration to obtain a target product. The ciprofloxacin C3 amide derivative has good sonodynamic activity and is obviously superior to ciprofloxacin in terms of microwave synergistic antibacterial effect. 本发明公开了种环丙沙星C3酰胺衍生物及其制备方法和应用。环丙沙星C3酰胺衍生物具有通式(Ⅰ)的结构。