Molecular Formula | C19H15F3N4O3 |
Molar Mass | 404.34 |
Density | 1.558±0.06 g/cm3(Predicted) |
Boling Point | 614.4±55.0 °C(Predicted) |
pKa | 5.79±0.70(Predicted) |
Physical and Chemical Properties | Chemical properties colorless needle crystal, melting point 266~268 ℃. |
Use | The use has broad-spectrum antibacterial activity. It has strong antibacterial activity against Gram-positive bacteria including Staphylococcus aureus, epiporum, suppuration and Streptococcus pneumoniae, and has strong antibacterial activity against Gram-negative bacteria including Pseudomonas aeruginosa and anaerobic bacteria. Strong antibacterial activity and bactericidal effect. Used for respiratory tract infection, soft tissue injury, pneumonia, urinary tract infection, gynecological infection, oral and otolaryngological infection. |
Raw Materials | p-Toluenesulfonic acid Glycine Pyrrolidine 2,4-Difluoroaniline 2-Chloropyridine-N-oxide Ethyl fluoroacetate 3-Aminopyrrolidine Tosufloxacin |
The process using orthopyridine as raw material is as follows.
In addition, 2, 6-dichloro-5-fluoro-3-acetylchloropyridine is used as the raw material, and diethyl malonate is reacted to form malonic acid derivatives, and then hydrolyzed and decarboxylated to form acetic acid derivatives, and then first with the original Methyl triethyl ester, then react with 2, 4-difluoroaniline, and then cyclize to form naphthalene derivatives, react with 3-aminotetrahydropyrrole to form polyfluorinated acid, and finally with p-toluene sulfonic acid in aqueous ethanol Salt, tofloxacin was obtained.
Its main intermediate 2, 6-dichloro-5-fluoro-3-acetylchloropyridine can be formed by the following reaction with ethyl fluoroacetate as raw material.
Another intermediate, 3-aminotetrahydropyrrole, can be prepared from glycine.