Synthesis and Application of Ceftazidime

Synthesis and Application of Ceftazidime

Introduction of Ceftazidime:
Ceftazidime Antibiotic Powder is a third-generation cephalosporin antibiotic. CAS: 72558-82-8, Ceftazidime Raw Material white high-purity powder, exported from Chinese pharmaceutical raw material factory, easy customs clearance, short lead time, factory price supply.
Ceftazidime is a third-generation cephalosporin antibiotic. Similar to other third-generation cephalosporins, it has a broad response against both Gram-positive and Gram-negative bacteria. The difference is that it is effective against Pseudomonas aeruginosa, but weak against Gram-positive bacteria, so it would not be used for this infection. Cefotaxime is sold under trademarks including "Vidaxin®". Ceftazidime is a semi-synthetic third-generation cephalosporin. Compared with the first and second-generation cephalosporins, its antibacterial spectrum is further expanded and its antibacterial activity is stronger. Ceftazidime Pseudomonas aeruginosa, Escherichia coli, Enterococcus, Salmonella, Shigella, Neisseria gonorrhoeae, hemolytic streptococcus, pneumococcus, etc. have strong antibacterial activity. Ceftazidime is mainly used clinically for sepsis, bacteremia, pleurisy, peritonitis, prostatitis, cystitis, otitis media, malignant otitis externa, sinusitis, skin infection, pelvic inflammatory disease, etc. Ceftazidime is widely used in the treatment of various moderate and severe infections, and is the drug of choice for the treatment of critically ill patients infected with Gram-negative bacteria.

Ceftazidime mechanism of action:
Ceftazidime (containing sodium carbonate) is a third-generation cephalosporin. Enterobacteriaceae bacteria are highly sensitive to this product, and its antibacterial activity is slightly worse than that of cefotaxime. It has good antibacterial effect on Pseudomonas aeruginosa, and it is a cephalosporin. The one with the strongest activity; combined with tobramycin and amikacin showed obvious synergistic effect on multidrug-resistant Pseudomonas aeruginosa, and combined with cefsulodin, mezlocillin or piperacillin on Pseudomonas aeruginosa Bacteria and Escherichia coli can produce synergistic or additive effects; Legionella pneumophila is sensitive to this product; it also has antibacterial effects on Gram-positive bacteria and some anaerobic bacteria, and its antibacterial activity is lower than that of cefazolin and cefotaxime ; No antibacterial effect on methicillin-resistant Staphylococcus, Enterococcus and Campylobacter pylori or Clostridium difficile. It is suitable for the treatment of various serious Gram-negative bacilli infections including Pseudomonas aeruginosa.

Ceftazidime Uses:
Ceftazidime Antibiotic Powder (containing sodium carbonate) is used for pneumonia and lower respiratory tract infection, intra-abdominal and biliary tract infection, complicated urinary tract infection and severe skin and soft tissue infection caused by gram-negative bacilli. It is especially suitable for infection of immunocompromised persons caused by multiple drug-resistant Gram bacteria, nosocomial infection, and central nervous system infection caused by Gram-negative bacilli or Pseudomonas aeruginosa. Ceftazidime Antibiotic Powder is the third-generation broad-spectrum cephalosporin, which is stable to a variety of β-lactamases, has strong bactericidal effect on Gram-positive bacteria, negative bacteria and anaerobic strains, and is highly effective against Pseudomonas aeruginosa. Ceftazidime Antibiotic Powder is the only cephalosporin antibiotic that can replace aminoglycosides, so some people call it the fourth-generation cephalosporin antibiotic. Ceftazidime Raw Material is clinically used for common serious infections caused by sensitive bacteria (such as sepsis, meningitis, bacteremia, etc.), respiratory tract infections (such as pneumonia, bronchitis, etc.), ear, nose and throat infections, skin and soft tissue infections, urinary tract infections Infection, gastrointestinal, gallbladder and abdominal infection, bone and joint infection, etc. Semi-synthetic broad-spectrum cephalosporins are mainly used for infections of the respiratory system, urinary system, and soft tissue systems caused by sensitive bacteria.

Ceftazidime Powder Raw Material Synthesis:
Using cefotaxime as a raw material, because cefotaxime has 3-pyridyl methyl group. After silylation with trimethylsilyl chloride, react with phosphorus pentachloride at low temperature, add lower alcohols or diols to obtain amorphous solids, and then use suitable solvents such as acetonitrile or isopropanol containing hydrochloric acid to remove Work-up yields pure crystalline compound (VI). Then react with the dichloromethane solution of compound (II), after the reaction liquid is washed with water and steamed to remove dichloromethane, dimethylformamide is added to obtain pure compound (VII) containing 2.5 molecular dimethylformamide, basically No impurities. Add a mixture of formic acid and hydrochloric acid to the dimethylformamide solution of compound (VII) for treatment, remove the precipitate by filtration, and then add acetone or methanol to obtain very pure compound (VIII). The compound (Ⅷ) is dissolved in water, the pH value is adjusted to the isoelectric point, and the precipitated ceftazime pentahydrate is crystallized, with a high yield and a pure and stable product. The side chain compound (I) used can be synthesized by the following method.