Pharmaceutical raw material Ofloxacin CAS 82419-36-1

CAS:82419-36-1

MF: C18H20FN3O4

MW:361.37

EINECS:680-263-1

Specification: 99% min Ofloxacin

Sample:Ofloxacin Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance:Colorless needles from ethanol

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Ofloxacin Usage and Synthesis.

Oxyfloxacin has the third generation quinolone antibacterial activity, it has good antibacterial effect on Staphylococcus, Streptococcus, Streptococcus pneumoniae, Neisseria gonorrhoeae, Bacillus citriodora, Shigella, Klebsiella pneumoniae, Enterobacteriaceae, Serratiaceae, Aspergillus, Haemophilus influenzae, Fusobacterium indolentum, Campylobacter, etc., and it also has certain antibacterial effects on Pseudomonas aeruginosa and Chlamydia trachomatis, and has the function of anti-TB. It also has the effect of anti-tuberculosis mycobacteria, and can be used with isoniazid and rifampicin in the treatment of tuberculosis. It has strong antibacterial effect on Gram-positive and negative bacteria.

It also has good effect on anaerobic bacteria and Mycoplasma pneumoniae. Antibacterial activity against Aureus, haemolytic streptococcus, etc. is 4-8 times stronger than that of haloperidol.

Clinically, it is mainly used for acute and chronic infections of respiratory tract, pharynx, tonsils, urinary tract including prostate, skin and soft tissues, intestines and otolaryngology caused by sensitive bacteria.

Uses and functions of Ofloxacin.

The third generation of quinolone synthetic antimicrobials has the advantages of wide antimicrobial spectrum, strong antimicrobial activity, good bioavailability, safe and effective for oral administration, low toxicity effect, no drug resistance and so on.

It has good antibacterial effect on a variety of Gram-positive and Gram-negative bacteria, and also has antibacterial effect on Pseudomonas aeruginosa and Chlamydia.

For strains resistant to neopenicillin, clindamycin, gentamicin and strains resistant to haloperidol, the product works well without cross-resistance.

In addition, it also has a certain antibacterial effect on anaerobic bacteria. It is used for respiratory infections, intestinal infections, skin and soft tissue infections, urinary system infections caused by sensitive bacteria.

Drug interactions of Ofloxacin.

Ofloxacin is widely used in combination with other antibiotics, antipyretic and analgesic drugs, antiviral drugs, immunomodulators or developed into compound preparations.

According to the market survey, some provinces and cities have approved more compounded ofloxacin preparations, such as ofloxacin diclofenac sodium injection, ofloxacin hydrochloride levamisole tablets, etc., to expand the antimicrobial spectrum for comprehensive prevention and treatment, especially for other antibiotics with relatively poor efficacy of streptococcus, pneumococcus, mycoplasma, anaerobic bacteria and so on, have a good effect.

Commonly paired with drugs are:

1. with astragali polysaccharide, Panax quinquefolium or Qianlong and other antiviral drugs, used for bacterial and viral combined infections;

2. with antipyretic and analgesic drugs such as anacin or diclofenac sodium, ketorolac, used for bacterial fever;

3. Compounding with herbs such as fritillaria and chaihu for summer fever;

4. Compounding with metronidazole for severe anaerobic infections;

5. Combined with doxycycline hydrochloride and sulphonamides for haematological protozoa;

6. Combined with dysentery and safranin, used for intestinal disorders.

Production Methods of Bulk Ofloxacin.

Method 1: Using 2,3,4-trifluoronitrobenzene as the starting material, the product is obtained by selective alkali hydrolysis, etherification, reduction, condensation with C2H5OCH=C(COOEt)2 or (CH3)2NCH=C(COOEt)2, cyclohexylation, hydrolysis, and the action of boron acetate, and then the introduction of N-methyl piperazine.

Method 2: Taking phthalimide derivatives as raw materials, tetrafluorophthalimide was generated by fluorination, hydrolysis and decarboxylation to generate 2,3,4,5-tetrafluorobenzoic acid, then chlorination, acylation and decarboxylation to generate 2,3,4,5-tetrafluorobenzoylacetic acid ethyl ester, then reacted with diethyl orthoformate, then 2-aminopropanol, and then cyclised to generate pyrido[1,2,3-de][1,4]phenyl and heyzine derivatives, and finally reacted with piperazine to form ofloxacin.

Method 3: The ethyl tetrafluorobenzoylacetate obtained above was first reacted with methyl piperazine to introduce a piperazine group, then introduced a side chain and then cyclised, and then hydrolysed to obtain ofloxacin. In the preparation of ofloxacin, the introduction of piperazine group is a research hot spot.

The later the introduction, the greater the effect on its yield. This method introduces piperazine first, and its introduction yield can reach 88%. However, a strong base, such as sodium hydride, must be used for cyclisation.