Raw material intermediate Norfloxacin Lactate Powder

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Norfloxacin Lactate Powder Usage and Synthesis.

Norfloxacin lactate is a broad-spectrum antibacterial drug that can be used to treat a variety of infectious diseases, especially for respiratory tract, urinary tract and gastrointestinal tract infections.

Uses and functions of Norfloxacin Lactate.

1.Upper respiratory tract infection: suitable for pharyngitis, tonsillitis, sinusitis and other upper respiratory tract infection.

2. Lower respiratory tract infection: suitable for acute bronchitis, pneumonia and other diseases.

3. Genitourinary system infection: suitable for cystitis, prostatitis, urethritis and other diseases.

4. Digestive tract infection: suitable for dysentery, gastroenteritis, gastritis, gastric ulcer and other diseases.

Physiological Effect of Norfloxacin Lactate.

Norfloxacin lactate is a fluoroquinolone antibiotic that inhibits bacterial growth and reproduction by blocking the activity of bacterial DNA synthase. In terms of pharmacology, it also has the following advantages:

1. Has a strong bactericidal effect, can kill a variety of gram-negative bacteria and Gram-positive bacteria, high sensitivity to drug-resistant bacteria.

2, the effect is rapid, absorption is good, similar to oral or injection.

3.It has strong penetration to tissues and can easily penetrate through cell membranes and tissues and accumulate in the interior of tissues.

4. Long half-life, lasting efficacy, oral once a day.

Production Method of  Bulk Norfloxacin Lactate Powder.

3,4-Dichloronitrobenzene is obtained by nitration of o-dichlorobenzene or chlorination of p-nitrochlorobenzene. In dimethyl sulphoxide and potassium fluoride, 3-chloro-4-fluoronitrobenzene is refluxed and fluorinated. In the presence of aqueous hydrochloric or acetic acid, 3-chloro-4-fluoroaniline was reduced with iron powder. This is then refluxed with triethyl orthoformate and diethyl malonate (producing diethyl ethoxymethylene malonate) in the presence of ammonium nitrate to give the condensation product. Heated cyclisation in liquid paraffin or diphenyl ether produces ethyl 7-chloro-6-fluoro-4-hydroxyquinoline-3-carboxylate.

Ethylation is carried out and then hydrolysed to give the ethylated product. Finally, it is condensed with piperazine to obtain norfloxacin. Its process is relatively mature, the yield is high, generally can reach 40% to 65%, but when the piperazine group is introduced in the 7 position, the by-product of the 6 fluorine atom being replaced can account for 25%, which is difficult to separate and affects the yield. The total yield was more than 8% by p-nitrochlorobenzene.

Before the introduction of pyrazine ring, 1-ethyl-6-fluoro-7-chloro-1,4-dihydro-4-oxoquinoline-8-carboxylic acid ethyl ester first and fluoroboric acid or boron trifluoride-ether or boron acetate reaction, so that the carbonyl group on the 4-position to form a boron chelate, and then the introduction of pyrazine group, the 7-position fluorine is replaced by the reduction of by-products, the yield can be increased by more than 15%, and the quality of the product improved.

The synthesis of norfloxacin has been studied more at home and abroad, but not many of them are really used in industrial production. The improvement of its synthetic route is mainly reflected in two aspects. One is to improve the ring-forming process, and the other is to do something about the introduction of piperazine group.

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