Lomefloxacin

Product Introduction

Lomefloxacin (lomefloxacin) chemical name l-ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, off-white to yellow crystals, the molecular formula for C17H19F2N3O3, molecular weight of 351.34800, density of 1.342 g/cm3, melting point 239-240 ºC, boiling point of 542.7 ºC at 760 mmHg. 240ºC, boiling point 542.7ºC at 760 mmHg, clinically effective in urinary tract, respiratory tract and intestinal tract infections.

 

Product Photo and action

 

Product Specification 

 

 

Product Function

1. It is a long-acting quinolone oral antibacterial drug. It exerts antibacterial effect by inhibiting bacterial DNA gyrase and stopping bacterial growth. It has wide antimicrobial spectrum, high efficiency, safety, stable metabolism and good tolerance. Because there is no cross effect with theophylline, there is no contraindication to the concurrent use of asthma patients, so it is especially suitable for the use of the elderly. It can be used for respiratory tract infections, sepsis, enteritis, urinary tract infections, gynecological infections, eye and oral infections, and can also be used to prevent infection after surgery.
2. Used as anti-infective drug
3.Mainly used in the treatment of acute and chronic infectious diseases caused by various gram-positive and negative bacteria.

 

Production Methods
Method 1: 2,3,4-Trifluoronitrobenzene and RaneyNi were dissolved in ethanol and hydrogenated at atmospheric pressure. The catalyst was filtered off and concentrated to give 2,3,4-trifluoroaniline (I) in 91.7% yield. Diethyl ethoxymethylene malonate (EMME) was added to (I) and ethoxymethylene malonate (EMME) and stirred at 140-150 °C. The resulting ethanol was evaporated, diphenylethane was added, and the reaction was raised to 220 to 240°C to continue. Filtration and petroleum ether washing gave compound (II) in 88.3% yield. To a mixture of compound (Ⅱ), dimethylformamide and potassium carbonate, slowly drop ethyl bromide under stirring, and reacted at 50~60℃. Cooled to room temperature, filtered, concentrated and recrystallized with ethylene dichloride to give compound (III) in 90.3% yield. Boric acid and ethanoic anhydride, stirred at room temperature and then reflux reaction. Cooling, add compound (III), 90 ℃ reaction. Add water, filter and wash with water to obtain compound (IV) in 90.6% yield. Compound (IV), triethylamine and 2-methylpiperazine, room temperature reaction. Triethylamine was recovered, ethanol was added and compound (V) was obtained by filtration in 82.1% yield. Compound (V), 95% ethanol and triethylamine, reflux together. Cooled, filtered the solid and washed with a little ethanol to give white powdery crystalline lomefloxacin in 87.5% yield. Recrystallization with dimethylformamide gave colorless needle-like crystalline lomefloxacin with melting point 241-241.9°C. The crystalline lomefloxacin was obtained as a result of recrystallization with dimethylformamide. Lomefloxacin hydrochloride was obtained by the usual method in almost quantitative yield, and white needle-like crystals were obtained by recrystallization with water, melting point 296~300°C. Method 2: Take 2,3,4,5-fluorobenzoic acid as raw material, chlorinated by sulfoxide chloride to chloride, then condensed with diethyl ethoxy malonate, then decarboxylated to generate ethyl tetrafluorobenzoyl acetate, then condensed with triethyl orthoformate under the action of acetic anhydride to get the alkenyl bond, reacted with ethylamine to replace the ethoxy, and cyclized under the action of sodium hydride to generate the quinolinyl ring derivatives, the hydrolysis of ester group to carboxyl group, and finally reacted with 2- methylpiperazine to give lomefloxacin.2,3,4,5-Tetrafluorobenzoic acid can be obtained by the following reactions.

 

Product Application 

It is suitable for respiratory tract infections such as acute exacerbation of chronic bronchitis caused by sensitive bacteria, bronchial dilatation with infection, acute bronchitis, pneumonia and other infections of the genitourinary system, abdominal infections, biliary tract infections, intestinal infections, typhoid fever infections, soft tissue skin infections. Oral or IV, 400～600mg a day, qd～bid. the course of treatment varies from 3～14 days, according to the disease condition. When used as a prophylactic drug for transurethral operation and transrectal prostate biopsy, 400mg single dose should be taken 1~6 hours before operation. Dosage adjustment is required in patients with renal insufficiency. Lomefloxacin can be used for the following infections caused by sensitive bacteria:
(1) Genitourinary infections: including simple and complicated urinary tract infections, acute and chronic prostatitis, gonococcal urethritis or cervicitis (including those caused by enzyme-producing strains), acute cystitis, acute pyelonephritis and so on.
(2) Respiratory system infections: including pharyngolaryngitis, tonsillitis, sinusitis, otitis media, acute exacerbation of chronic bronchitis, acute exacerbation of chronic obstructive pulmonary disease (foreign data), bronchodilatation with infections, acute bronchitis, pneumonia and so on.
(3) Digestive system infections: including enteritis, cholecystitis, perianal abscess, etc.
(4) Prevention of surgical infections (e.g. for transrectal prostate puncture biopsy and urethra surgery to prevent urinary tract infections).
(5)This drug can be used for external eye infections, such as conjunctivitis, keratitis, corneal ulcers, dacryocystitis.
(6)This drug ear drops is used for otitis media, otitis externa, tympanitis caused by sensitive bacteria.
(7) Others: typhoid fever, bone and joint infections, skin and soft tissue infections and systemic infections such as sepsis.

 

Delivery & Packaging

We usual packaging the PS with foil bag powder 1kg/bag, export drum 25kg/drum.

Also accept customization service according your inquire.

As delivery,we can delivery product by courier,by sea, by air, ect.

The more details please check follow picture for reference:

 

If you have any question or inquire of Lomefloxacin, please contact our mail:info@haozbio.com

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