China Largest Manufacturer factory sales Prulifloxacin CAS 123447-62-1

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Prulifloxacin Basic information Abstract Quinolone antibiotics Indication Pharmacokinetics Prulifloxacin Intermediate Side effects References Product Name: Prulifloxacin Synonyms: 1h,4h-(1,3)thiazeto(3,2-a)quinoline-3-carboxylicacid,6-fluoro-1-methyl-7-(4-(;3-dioxol-4-yl)methyl)-1-piperazinyl)-4-oxo-(5-methyl-2-oxo-;(1R)-6-fluoro-1-methyl-7-[4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]-1-piperazinyl]-4-oxo-1H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid;Prulifloxacin(NM441,AF3013);CS-1352;Prulifloxacin, NM 441;nm441;Prulifloxacine CAS: 123447-62-1 MF: C21H20FN3O6S MW: 461.46 EINECS: 819-932-1 Product Categories: API;Other Products;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;QUISNON Mol File: 123447-62-1.mol   Prulifloxacin Chemical Properties Melting point  211-214°C Boiling point  633.2±65.0 °C(Predicted) density  1.62±0.1 g/cm3(Predicted) storage temp.  Sealed in dry,Store in freezer, under -20°C solubility  1 M NaOH: soluble25ML, clear, colorless (Solvent: 1 mg + 25 mL of NaOH) pka 5.85±0.40(Predicted) form  White to yellow crystalline solid. color  Off-White to Pale Yellow λmax 276nm(H2O)(lit.) Merck  14,7908 CAS DataBase Reference 123447-62-1(CAS DataBase Reference)   Safety Information RTECS  XJ0600000 MSDS Information   Prulifloxacin Usage And Synthesis Abstract Prulifloxacin, a prodrug of Ulifloxacin inhibits replication of bacterial DNA (nuclear material) by inhibition of DNA-gyrase in microbes, is a newer class of fluoroquinolone exerts broad-spectrum anti-bacterial activity against several Gram-positive and Gram-negative organisms. Prulifloxacin is generally prescribed for the treatment of uncomplicated lower urinary tract infections, acute exacerbations of chronic bronchitis and complicated lower urinary tract infections. Quinolone antibiotics Prulifloxacin is a quinolone antibiotic, a fluoroquinolone antibiotics prodrug NM394 by the Japan Pharmaceutical Co. and Meiji Seika Kaisha, Ltd. joint research and development in the late eighties, and it was first approved for marketing in December 2002 in Japan. the dosage form is 100mg tablets, by inhibiting bacterial DNA topoisomerase ⅱ and ⅳ activity and bacterial DNA synthesis, completing sterilization, which is different from the traditional model, without drug resistance to other classes of antibiotics. It is used for the treatment of respiratory gram-positive bacteria and negative bacteria clinically, which is caused by infections, urogenital infections, otolaryngology infection, biliary tract infections, enteritis, skin and soft tissue infections and surgical infections. Notable features are as follows: Anti-gram-positive bacteria are similar with ciprofloxacin. The anti-Gram-negative bacteria, led by pseudomonas aeruginosa, is better than the similar products, such as ciprofloxacin, ofloxacin, levofloxacin, resistance to green pus bacillus particularly high sensitivity, and the antibacterial abilitu is better than the gatifloxacin class and other antibiotics currently listed. The oral absorption is good without savings and cerebrospinal fluid distribution,  and the side effects is little. The half-life is as long as 8-9 hours, and the number of eating medication is few. Rapid onset, time to peak within 0.5 to 1 hour, the effet is stronger (due to bacterial accumulation in good). Indication It is used for the treatment of prulifloxacin sensitive staphylococcus, streptococcus, Neisseria gonorrhoeae, (except typhoid, paratyphoid) pneumoniae, Enterococcus, Moraxella Alex Salmonella, E. coli, Shigella, Salmonella, lemon acid bacteria, Klebsiella pneumoniae, Serratia, Proteus, Vibrio cholerae, Pseudomonas aeruginosa, Streptococcus digestion, they can cause the following infections: Superficial skin infections (acute superficial folliculitis, infectious impetigo), deep skin infections (cellulitis, erysipelas, boils, boils swollen disease, appendicitis, suppurative paronychia), chronic pyoderma (sebaceous cyst infection, purulent, etc.). Superficial secondary infections, such as abscess, trauma, burns, and surgical trauma. Acute respiratory infections (pharyngitis, tonsillitis, acute bronchitis), chronic respiratory disease secondary infection (chronic bronchitis, diffuse bronchiolitis, bronchiectasis, emphysema, pulmonary fibrosis, bronchial asthma, etc.) and pneumonia. Cystitis, pyelonephritis, prostatitis. Cholecystitis, cholangitis. Infectious enteritis, bacillary dysentery, salmonellosis, cholera. The uterine infection, adnexitis. Blepharitis, stye. Otitis media, sinusitis. Pharmacokinetics After oral administration, Prulifloxacin is rapidly metabolized as an active form of drug, Ulifloxacin. The drug exerts good penetration into the target tissue with prolonged elimination half-life with once-daily administration. After absorption, Cmax is generally achieved within one hour, and apparent Vss is 1231 L. About 45% of the administered drug is bound to plasma proteins. The drug is extensively metabolized by first-pass metabolism into active metabolites. The terminal half-life of Ulifloxacin is 10.6-12.1 hours. The drug is mainly excreted via the urine as unmetabolized drug. Prulifloxacin Intermediate Prulifloxacin Intermediate PL-7 Appearance: white to light yellow powder Chemical name: 6,7-difluoro-2-mercapto-ethyl-4-hydroxy-quinoline-3-carboxylic acid ethyl ester CAS: 154330-68-4  Molecular Formula: C14H13F2NO3S Prulifloxacin intermediate PL-9 Appearance: white to light yellow powder Chemical name: 6,7-difluoro-1-methyl-4-oxo--4H-(1,3) thiazine (3,2a) and quinoline-3-carboxylate CAS: 113046-72- Molecular Formula:C14H11F2NO3S Prulifloxacin Intermediate PL-10 Appearance: white to light yellow powder Chemical Name: 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl) 4H-(1,3) thiazine (3,2a) and quinoline-3-carboxylate CAS: 113028-17-4  Molecular Formula:C18H20FN3O3S Prulifloxacin Intermediate PL-11 Appearance: white to light yellow powder Chemical Name: 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3) thiazine (3,2a) and quinoline-3-carboxylic acid CAS : 112984-60-8 Molecular Formula:C16H16FN3O3S Application:For the total synthesis of gatifloxacin antibacterials Side effects Abdominal cramp, Confusion, Diarrhoea, Drowsiness, Altered taste, Epigastric pain, Gastritis, Headache, Hot flashes, Increased bilirubin in the blood, Itching, Loss of appetite, Sedation, Skin rash, Sleep disorder, Vomiting, Nausea. References # //www.drugsupdate.com/generic/view/1110/Prulifloxacin Description Prulifloxacin was launched as the third fluoroquinone. It was introduced in Japan as an oral treatment for urinary tract infections (UTls), respiratory tract infections (RTls) and bacterial pneumoniae. It can be synthesized in 10 steps from commercially available 3,4-difluoroaniline. Key steps involve the cyclization of 6,7-difluoro-rl-hydroxy-2- thioquinoline-3carboxylic acid ethyl ester with 1 ,I-dibromomethane to give the corresponding thiazeto-[3,2a]quinoline. Aromatic nucleophilic substitution of the 7-fluoro atom with piperazine followed by hydrolysis of the ethyl ester and finally alkylation of the piperazinyl moiety with 4-(bromomethyl)-5-methyl-l ,bdioxol-Bone complete the synthesis. Prulifloxacin is a lipophilic prodrug, which is rapidly hydrolyzed to the corresponding Ndealkylated piperazine, NM 394, by paraoxonase type enzymes in blood and liver following intestinal absorption. The DNA gyrase inhibitor NM 394 accounts for all antimicrobial activity: it shows a similar or greater activity against gram-positive bacteria compared to ciprofloxacin, and a greater activity in the case of gram-negative bacteria. In clinical studies, prulifloxacin has shown good efficacy against UTls and RTls. The drug is mainly excreted in the urine and in the feces as unchanged NM 394, which has a plasma half-life of approximately 8 h. Phototoxicity in animal models is less severe than with other quinolones. Prulifloxacin is well tolerated with an adverse effect profile similar to that of other fluoroquinolones. Chemical Properties Off-White Solid Originator Nippon Shinyaku (Japan) Uses Fluoroquinoline antibacterial; prodrug for active metabolite, Ulifloxacin. Antibacterial. Uses Prulifloxacin Polymorph I is a crystallization form of a synthetic chemotherapeutic antibiotic of the fluoroquinolone drug class. Prulifloxacin is a prodrug for active metabolite, Ulifloxacin. Antibacterial. Uses Prulifloxacin is a synthetic chemotherapeutic antibiotic of the fluoroquinolone drug class. Prulifloxacin is a prodrug for active metabolite, Ulifloxacin. Antibacterial. Brand name Sword Pharmaceutical Applications A lipophilic prodrug which is very rapidly metabolized by esterase into ulifloxacin, a 6-fluoro, 7-piperazinyl thiazetoquinoline. Ulifloxacin is moderately active against Staph. aureus (MIC 0.4–0.8 mg/L) and inactive against Str. pneumoniae (MIC 2–8 mg/L) as well as against Enterococcus spp. Against Enterobacteriaceae (MIC 0.05–0.8 mg/L) and Ps. aeruginosa (MIC 0.2–0.8 mg/L) activity is similar to that of ciprofloxacin. It is active against fastidious Gram-negative bacilli, but not against anaerobes and non-fermentative Gram-negative bacilli. Activity against Acinetobacter spp. is modest. Prulifloxacin is rapidly converted into ulifloxacin and after 3 h is no longer detected in blood. In volunteers receiving a single oral dose, peak plasma concentrations of 0.68 mg/L (300 mg dose) to 1.88 mg/L (for 400 mg dose) were attained between 0.67 and 1.25 h. The mean apparent elimination half-life was 8 h and the mean cumulative elimination rate in urine within 48 h was 31–46%. Other inactive metabolites account for 7% of the dose. Half the administered dose is eliminated in feces within 72 h as ulifloxacin and 4% as prulifloxacin. Protein binding is 45%. Chemical Synthesis The synthesis of prulifloxacin (22)started with the treatment of 3,4- difluoroaniline (183) with carbon disulfide in the presence of TEA to give the triethylammonium dithiocarbamate, which by reaction with ethyl chloroformate and TEA in chloroform, was converted into isothiocyanate 184 in 74% yield. Reaction of 184 with diethyl malonate in the presence of KOH in dioxane yielded methylenemalonate 185 potassium salt, which was ethylated with ethyl sulfate in ethanol to give compound 186 in excellent yield. 6,7- Difluoroquinoline 187 was obtained with the highest yield and regioselectivity when precursor 186 was heated in refluxing xylene. To suppress the side reaction in the subsequent chlorination, quinoline 187 was acylated to give 188 with acetyl chloride in chloroform. Chlorination of 188 with sulfuryl chloride gave compound 189 in 79% yield. Compound 189 was treated with sodium acetate in THF to afford cyclized compound 190, which was condensed with piperazine in DMF to give compound 191. The hydrolysis of ester 191 with KOH in hot t-butanol gave free acid 192, which was finally condensed with 4-(bromomethyl)-5- methyl-1, 3-dioxol-2-one (163) by treatment of potassium bicarbonate in DMF to give prulifloxacin (22).   Prulifloxacin Preparation Products And Raw materials

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Leader Biochemical Group is a large leader incorporated industry manufacturers and suppliers of advanced refined raw materials From the year of 1996 when our factory was put into production to year of 2020, our group has successively invested in more than 52 factories with shares and subordinates.We focus on manufacture Pharm & chemicals, functional active ingredients, nutritional Ingredients, health care products, cosmetics, pharmaceutical and refined feed, oil, natural plant ingredients industries to provide top quality of GMP standards products.All the invested factories' product lines cover API and intermediates, vitamins, amino acids, plant extracts, daily chemical products, cosmetics raw materials, nutrition and health care products, food additives, feed additives, essential oil products, fine chemical products and agricultural chemical raw materials And flavors and fragrances. Especially in the field of vitamins, amino acids, pharmaceutical raw materials and cosmetic raw materials, we have more than 20 years of production and sales experience. All products meet the requirements of high international export standards and have been recognized by customers all over the world. Our manufacture basement & R&D center located in National Aerospace Economic & Technical Development Zone Xi`an Shaanxi China. Now not only relying on self-cultivation and development as well as maintains good cooperative relations with many famous research institutes and universities in China. Now, we have closely cooperation with Shanghai Institute of Organic Chemistry of Chinese Academy of Science, Beijing Institute of Material Medical of Chinese Academy of Medical Science, China Pharmaceutical University, Zhejiang University. Closely cooperation with them not only integrating Science and technology resources, but also increasing the R&D speed and improving our R&D power. Offering Powerful Tech supporting Platform for group development. Keep serve the manufacture and the market as the R&D central task, focus on the technical research.  Now there are 3 technology R & D platforms including biological extract, microorganism fermentation and chemical synthesis, and can independently research and develop kinds of difficult APIs and pharmaceutical intermediates. With the strong support of China State Institute of Pharmaceutical Industry (hereinafter short for CSIPI), earlier known as Shanghai Institute of Pharmaceutical Industry (SIPI), we have unique advantages in the R & D and industrialization of high-grade, precision and advanced products.  Now our Group technical force is abundant, existing staff more that 1000 people, senior professional and technical staff accounted for more than 50% of the total number of employees, including 15 PhD research and development personnel, 5 master′ S degree in technical and management personnel 9 people. We have advanced equipment like fermentation equipment and technology also extraction, isolation, purification, synthesis with rich production experience and strict quality control system, According to the GMP required, quickly transforming the R&D results to industrial production in time, it is our advantages and our products are exported to North and South America, Europe, Middle East, Africa, and other five continents and scale the forefront in the nation, won good international reputation.  We believe only good quality can bring good cooperation, quality is our key spirit during our production, we are warmly welcome clients and partner from all over the world contact us for everlasting cooperation, Leader will be your strong, sincere and reliable partner in China.

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