China Largest Manufacturer factory sales Bezafibrate CAS 41859-67-0 CAS NO.41859-67-0

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Bezafibrate Basic information Product Name: Bezafibrate Synonyms: Bezafibrate D6 (dimethyl D6);Bezabrate D6 (DiMethyl D6);2-(4-{2-[(4-chlorophenyl)forMaMido]ethyl}phenoxy)-2-Methylpropanoic acid;Bezafibrate-d6;BEZAFIBRATE EPB(CRM STANDARD);BEZAFIBRATE MM(CRM STANDARD);bezafibrat;bezafibrato CAS: 41859-67-0 MF: C19H20ClNO4 MW: 361.82 EINECS: 255-567-9 Product Categories: Intracellular receptor;Intermediates & Fine Chemicals;Active Pharmaceutical Ingredients;Pharmaceuticals;Pharmaceutical intermediates;Cardiovascular Drugs Mol File: 41859-67-0.mol   Bezafibrate Chemical Properties Melting point  184 °C Boiling point  572.1±45.0 °C(Predicted) density  1.260±0.06 g/cm3(Predicted) storage temp.  2-8°C solubility  DMF: soluble form  solid pka 3.29±0.10(Predicted) color  White to Off-White Merck  14,1195 Stability: Hygroscopic CAS DataBase Reference 41859-67-0(CAS DataBase Reference) EPA Substance Registry System Propanoic acid, 2-[4-[2-[(4-chlorobenzoyl)amino]ethyl]phenoxy]-2-methyl- (41859-67-0)   Safety Information Hazard Codes  Xn Risk Statements  22 Safety Statements  36 WGK Germany  1 RTECS  UE8755000 HS Code  29242990 Toxicity LD50 oral in rat: 1082mg/kg MSDS Information Provider Language 2-[4-[2-(4-Chlorobenzamido)ethyl]phenoxy]-2-methylpropanoic acid English SigmaAldrich English   Bezafibrate Usage And Synthesis Description Bezafibrate is a non-selective agonist of peroxisome proliferator-activated receptors (PPARs; EC50s = 50, 60, and 20 μM for human PPARα, PPARγ, and PPARδ, respectively). It reduces triglyceride levels and the size of lipid droplets in an oleic acid-induced HepaRG hepatocyte model of steatosis when used at a concentration of 25 μM. Bezafibrate (10 mg/kg per day) reduces plasma VLDL and LDL mass and triglyceride and free fatty acid levels in a high-fructose plus lard diet-induced rat model of insulin resistance. Chemical Properties Off-White Solid Originator Bezafibrate,Eipico Co. Uses Antilipemic Uses antihyperlipidemic Uses anti-hyperlipoproteinemic Uses Bezafibrate has been used: a supplement in the standard diet (SD) for mice to study its effect on diabetes to evaluate its effect on hepatitis C virus (HCV) assembly and secretion to evaluate its effect on gonadal steroidogenesis and spermatogenesis of zebrafish and also used as standard for HPLC Manufacturing Process 0.292 moles p-chlorobenzoyl chloride and 50 ml dry pyridine were added dropwise to 0.146 moles tyramine in 60 ml dry pyridine for 10 minutes. Then the mixture was poured in about 500 g of ice with water. The fallen-out crystals was filtered off, washed with diluted HCl, water and NaHCO3 solution and dried. It was recrystallized from acetone to give di(4-chlorobenzoyl) tyramine; yield 98 %; MP: 203°-205°C. 0.11 moles above product in 400 ml methanol was mixed with 130 ml 2 N KOH and heated at 40°-45°C for 1 hour. On cooling 130 ml 2 N HCl was added. The fallen-out precipitate was filtered off, filtrate was distilled off to dryness. The residue was washed with water, NaHCO3 solution and recrystallized from ethanol to give N-(4-chlorobenzoyl)tyramine; yield 91%; MP: 174°-176°C. 2.14 g sodium was dissolved in 50 ml of absolute methanol and mixed with 0.93 mole N-(4-chlorobenzoyl)tyramine. Methanol was removed in vacuum to dryness. The residue was slurried in 100 ml absolute toluene and 0.137 moles 2-bromo-2-methylpropionic acid ethyl ester was added. The suspension was heated for 25 hours at 80°C. Then it was distilled in vacuum to dryness and the residue was dissolved in CH2Cl2, washed with diluted HCl, NaOH and water, and dried over CaCl2. On removing of the solvent, the crude 2-{4-[2- (4-chlorobenzoylamino)ethyl]phenoxy}-2-methylpropionic acid ethyl ester was obtained. After recrystallization from ether/ ligroin and acetone it had MP: 96°-97°C; yield 67 %. 0.1 mole above ester in 1.5 L of dioxane was slowly mixed with 200 ml 1 N KOH at ambient temperature and stood for 2 hours, then it was heated at 40°C for 1 hour. The substance was dissolved completely. On cooling the mixture was neutralized with 200 ml 1 N HCl. The solvents were removed in vacuum. The residue was washed with water and recrystallized from acetone to give 2-{4-[2-(4-chlorobenzoylamino)ethyl]phenoxy}-2-methylpropionic acid; yield 84%; MP: 186°C. Therapeutic Function Antihyperlipidemic Biochem/physiol Actions The peroxisome proliferator-activated receptor (PPAR) is a member of the steroid nuclear receptor superfamily. Bezafibrate is a peroxisome proliferator-activated receptor agonist for PPARα, PPARδ, and PPARγ. Lipoprotein lipase (LPL) activator.PPARgamma agonists, including Bezafibrate, have beneficial effects in the suppression of the inflammatory response during RSV infection and therefore might have clinical efficacy in the course of severe RSV-infection. Clinical Use Hyperlipidaemia Drug interactions Potentially hazardous interactions with other drugs Antibacterials: increased risk of myopathy with daptomycin - try to avoid concomitant use. Anticoagulants: enhances effect of coumarins and phenindione; dose of anticoagulant should be reduced by up to 50% and adjusted by monitoring INR. Antidiabetics: may improve glucose tolerance and have an additive effect with insulin or sulphonylureas. Ciclosporin: may increase nephrotoxicity and reduce ciclosporin levels. Colchicine: possible increased risk of myopathy. Lipid-regulating drugs: increased risk of myopathy in combination with statins and ezetimibe - avoid with ezetimibe; do not exceed 10 mg of simvastatin and 20 mg of rosuvastatin. Metabolism 50% of the administered bezafibrate dose is recovered in the urine as unchanged drug and 20% in the form of glucuronides. Elimination is rapid, with excretion almost exclusively renal. 95% of the activity of the [14C]-labelled drug is recovered in the urine and 3% in the faeces within 48 hours.   Bezafibrate Preparation Products And Raw materials Raw materials 4-Chlorobenzoyl chloride-->Tyramine-->Ethyl 2-bromoisobutyrate-->Sodium

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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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Bezafibrate Basic information Product Name: Bezafibrate Synonyms: Bezafibrate D6 (dimethyl D6);Bezabrate D6 (DiMethyl D6);2-(4-{2-[(4-chlorophenyl)forMaMido]ethyl}phenoxy)-2-Methylpropanoic acid;Bezafibrate-d6;BEZAFIBRATE EPB(CRM STANDARD);BEZAFIBRATE MM(CRM STANDARD);bezafibrat;bezafibrato CAS: 41859-67-0 MF: C19H20ClNO4 MW: 361.82 EINECS: 255-567-9 Product Categories: Intracellular receptor;Intermediates & Fine Chemicals;Active Pharmaceutical Ingredients;Pharmaceuticals;Pharmaceutical intermediates;Cardiovascular Drugs Mol File: 41859-67-0.mol   Bezafibrate Chemical Properties Melting point  184 °C Boiling point  572.1±45.0 °C(Predicted) density  1.260±0.06 g/cm3(Predicted) storage temp.  2-8°C solubility  DMF: soluble form  solid pka 3.29±0.10(Predicted) color  White to Off-White Merck  14,1195 Stability: Hygroscopic CAS DataBase Reference 41859-67-0(CAS DataBase Reference) EPA Substance Registry System Propanoic acid, 2-[4-[2-[(4-chlorobenzoyl)amino]ethyl]phenoxy]-2-methyl- (41859-67-0)   Safety Information Hazard Codes  Xn Risk Statements  22 Safety Statements  36 WGK Germany  1 RTECS  UE8755000 HS Code  29242990 Toxicity LD50 oral in rat: 1082mg/kg MSDS Information Provider Language 2-[4-[2-(4-Chlorobenzamido)ethyl]phenoxy]-2-methylpropanoic acid English SigmaAldrich English   Bezafibrate Usage And Synthesis Description Bezafibrate is a non-selective agonist of peroxisome proliferator-activated receptors (PPARs; EC50s = 50, 60, and 20 μM for human PPARα, PPARγ, and PPARδ, respectively). It reduces triglyceride levels and the size of lipid droplets in an oleic acid-induced HepaRG hepatocyte model of steatosis when used at a concentration of 25 μM. Bezafibrate (10 mg/kg per day) reduces plasma VLDL and LDL mass and triglyceride and free fatty acid levels in a high-fructose plus lard diet-induced rat model of insulin resistance. Chemical Properties Off-White Solid Originator Bezafibrate,Eipico Co. Uses Antilipemic Uses antihyperlipidemic Uses anti-hyperlipoproteinemic Uses Bezafibrate has been used: a supplement in the standard diet (SD) for mice to study its effect on diabetes to evaluate its effect on hepatitis C virus (HCV) assembly and secretion to evaluate its effect on gonadal steroidogenesis and spermatogenesis of zebrafish and also used as standard for HPLC Manufacturing Process 0.292 moles p-chlorobenzoyl chloride and 50 ml dry pyridine were added dropwise to 0.146 moles tyramine in 60 ml dry pyridine for 10 minutes. Then the mixture was poured in about 500 g of ice with water. The fallen-out crystals was filtered off, washed with diluted HCl, water and NaHCO3 solution and dried. It was recrystallized from acetone to give di(4-chlorobenzoyl) tyramine; yield 98 %; MP: 203°-205°C. 0.11 moles above product in 400 ml methanol was mixed with 130 ml 2 N KOH and heated at 40°-45°C for 1 hour. On cooling 130 ml 2 N HCl was added. The fallen-out precipitate was filtered off, filtrate was distilled off to dryness. The residue was washed with water, NaHCO3 solution and recrystallized from ethanol to give N-(4-chlorobenzoyl)tyramine; yield 91%; MP: 174°-176°C. 2.14 g sodium was dissolved in 50 ml of absolute methanol and mixed with 0.93 mole N-(4-chlorobenzoyl)tyramine. Methanol was removed in vacuum to dryness. The residue was slurried in 100 ml absolute toluene and 0.137 moles 2-bromo-2-methylpropionic acid ethyl ester was added. The suspension was heated for 25 hours at 80°C. Then it was distilled in vacuum to dryness and the residue was dissolved in CH2Cl2, washed with diluted HCl, NaOH and water, and dried over CaCl2. On removing of the solvent, the crude 2-{4-[2- (4-chlorobenzoylamino)ethyl]phenoxy}-2-methylpropionic acid ethyl ester was obtained. After recrystallization from ether/ ligroin and acetone it had MP: 96°-97°C; yield 67 %. 0.1 mole above ester in 1.5 L of dioxane was slowly mixed with 200 ml 1 N KOH at ambient temperature and stood for 2 hours, then it was heated at 40°C for 1 hour. The substance was dissolved completely. On cooling the mixture was neutralized with 200 ml 1 N HCl. The solvents were removed in vacuum. The residue was washed with water and recrystallized from acetone to give 2-{4-[2-(4-chlorobenzoylamino)ethyl]phenoxy}-2-methylpropionic acid; yield 84%; MP: 186°C. Therapeutic Function Antihyperlipidemic Biochem/physiol Actions The peroxisome proliferator-activated receptor (PPAR) is a member of the steroid nuclear receptor superfamily. Bezafibrate is a peroxisome proliferator-activated receptor agonist for PPARα, PPARδ, and PPARγ. Lipoprotein lipase (LPL) activator.PPARgamma agonists, including Bezafibrate, have beneficial effects in the suppression of the inflammatory response during RSV infection and therefore might have clinical efficacy in the course of severe RSV-infection. Clinical Use Hyperlipidaemia Drug interactions Potentially hazardous interactions with other drugs Antibacterials: increased risk of myopathy with daptomycin - try to avoid concomitant use. Anticoagulants: enhances effect of coumarins and phenindione; dose of anticoagulant should be reduced by up to 50% and adjusted by monitoring INR. Antidiabetics: may improve glucose tolerance and have an additive effect with insulin or sulphonylureas. Ciclosporin: may increase nephrotoxicity and reduce ciclosporin levels. Colchicine: possible increased risk of myopathy. Lipid-regulating drugs: increased risk of myopathy in combination with statins and ezetimibe - avoid with ezetimibe; do not exceed 10 mg of simvastatin and 20 mg of rosuvastatin. Metabolism 50% of the administered bezafibrate dose is recovered in the urine as unchanged drug and 20% in the form of glucuronides. Elimination is rapid, with excretion almost exclusively renal. 95% of the activity of the [14C]-labelled drug is recovered in the urine and 3% in the faeces within 48 hours.   Bezafibrate Preparation Products And Raw materials Raw materials 4-Chlorobenzoyl chloride-->Tyramine-->Ethyl 2-bromoisobutyrate-->Sodium