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LIST of PRODUCTS BULK DRUGS Sl. No Name of the Product Production TPM 1. Carvedilol Phosphate 2.50 2. Citalopram Hydrobromide 10

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LIST OF PRODUCTS BULK DRUGS Sl. No Name of the product Production TPM 1. Carvedilol phosphate 2.50 2. Citalopram Hydrobromide 10.00 3. Closantel sodium 5.00 4. Esomeprazole magnesium trihydrate 1.50 5. Fexofinadine hydrochloride 2.00 6. Fosfomycin trometamol 3.00 7. Gaba-pentin 3.00 8. Itraconozole 2.00 9. Lansoprazole 3.00 10. Lornoxicam 4.00 11. Montelukast sodium 3.00 12. Omeprazole 5.00 13. Ondansetron 3.00 14. Oxyclozanide 5.00 15. Ritonavir 3.00 16. Rosuvastatin calcium 3.00 17. Setraline hydrochloride 2.00 18. Sparfloxacin 2.00 19. Terbinafine hydrochloride 3.00 Total 65.00 INTERMEDIATES Sl. No Name of the product Production TPM 1 Tri Chloro Salisylic Acid 3.00 2 5-AminO-2-Hydroxy Benzoic acid 2.00 3 5-Amino-2-dibenzylamino-1,6-diphenyl-hex-4-en-3-one 2.00 4 2-Amino-6-chloro-3-nitro pyridine 3.00 5 4-Chloro butyryl chloride 3.00 CHEMICALS Sl.No Name of the product Production TPM 1 Tributyl Tin chloride 90 2 L-Menthol 90 3 Dicyclo Hexylcarbomidiimide 90 SOLVENT RECOVERY Sl.No Name of the product Production TPM 1 All solvents 450 Industry proposes to produce • 2.0 TPD either from bulk drug group or intermediate group • 3.0 TPD from chemicals group • 15.0 TPD solvent recovery CARVEDILOL PHOSPHATE Carvedilol Phosphate can be manufactured in four stages. Stage-1: 1-(2-bromo ethoxy)-2-methoxy benzene and benzyl amine reacts together in the presence of toluene solvent medium forms stage-1 compound. O Toluene Br + NH2 O 1-(2-Bromo-ethoxy)- 2-methoxy-benzene Benzylamine C9H11BrO2 C7H9N Mol. Wt.: 231.1 Mol. Wt.: 107 O NH HBr + O Stage-1 Hydrobromic acid C16H19NO2 Mol.Wt.:81 Mol.Wt.:257 Stage-2: Statge-1 compound reacts with 2-chloro ethyl-oxirane in the presence of methanol solvent medium forms the stag-2 compound. O Cl N O OH NH + Cl O Methanol O O Stage-2 Stage-1 2-Chloromethyl-oxirane C H ClNO C16H19NO2 C3H5ClO 19 24 3 Mol. Wt.: 257 Mol. Wt.: 92 Mol. Wt.: 349.8 Stage-3: Stage-2 compound reacts with 9H-carbazol-4-ol in the presence of potassium carbonate forms the stage-3 compound. OH O K CO Cl N 2 3 OH + O N H Stage-2 9H-Carbazol-4-ol C H NO C19H24ClNO3 12 9 Mol. Wt.: 349.8 Mol. Wt.: 183 O O N OH O HCl + N H Hydrochloric Stage-3 acid C31H32N2O4 Mol.Wt.:36.5 Mol. Wt.: 496.6 Stage-4: Stage-3 compound undergoes reduction in the presence of H2; Pd/C forms the carvedilol free base. O O N H2, Pd/C OH + H2 O N Stage-3 H Hydrogen C31H32N2O4 Mol. Wt.: 496.6 Mol. Wt.: 2 O O NH OH CH3 O + N H Toluene Carvedilol free base C7H8 C24H26N2O4 Mol. Wt.: 92 Mol. Wt.: 406.5 Stage-5: Carvedilol free base reacts with phosphoric acid and water forms carvedilol phosphate. The reaction proceeds as per the below equation. O O NH OH OH H2O + OH P OH +1/2 HO O 2 O NH Carvedilol free base Phosphoric acid Water C24H26N2O4 H3O4P Mol. Wt.: 406.5 Mol. Wt.: 98 Mol.Wt.: 9 O O NH OH CH3 O . H3PO4 .1/2 H2O Carvedilol phosphate C25H30NO8P Mol. Wt.: 513.5 FLOW CHART OF CARVEDILOL PHOSPHATE Stage-1 1-(2-bromo ethoxy)-2-methoxy benzene benzyl amine Reactor Spent toluene to recovery Toluene Centrifuge Layer Seperator Forms hydrobromic acid Stage-1 Stage-2 stage-1 product 2-chloro ethyl-oxirane Reactor Spent methanol to recovery Methanol Centrifuge Stage-2 Stage-3 Stage-2 9H-carbazol-4-ol Reactor HCl gas to scrubbing Potassium carbonate Centrifuge Layer separation Stage-3 Stage-4 Stage-3 comound Reactor Toluene to recovery H2, Pd/C Centrifuge Layer separation Cavedilol free base Stage-5 Carvedilol free base Phosphoric acid Reactor Water Centrifuge Waste water to recovery Distillation Pharma CITALOPRAM HYDROBROMIDE The product is manufactured in three stages. Stage-1: 4-[4-Dimethylamino-1-(4-fluoro-phenyl)-1-hydroxy-butyl]-3-hydroxymethyl-benzonitrile on Cyclisation in presence of Phosphoric acid and Ammonia solution produces stages-1 product. F F CH3 CH3 N Phosphoric acid + .H O OH N 2 CH3 Liq.Ammonia,Toluene O OH CH NC NC 3 4-[4-Dimethylamino-1-(4-fluoro-phenyl)- 1-hydroxy-butyl]-3-hydroxymethyl-benzonitrile Stage-1 Water C H FN O C20H23FN2O2 20 22 2 Mol. Wt.: 18 Mol. Wt.: 342 Mol. Wt.: 324.4 Stage-2: Citalopram Hydro bromide is produced when stage-1 compound reacts with Hydrobromic acid . Isopropyl alcohol, Carbon and Di isopropyl ether is used in the process. F F CH3 IPA CH3 N + HBr O N CH3 O CH3 NC NC HBr Stage-1 Hydro bromicacid Citalopram Hydrobromide C20H22FN2O BrH C20H22BrFN2O Mol. Wt.: 324.4 Mol. Wt.: 80.9 Mol. Wt.: 405.3 FLOW CHART OF CITALOPRAM HYDROBROMIDE Stage-1 4-[4-Dimethylamino-1-(4-fluoro-phenyl)- 1-hydroxy-butyl]-3-hydroxymethyl-benzonitrile Phosphoric acid Reactor Toluene to recovery Liq.Ammonia,Toluene Water Centrifuge Ammonium phosphate salt solution for sale Stage-1 Stage-2:Pharma Stage-1 Hydrobromic acid Spent solvent to recovery Di Isopropyl ether Reactor Iospropyl alcohol Centrifuge Di Isopropyl ether Stage-Pharma CLOSANTEL SODIUM The product is manufactured in three stages. Stage-1: Step-A: Sodium bicarbonate and Sodium sulphide react together in presence of water to produce Sodium hydrogen sulphide Water NaHS + Na2CO3 NaHCO3 + Na2S Sodium Sodium Sodiumhydrogen Sodium bicarbonate sulphide sulphide Carbonate Mol. Wt.: 84 Mol.Wt.:78 Mol. Wt.: 56 Mol.Wt.:106 Step-B: This mass is made to react with 1-chloro-3-methyl-5-nitro benzene and p-Chloro Benzyl cyanide in presence of toluene solvent medium and water to produce the stage-1 compound. Cl Cl Cl CN –O Cl N Toluene N+ + + O NaHS H2N 2 O CH3 CH3 1-Chloro-3-methyl parachloro -5-nitro-benzene benzyl cyanide Stage-1 Oxygen O C7H6ClNO2 C8H6ClN C15H12Cl2N2 2 Mol. Wt.: 171.6 Mol. Wt.: 151.6 Mol. Wt.: 291.2 Mol. Wt.: 32 Stage-2: Stage-1 on reaction with 2-Hydroxy-3, 5-diiodo-benzoicacid by means of phosphorous trichloride in presence of toluene solvent medium and water to form the stage-2 compound Cl OH O I Cl CN OH Toluene/PCl + 3 Water H2N I CH3 2-Hydroxy-3,5-diiodo Stage-1 -benzoic acid C15H12Cl2N2 C7H4I2O3 Mol. Wt.: 291.2 Mol. Wt.: 389.9 OH O Cl C N I NH CH Cl H2O + I CH3 Water Closantel C22H14Cl2I2N2O2 Mol. Wt.: 18 Mol. Wt.: 663.1 Stage-3: Stage-2 compound with Formic acid and Sodium Hydroxide in Water and Acetone OH O Cl C N I OH NaOH NH CH Cl + + O I CH3 Closantel Formic acid Sodium Hydroxide C22H14Cl2I2N2O2 CH2O2 Mol. Wt.: 663.1 Mol. Wt.: 46 Mol. Wt.: 40 I CH 3 Water + I NH Cl H2O O Acetone OH O O- Na+ Cl N Water Closantel Sodium C23H15Cl2I2N2NaO4 Mol. Wt.: 18 Mol. Wt.: 731.1 FLOW CHART OF CLOSANTEL SODIUM Stage-1 Sodiumbicarbonate Sodium Sulphide Reactor Inorganic salt solution to waste Water 1-chloro3-methyl-2-nitro benzene parachlorobenzyl cyanide Tolouene to recovery Reactor Sodium Hydrogen Sulfide O2 gas to scrubbing Toluene Centrifuge Stage-1 Stage-2: Stage-1 2-Hydroxy-3,5-diiodo-benzoic acid Toluene Reactor Toluene to recovery Phosphorus tri chloride water Centrifuge Inorganic salt solution to waste Stage-2 Stage-3: Closantel Formic acid Sodium Hydroxide Reactor Acetone to recovery Water Acetone Centrifuge Water to waste Final compound ESOMEPRAZOLE MAGNESIUM TRIHYDRATE The product is produced in two stages. Stage-1: 5-Methoxy-2-(4-methoxy-3, 5-dimethyl-pyridin-2-yl-methyl sulfanyl)-1H-benzoimidazole reacts with cumene hydro peroxide and potassium Hydroxide by means of titanium isopropoxide in presence of Methylene dichloride solvent medium to form the stage-1 product. O H O N NH Titanium S isoperoxide + + KOH O N O MDC 5-Methoxy-2-(4-methoxy-3,5-dimethyl-pyridin-2- ylmethylsulfanyl)-1H-benzoimidazole cumene hydroperoxide Potassium C17H19N3O2S C9H12O2 Hydroxide Mol. Wt.: 329.4 Mol. Wt.: 152.2 Mol. Wt.: 56.1 O N OH N CH3 S + H O + N CH3 O 2 O O K Phenyl-acetic acid Esomeprazole Potassium Water C8H8O2 C17H18KN3O3S Mol.Wt.:18 Mol. Wt.: 136.2 Mol. Wt.: 383.5 Stage-2: Stage-1 compound on reaction with Magnesium Chloride solution in presence of acetone solvent medium to form the final compound N N CH3 Acetone 2 + Mg.Cl + 3 H O S 2 2 N O O O CH3 K Esomeprazole Potassium Magnesium Water C34H36N6O6S2K2 Chloride H6O3 Mol. Wt.: 767 Mol. Wt.: 95 Mol. Wt.: 54 O O N S N N O Mg O N N S 2 KCl + N O O H O H2O H2O 2 Potassium Chloride Cl2K2 Esomeprazole Magnesium trihydrate Mol. Wt.: 149 C34H42MgN6O9S2 Mol. Wt.: 767.2 FLOW CHART OF ESOMEPRAZOLE MAGNESIUM TRIHYDRATE Stage-1: 5-Methoxy-2-(4-methoxy-3, 5-dimethyl- pyridin-2-yl-methyl sulfanyl)-1H-benzoimidazole Cumene hydro peroxide Potassium hydroxide Reactor Solvent Mls Titanium isopropoxide Methylene Dichloride Centrifuge Water to waste Layer separator Phenyl acetic acid Stage-1 Stage-2: Stage-1 Magnesium Chloride Reactor Water Acetone to recovery Acetone Centrifuge Inorganic salt solution to waste Pharma FEXOFINADINE HYDROCHLORIDE The product is produced in three stages. Stage-1: 2-[4-(4-Chloro-butyryl)-phenyl]-2-methyl-propionic acid methyl ester undergoes condensation with Azacyclonol and Sodium Bicarbonate by means of Methyl isobutyl ketone in presence of Ethyl alcohol solvent medium to form the stage-1 compound.
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  • [(4-Chlorophenyl) Sulfanyl] Ethoxy- 3-Methoxy-5-[5-(3,4,5-Trimethoxyphenyl)-2-Furyl]Benzonitrile

    [(4-Chlorophenyl) Sulfanyl] Ethoxy- 3-Methoxy-5-[5-(3,4,5-Trimethoxyphenyl)-2-Furyl]Benzonitrile

    Available online a t www.derpharmachemica.com Scholars Research Library Der Pharma Chemica, 2015, 7(3):242-247 (http://derpharmachemica.com/archive.html) ISSN 0975-413X CODEN (USA): PCHHAX Synthesis and antibacterial activity of 2-2-[(4-chlorophenyl) sulfanyl] ethoxy- 3-methoxy-5-[5-(3,4,5-trimethoxyphenyl)-2-furyl]benzonitrile P. Veerabhadra Swamy*a,b , K. B. Chandrasekhar c and Pullaiah China Kambhampati a aLaxai Avanti Life Sciences, Lab#9, ICICI Knowledge park, Shameerpet, Turkapally Village, Hyderabad bDepartment of Chemistry, Jawaharlal Nehru Technological University, Hyderabad, Hyderabad, Telengana, India cDepartment of Chemistry, Jawaharlal Nehru Technological University, Anantapur, Anantapuramu, A.P., India _____________________________________________________________________________________________ ABSTRACT The present paper describes the synthesis and of (2-(4-chlorophenylthio)ethoxy)-3-methoxy-5-(5-(3,4,5- trimethoxyphenyl)furan-2-yl)benzonitrile from commercially available vanillin and 3,4,5-trimethoxy acetophenone as starting materials utilizing green reagents and solvents. The antibacterial test results indicated that the title compound displayed excellent activity against both Gram-positive bacteria (Staphylococcus aureus and Bacillus cereus) and Gram-negative bacteria: (Escherichia Coli and Pseudomonas aeruginosa). Keywords: Antibacterial activity, Furan, 3,4,5-trimethoxy acetophenone, vanillin, synthesis _____________________________________________________________________________________________ INTRODUCTION Furan derivatives
  • Studies on Isotope Separation of Lithium by Electromigration in Fused Lithium Bromide and Potassium Bromide Mixture, (II) Composition of Salt in Anode Compartment

    Studies on Isotope Separation of Lithium by Electromigration in Fused Lithium Bromide and Potassium Bromide Mixture, (II) Composition of Salt in Anode Compartment

    Journal of NUCLEARSCIENCE and TECHNOLOGY,7 (10), p. 522~526 (October 1970). Studies on Isotope Separation of Lithium by Electromigration in Fused Lithium Bromide and Potassium Bromide Mixture, (II) Composition of Salt in Anode Compartment Yoshinobu YAMAMURA* and Shin SUZUKI* Received May 13, 1970 Accurate knowledge on the salt composition in the anode compartment is indispensable when 6Li is to be highly enriched by electromigration in fused LiBr-KBr mixture. A study was made on the dependence on temperature shown by the salt composition in the anode com- partment. It was observed that sustained electromigration led to a salt composition in the anode compartment that was determined by the prevailing temperature. The composition was observed for various temperatures between 380- and 740-C: In terms of the ratio Li/K in chemical equivalent, the values were 1.31 at 380-C, 1.29 at 420-C, 1.31 at 460-C, 1.41 at 500-C, 1.76 at 540-C, 1.82 at 580-C, 1.95 at 620-C, 2.16 at 680-C and 2.34 at 740-C. These results can be explained by assuming that the fused LiBr-KBr mixture is a system composed of two simple salts and their eutectic, and that at temperatures below 550-C, which is the melting point of LiBr, LiBr and KBr are dissolved in fused eutectic, while KBr is dissolved in the fused eutectic and LiBr at temperatures between 550- and 738-C, which latter is the melting point of KBr. I. INTRODUCTION . EXPERIMENTAL In a previous study(1), one of authors suc- 1.