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Recent inventory of green synthesis of telmisartan pharmaceutical innovation process by srf regherh





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Recent inventory of green synthesis of telmisartan pharmaceutical innovation process by
Article Posted: 06/11/2011
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Recent inventory of green synthesis of telmisartan pharmaceutical innovation process


 
Business,Business News,Business Opportunities
Synthesis of Quinapril hydrochloride Quinapril hydrochloride synthesis route are many advantages and disadvantages. Not long ago, Qingdao University of Science and Technology Chemical industry Institute of Lin-Sheng Tang and other scientific and technical personnel through trial and error, put forward a synthesis of Quinapril hydrochloride new process: first use of acetophenone, glyoxylic acid and ethanol, "pot" was prepared 3 - benzoyl ethyl acrylate ( As the "pot" so that operation becomes simplified); in the next Quinapril hydrochloride preparation, the previously used expensive synthesis of the Pt / C as catalyst and longer reaction time (about 3) , the new technology to 10% Pd / C, supplemented by a small amount of the compound NiB/SiO2 amorphous alloy catalyst, the composite catalyst of lower prices, at 35 for 10 hours when the hydrogenation reaction can yield up to 72.9 %.

Each step of the process on the reaction conditions and solvents were also optimized, improved process yield of 22% of the total. Green Synthesis of Telmisartan

Telmisartan recent clinical application of our growing. Telmisartan high cost of foreign production processes do not meet the conditions of our country, most recently, Zhengzhou Institute of Light Industry Chengchuan Ling and other researchers through trial and error, combined with the actual situation of China's raw material supply and production of the actual test conditions, telmisartan Improved synthetic route is optimized.

New technology used in organic synthesis in recent years, widely used international green synthetic methods, using ionic liquids (tetrahydro borate or hexafluorophosphate available) of this new environment-friendly reaction media to replace the original Process greater toxicity of methanol as the reaction medium, so that the optimized route reactant, simple, high yield, high product concentration (up to 99.96%), organic solvent residues in small, environmentally friendly, suitable for industrial production, per kg API Lower than the cost of more than 2000 yuan overseas.

Specific synthesis methods are: in the ionic liquid [bmim] BF4 in a 3 - methyl -4 - nitrophenyl methyl was synthesized by esterification, reduction, acylation, nitration, reduction, cyclization , condensation, hydrolysis was 2 - n-propyl -4 - methyl -6 - carboxy-benzo Imidazole In polyphosphoric acid N-methyl-under and condensation of o-phenylenediamine, the resulting product and then with 4 - bromomethyl biphenyl -2 - carboxy methyl ester condensation, hydrolysis, ultimately, telmisartan, the yield 93.8%, 65.8% of total production rate of more than the quality of refined products in the HPLC fraction up to 99.96%.

Chitosan production by Aspergillus niger Present, the industrial production of chitosan is usually from the shrimp, crab shell extract, but the shrimp and crab are the source of all factors. In recent years, people began to study chitosan extracted from filamentous fungi, but this research is still in research stage.

Hunan Institute of Chemical Technology Department of Chemical Engineering Ho-ho-yin and other research personnel to Aspergillus niger fermentation of chitosan, and orthogonal in-depth study by Aspergillus niger fermentation by chitosan conditions to optimize the culture medium and fermentation process, to determine the best culture medium: corn steep liquor 3%, 3% glucose, magnesium sulfate 1.0%, 0.01% ammonium dihydrogen phosphate, potassium dihydrogen phosphate 0.005%; optimum fermentation time was 90 hours, shaking speed 180r / min, pH 6, fermentation temperature 30 . The optimum cell dry weight under the 51.52mg/mL, use of acid-base extraction of chitosan, the deacetylation degree up to 78.09%. Synthesis of -artemether

-artemether antimalarial drug of choice recommended by the World Health Organization, with quick, low toxicity characteristics, its antimalarial activity is Artemisinin 6 times, and because of its greater solubility in oil, it is particularly suitable for preparing formulations. Now, at home and abroad on the physical and chemical properties of -artemether, pharmacological research and clinical applications of more, for the synthesis of -artemether less, few papers reported the yield of -artemether is also Only about 60%, and only in the laboratory synthesis.

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