- Synthetic method of metformin hydrochloride and application thereof
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The invention belongs to the field of medicine synthesis, and discloses a synthesis method of metformin hydrochloride and an application thereof, the synthetic method comprises the following steps: dissolving dicyandiamide and dimethylamine in lower alcohol, adding sodium alkoxide, uniformly mixing, gradually raising the temperature for condensation reaction, and after the reaction is finished, adding hydrochloric acid to adjust the pH value to be acidic to obtain the metformin hydrochloride. According to the synthetic method of metformin hydrochloride, energy consumption in the reaction process is reduced, the production cost is reduced, and the purification difficulty of the product is reduced. The method is suitable for synthesizing the metformin hydrochloride, and the synthesized metformin hydrochloride is used for preparing the metformin hydrochloride sustained release tablets.
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Paragraph 0029-0047
(2021/08/14)
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- SOLVENT FREE CONTINUOUS PROCESS FOR THE SYNTHESIS OF METFORMIN HYROCHLORIDE
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The present invention provides a continuous solvent free and additive free process for the synthesis of Metformin Hydrochloride in a screw reactor. >90% conversion of the solid substrates without solvent is obtained in a screw reactor to produce Metformin Hydrochloride with at least 90% selectivity.
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Paragraph 0052; 0056
(2021/03/13)
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- PREPARATION OF METFORMIN HYDROCHLORIDE FREE FROM GENOTOXIC IMPURITY
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A high purity metformin hydrochloride, having a purity equal to or greater than 99% by area percentage of LCMS and no detectable amount of N-Nitrosodimethylamine (NDMA), wherein the LCMS method for the determination of NDMA content in Metformin hydrochloride has a Limit of detection of 0.004 ppm and a Limit of quantification of 0.009 ppm.
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- PROCESS FOR THE PREPARATION OF METFORMIN
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The present invention relates to an improved process for the preparation of metformin hydrochloride, an important drug in the first line treatment of Type II Diabetes.
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Page/Page column 11; 12
(2019/08/29)
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- Preparation method of metformin hydrochloride
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The invention relates to a preparation method of metformin hydrochloride. The preparation method comprises the following steps: utilizing diphenyl ether or HMPT as a solvent to perform the reaction, refluxing when the reaction temperature is 200 DEG C, after the reaction is ended, cleaning a product with isoamyl alcohol at 100 DEG C, re-crystallizing and refining by using ethanol, so that not onlyis the reaction time shortened, but also the satisfactory yield can be realized; and in addition, a boiling point of the used solvent is far higher than the reaction temperature, so that the over-boiling phenomenon is maximally avoided.
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Paragraph 0012-0013; 0014-0015; 0016-0017; 0018-0019
(2018/03/24)
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- IMPROVED PROCESS FOR THE PREPARATION OF HIGH PURE METFORMINE
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The present invention provided an improved process for the preparation of Metformin compound of formula I or its pharmaceutically acceptable salts 5 thereof, by employing an alcoholic solvent throughout the process
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Page/Page column 8
(2016/12/26)
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- Preparation method of metformin hydrochloride
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The invention discloses a preparation method of metformin hydrochloride. The method is characterized by including the following steps of firstly, adding dicyandiamide and dimethylamine hydrochloride in a reaction still, and adding cyclohexanol, wherein the mole ratio of dicyandiamide to dimethylamine hydrochloride is 1:1.2, and the mole ratio of cyclohexanol to dicyandiamide is 3:1; secondly, starting a stirring device, controlling the rotating speed at 45-50 r/min, regulating the vacuum degree in the reaction still to 0.08-0.09 MPa, heating the mixture to 135-145 DEG C, and preparing crude metformin hydrochloride after the reaction is conducted for 2.5 hours; thirdly, conducting recrystallization on the crude product through ethyl alcohol, and conducting filtering and drying to obtain the metformin hydrochloride. By means of the method, the reaction time is greatly shortened, the production cost is reduced, side reactions can be effectively restrained, the impurity content is reduced, and therefore the yield of the product is greatly improved.
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Paragraph 0010; 0011
(2016/11/21)
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- PROCESSES FOR PREPARING METFORMIN HYDROCHLORIDE
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A process for reducing dimethylamine content in metformin hydrochloride is disclosed. The process comprises: (a) providing metformin hydrochloride having dimethylamine content more than 15 ppm;(b) pulverizing the metformin hydrochloride;(c) slurrying the metformin hydrochloride in one or more C1-C4 alcohol solvents; and(d) isolating the metformin hydrochloride.
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Page/Page column 3-4
(2011/02/18)
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- PROCESS FOR STRAIGHTENING KERATIN FIBRES WITH A HEATING MEANS AND DENATURING AGENTS
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The invention relates to a process for straightening keratin fibres, comprising: (i) a step in which a straightening composition containing at least two denaturing agents is applied to the keratin fibres, (ii) a step in which the temperature of the keratin fibres is raised, using a heating means, to a temperature of between 110 and 250° C.
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- PROCESSES FOR PREPARING METFORMIN HYDROCHLORIDE
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A process for reducing dimethylamine content in metformin hydrochloride is disclosed. The process comprises: (a) providing metformin hydrochloride having dimethylamine content more than 15 ppm; (b) pulverizing the metformin hydrochloride; (c) slurrying the metformin hydrochloride in one or more Cj-C4 alcohol solvents; and (d) isolating the metformin hydrochloride.
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Page/Page column 8
(2010/12/31)
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- N, N- DIMETHYL IMIDODICARBONIMIDIC DIAMIDE ACETATE, METHOD FOR PRODUCING THE SAME AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
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The present invention relates to N,N -dimethyl imidodicarbonimidic diamide acetate, a method of preparing the same and a pharmaceutical composition comprising the same, and more particularly, to N,N-dimethyl imidodicarbonimidic diamide acetate which is a crystalline acid addition salt prepared by reacting N,N-dimethyl imidodicarbonimidic diamide with acetic acid, and which is very effective as a therapeutic agent for treating metabolic syndromes that glycosuria and diabetes mellitus, obesity, hyperlipidemia, fatty liver, coronary heart disease, osteoporosis, polycystic ovarian syndrome, a cancer depleted of gene P53, etc. are complexly occurred; treating diabetes mellitus and preventing its complication; and treating a cancer and preventing myalgia, muscle cell cytotoxicity and rhabdomyolysis, etc. since the acid addition salt is excellent in physicochemical properties such as solubility, stability, non-hygroscopicity, anti-adhering property, etc., and low toxicity, a method of preparing the same and a pharmaceutical composition comprising the same.
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Page/Page column 29
(2008/12/07)
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- Synthesis, crystal structure and biological properties of a new series of lipophilic s-triazines, dihydrofolate reductase inhibitors
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A number of adamantyl-group-bearing diamino-s-triazines were synthesized as potential dihydrofolate reductase (DHFR) inhibitors and their pharmacological properties were tested. The crystal structures of certain compounds were determined by X-ray crystallography. With the aid of computer graphics, model structures of the L1210 mouse DHFR-ligand ternary complex were constructed. The binding affinities of the compounds to DHFR were determined experimentally. Compounds mono-substituted at the nitrogen of the amine group appear to be slightly better inhibitors. Weak activity was also enhanced by the presence of a methylene bridge between the adamantyl group and the s-triazine ring. The majority of the compounds was shown to have weak activity against P388 and KB cell lines in vitro; some compounds showed weak anti-bacterial activity and no anti-viral activity was detected.
- Tsitsa,Antoniadou-Vyza,Hamodrakas,Eliopoulos,Tsantili-Kakoulidou,Lada-Hytiroglou,Roussakis,Chinou,Hempel,Camerman,Ottensmeyer,Vanden Berghe
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p. 149 - 158
(2007/10/02)
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- SYNTHESIS OF N-SUBSTITUTED 2,4-DIAMINO-6-ALKYL-1,3,5-TRIAZINES CONTAINING LONG ALKYL RADICALS
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N-Substituted 2,4-diamino-1,3,5-triazines containing long normal alkyl radicals were obtained by the cyclocondensation of the methyl esters of higher aliphatic acids with biguanides.
- Kelarev, V. I.,Bellul', M.,Zav'yalov, V. I.,Ammar Dibi,Golovin, A. N.,et al.
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p. 994 - 998
(2007/10/02)
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