- Synthetic method and application of pantoprazole sodium
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The invention belongs to the field of medicine synthesis, and discloses a synthesis method and application of pantoprazole sodium. The pantoprazole sodium is synthesized by the following steps: firstly carrying out sulfinylation on 5-difluoromethoxy-2-sulfenyl-1H-benzimidazole, and then carrying out Suzuki reaction on the 5-difluoromethoxy-2-sulfenyl-1H-benzimidazole and ((3, 4-dimethoxypyridine-2-yl) methyl) boric acid. According to the invention, the synthesis method of pantoprazole sodium provided by the invention can effectively improve the utilization rate of raw materials, improve the yield of intermediates and further reduce the production cost; the purification process of the synthesized intermediate and the final product in the synthesis method is simple, and the technological process is further shortened; and the synthesis method provided by the invention is suitable for synthesizing pantoprazole sodium, and the synthesized pantoprazole sodium is used for preparing a pantoprazole sodium injection.
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Paragraph 0027-0028; 0031-0034; 0037-0040; 0043-0046; ...
(2021/07/28)
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- Preparation method of pantoprazole sodium sesquihydrate single crystal form
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The invention belongs to the technical field of chemical pharmacy, and relates to a preparation method of a pantoprazole sodium sesquihydrate single crystal form. The preparation method comprises thefollowing steps: (1) adding pantoprazole sodium monohydrate and a solvent into a reaction kettle, and heating to dissolve the pantoprazole sodium monohydrate in the solvent; (2) heating the solution in the reaction kettle to 60-65 DEG C, adding pantoprazole sodium sesquihydrate seed crystals, and separating out a pantoprazole sodium sesquihydrate crystal under stirring through programmed heating and cooling; and (3) centrifuging and drying the separated pantoprazole sodium sesquihydrate crystal. The preparation method of the pantoprazole sodium sesquihydrate single crystal form is simple to operate, low in cost, suitable for large-scale production and high in crystal form purity and is used for preparing the pantoprazole sodium sesquihydrate single crystal form.
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Paragraph 0032-0034
(2020/05/05)
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- Preparation of Pantoprazole sodium method and Pantoprazole sodium (by machine translation)
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The invention relates to the preparation of Pantoprazole sodium method and pantoprazole sodium. In particular, the invention relates to a method of preparing pantoprazole sodium, comprising the following steps: 1) to 2 - hydroxymethyl - 3, 4 - dimethoxy pyridine (II) as the starting material, in under the action of chloride, the compound of formula III; 2) will be of the formula III compound in the presence of an inorganic base with 5 - difluoro - 2 - mercapto - 1 H - benzimidazole condensation, the compound of formula IV; 3) will be of the formula IV compound is oxidized by an oxidant generating 5 - difluoro - 2 - [(3, 4 - dimethoxy - 2 - pyridyl) methyl] sulfinyl - 1 H - benzimidazole is pantoprazole; 4) the obtained 5 - difluoro - 2 - [(3, 4 - dimethoxy - 2 - pyridyl) methyl] sulfinyl - 1 H - benzimidazole with sodium hydroxide reaction to produce salt that pantoprazole sodium (I); and optionally a 5) the resulting pantoprazole sodium is refined. The method of the invention said product has high purity, and the related impurities such as oxidation impurity, reducing the impurity, decomposition low impurity content. (by machine translation)
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- A pantoprazole sodium production process (by machine translation)
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Pantoprazole sodium (Pantoprazole Sodium), chemical name 5 - difluoro - 2 - [[ (3, 4 - dimethoxy - 2 - pyridyl) - methyl] sulfinyl] - 1 H - benzimidazole sodium monohydrate, is the treatment of peptic ulcer and acute gastric mucosal lesion caused by bleeding of a safe, effective drug, to peptic ulcer and reflux esophagitis have very high cure rate. For the injection of the injection by the German hectogram (Byk Gulden) the pharmaceutical Company (now renamed Takeda pharmaceutical companies) lead to the successful development of, for 1994 years 10 months in south Africa listed for the first time, tradenames for pan tuo lOOc. The present invention provides a pantoprazole sodium production process. A specific process comprises the following process: 1, pantoprazole sodium intermediate synthesis of IV; 2, pantoprazole sodium crude synthesis of V; 3, crude refined product. (by machine translation)
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Paragraph 0007; 0008; 0009
(2018/09/08)
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- Method for refining pantoprazole sodium
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The invention discloses a method for refining pantoprazole sodium. The method comprises the following steps: suspending a crude product of pantoprazole sodium in an ethanol-water mixed solution, adjusting the pH value to be 7.0-8.0 by using 1mol/L of hydrochloric acid, washing, and drying so as to obtain pantoprazole; dissolving pantoprazole into a mixed liquid of methanol and dichloromethane, dropping a sodium hydroxide-water solution, filtering a crystal, washing, and drying in vacuum, so as to obtain medicinal-grade pantoprazole sodium. The method is simple and convenient to operate, low inrefining cost and applicable to industrial amplification operation, and the prepared pantoprazole sodium is high in yield, high in purity, low in solvent residue, good in color and good in stability.
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Paragraph 0033; 0036; 0037; 0038; 0041; 0042; 0043; 0046
(2018/09/28)
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- Method for preparing high-purity razole intermediate and medicine by using green technology instead of phosgene, thionyl chloride and other toxic and harmful substances
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The invention discloses a method for preparing a high-purity razole intermediate and a medicine by using a green technology instead of phosgene, thionyl chloride and other toxic and harmful substances. The preparation method comprises the following steps: dissolving Ph3PO in an organic solvent, placing the obtained solution in a reaction bottle, dropwise adding BTC to form a high-efficiency chloration reagent, carrying out a heat insulation reaction for a period of time after the dropwise addition is finished, dissolving a razole hydroxide in the organic solvent, dropwise adding the obtained solution to the above system, carrying out a heat insulation reaction for a period of time, carrying out suction filtration, and drying the obtained dried reaction product to obtain razole chloride. In the process, the Ph3PO is equivalently regenerated, a mother liquor part is concentrated to precipitate the Ph3PO at a low temperature, and the Ph3PO can be repeatedly used after being washed with a solvent with small polarity. The method has the advantages of few side reactions, high product quality, few "three wastes" pollutions, high atomic economy, and good promotion and application prospect. The invention also provides a relevant razole medicine prepared from the razole chloride obtained through the green technology. The medicine has obviously higher purity than medicines obtained through traditional methods.
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- A adopt the particle process crystal product molecular assembly and shape optimization technique preparation of Pantoprazole sodium compound and its preparation (by machine translation)
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The invention discloses a method for the preparation of pantoprazole sodium compound, the compound is [...] particle process crystal product molecular assembly and shape optimization technique to prepare. The compound as anhydrous pantoprazole sodium, has high purity, low hygroscopicity, the impurity content is low, good stability characteristics. At the same time, the invention also discloses a kind of Pantoprazole sodium pharmaceutical composition, said pharmaceutical composition comprising the following components by weight: pantoprazole sodium (to [...] ) 40-80 parts, metal ion complexing agent 0.05-0.1 parts and pH regulator proper amount. (by machine translation)
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Paragraph 0035; 0036; 0037; 0038; 0039
(2016/11/21)
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- A process for the preparation of Pantoprazole sodium
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The invention belongs to the technical field of medicines and particularly relates to a preparation method of pantoprazole sodium. Aiming at operation of condensation, oxidization and salification by adopting a one-pot process in the prior art, a phase transfer catalyst is added into the condensation process, so that the reaction speed and yield are increased. By virtue of catalytic oxidation of hydrogen peroxide in the presence of tungstate, the selectivity of the reaction is improved and the impurities are reduced. The method provided by the invention is simple to operate, the yield and the purity of the product are improved, and the method is suitable for industrial production.
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Paragraph 0034-0036
(2017/04/08)
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- PROCESS FOR THE PREPARATION OF 2-PYRIDINYLMETHYLSULFINYL BENZIMIDAZOLES, THEIR ANALOGS AND OPTICALLY ACTIVE ENANTIOMERS
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The present invention provides a commercially viable, cost effective and energy efficient process for the preparation of 2-pyridinylmethylsulfinyl benzimidazoles, their analogs and optically active enantiomers or pharmaceutically acceptable salts, hydrates or solvates thereof in high purity via application of reactors such as plug flow reactor, microreactor, microfluidic flow reactor, tubular flow reactor, coil-type flow reactor, laminar flow reactor, packed bed reactor, fluidized bed reactor or fixed bed reactor.
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Page/Page column 18; 19
(2013/07/31)
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- PROCESS FOR THE PREPARATION OF PANTOPRAZOLE SODIUM AND PANTOPRAZOLE SODIUM SESQUIHYDRATE
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The present invention relates to a process for the preparation of pantoprazol sodium sesquihydrate of formula (I) and pantoprazole sodium.
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Page/Page column 4
(2010/08/22)
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- PROCESS FOR THE PREPARATION OF PANTOPRAZOLE SODIUM
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Disclosed herein the improved and industrially viable process for the preparation of pantoprazole sodium in high yields and purity.
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Page/Page column 8
(2009/06/27)
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- Process for preparing 2-sulfinyl-1H-benzimidazoles
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The present invention relates to a process for preparing 2-(2-pyridinylmethylsulfinyl)-1H-benzimidazoles by oxidizing a thioether precursor in the presence of trifluoroethanol.
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Page/Page column 10-11
(2009/04/23)
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- PROCESS FOR PREPARING PANTOPRAZOLE SODIUM SESQUIHYDRATE
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Disclosed herein is a process for preparation of pantoprazole sodium sesquihydrate represented by Formula 1 from pantoprazole as a starting material.
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Page/Page column 5
(2009/07/17)
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- PROCESS FOR THE PREPARATION OP PANTOPRAZOLE SODIUM AND PANTOPRAZOLE SODIUM SESQUIHYDRATE
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The present invention relates to a process for the preparation of pantoprazol sodium sesquihydrate of formula (I) and pantoprazole sodium.
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Page/Page column 11
(2009/03/07)
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- PROCESS FOR PREPARATION OF PYRIDINYLMETHYLSULPHINYL BENZIMIDAZOLE COMPOUNDS AND PYRIDINE INTERMEDIATES
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Process for preparing 4-chloro-substituted pyridine intermediates of Formula (I), useful for preparation of pyridinylmethylsulphinyl benzimidazole compounds, especially Rabeprazole is disclosed herein. The invention, further describes process for preparation of stable Rabeprazole sodium of high purity in a reproducible and consistent manner.
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Page/Page column 16
(2009/10/22)
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- A PROCESS FOR THE PREPARATION OF BENZIMIDAZOLE DERIVATIVES AND THEIR SALTS
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The present relates to a process for the preparation of 2-(2-pyridylmethyl) sulfinyl-1H-benzimidazole derivatives and their pharmaceutically acceptable salts substantially free from their sulfide and the sulfone impurities.
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Page/Page column 27-28
(2008/06/13)
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- AN IMPROVED PROCESS FOR PREPARING OF, IMPURITIES FREE, SUBSTITUTED 2-BENZIMIDAZOLESULFOXIDE COMPOUND
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The present invention relates to an improved process for the preparation of pantoprazole free from overoxidation impurities. The process enables better control of the process and therefore the quality fo the products obtained, avoiding the formation of impurities.
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Page/Page column 16; 17; 18
(2008/06/13)
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- PROCESS
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A one-pot process for the preparation of pantoprazole sodium by reacting 2-chloro methyl 3, 4 - dimethoxy pyridine hydrochloride with 2-mercapto-5-difluoromethoxy benzimidazole in an organic solvent system in presence of a phase transfer catalyst and further treating with aqueous sodium hypohalite solution comprising sodium hydroxide to obtain pantoprazole sodium in high yield and purity. The process for conversion of pantoprazole sodium to pantoprazole sodium sesquihydrate and also pantoprazole sodium monohydrate are also disclosed herein.
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Page/Page column 8; 10-11
(2010/11/08)
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- A process for the preparation of pantoprazole and salts thereof
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A process for the preparation of pantoprazole and the salts thereof, comprising the reaction of a mercaptoimidazole with a picoline, to give a 2-pyridinyl-methylsulfinyl-2-benzimidazole intermediate, the oxidation thereof with ε-phthalimidoperhexanoic acid and the subsequent methoxylation.
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Page/Page column 5-6
(2010/02/11)
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- Process for the preparation of pantoprazole and salts thereof
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A process for the preparation of pantoprazole and the salts thereof, comprising the reaction of a mercaptoimidazole with a picoline, to give a 2-pyridinyl-methylsulfinyl-2-benzimidazole intermediate, the oxidation thereof with ε-phthalimidoperhexanoic acid and the subsequent methoxylation.
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Page/Page column 4
(2010/02/11)
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- PYRIDINE BENZIMIDAZOLE SULFOXIDES WITH HIGH PURITY
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A method for preparing a pyridine benzimidazole sulfoxide compound having the formula (I) with the step of oxidizing a pyridine benzimidazole thioether compound with an oxidation agent, during that oxidation step a pyridine benzimidazole sulfone compound is formed as an undesired by-product. It is proposed to stop the oxidation step prior the amount of undesired pyridine benzimidazole sulfone product exceeds 1,0 %-by weight based on the entire amounts of compounds.
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Page/Page column 19-20
(2008/06/13)
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- NOVEL POLYMORPHS OF PANTOPRAZOLE SODIUM
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The present invention relates to novel polymorphs of pantoprazole sodium, to processes for their preparation and to pharmaceutical compositions containing them.
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- NEW SOLID-STATE FORMS OF 5-(DIFLUOROMETHOXY)-2-[[3,4-DIMETHOXY-2-PYRIDINYL)METHYL]SULFINYL]-1H-BENZIMIDAZOLE SODIUM AQUA COMPLEXES
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The present disclosure relates to new solid-state forms of 5-(difluoromethoxy)--2-[[(3,4-dimethoxy-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole sodium aqua complexes, and to processes for their preparation. The disclosure is also directed to pharmaceutical compositions containing the solid-state forms, and the methods of treatment using the solid-state forms.
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- PROCESS FOR PREPARING 2-[(PYRIDINYL)METHYL]SULFINYL-SUBSTITUTED BENZIMIDAZOLES AND NOVEL CHLORINATED DERIVATIVES OF PANTOPRAZOLE
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The present invention provides a process comprising admixing a thioether with about 1.05 to about 1.6 molar equivalents of an active chlorine-containing oxidant, preferably sodium hypochlorite, and about 2.5 to about 5.0 molar equivalents of an alkali metal base; and recovering a sulfoxide that is preferably pantoprazole, lansoprazole, omeprazole, or rabeprazole. The process may further comprise contacting the sulfoxide with a source of sodium ions, preferably sodium hydroxide, to produce the sodium salt of the sulfoxide. The invention also relates to novel chlorinated derivatives of pantoprazole including 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)-chloromethyl]sulfinyl]-1H- benzimidazole and 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)-chlorohydroxymethyl] sulfinyl]-1H-benzimidazole and processes for making them. The invention also relates to processes of quantifying and identifying a compound other than pantoprazole in a mixture of pantoprazole and at least one other compound.
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- SOLID STATES OF PANTOPRAZOLE SODIUM, PROCESSES FOR PREPARING THEM AND PROCESSES FOR PREPARING KNOWN PANTOPRAZOLE SODIUM HYDRATES
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Crystalline pantoprazole sodium Forms II, IV, V, VI, VIII, IX, X, XI, XII, XIII, XIV, XV, XVI, XVII, XVIII, XIX and XX; pantoprazole sodium solvates containing water, acetone, butanol, methylethylketone, dimethylcarbonate, propanol and 2-methylpropanol; and amorphous pantoprazole sodium are disclosed.
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