cas 117976-90-6, Rebeprazole sodium | Articles data

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A right-handed thunder beira zuozuo sodium hydrate crystal form and its preparation method
The invention relates to a novel crystal form of rabeprazole sodium aquo-complex and a preparation method of the novel crystal form. The novel crystal form is called the Z-type crystal. The Z-type crystal of the rabeprazole sodium aquo-complex is characterized in that in the X-ray powder diffraction pattern expressed by Cu-K alpha radiation and a 2theta+/-0.2DEG diffraction angle, the Z-type crystal has characteristic diffraction peaks at 9.3, 10.7, 18.2, 19.6, 21.2, 23.0, 27.2 and 29.9.
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Paragraph 0054-0055

(2019/01/16)

Preparation method for key intermediate rabeprazole thioether
The invention discloses a preparation method for rabeprazole thioether 2-[[[4-(3- methoxypropoxy)-3-methylpyridin-2-yl] methyl] sulfo]-1H-benzimidazole. By using Mitsunobu reaction, the rabeprazole thioether is prepared from rabeprazole oxhydryl in one-step synthesis way without chlorination reaction. In the reaction process, the high-corrosive chloride agent, such as, thionyl chloride, is not used, so that the violent corrosion of the reaction to the device is obviously reduced, and meanwhile, the reaction yield is obviously increased due to the shortened reaction step. According to the invention, the process is simple, the reaction condition is mild, the corrosion to the device is small, the yield is higher (70%-80%) and the method is suitable for industrial production.
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(2017/07/12)

Method for preparing optically-pure Rabeprazole
The invention discloses a method for preparing optically-pure Rabeprazole. The method is used for preparing a chiral 2-[[4-(3-methoxypropoxy)-3-methylpyrid-2-yl]methylsulfinyl]-1H-benzimidazole compound (Rabeprazole), which is present in a single-enantiomer form or rich-enantiomer form, in an enantioselective manner. The same effects, i.e., identical enantioselectivity and conversion ratio can be achieved through complexing a tartaric acid diamide ligand and titanium and adding an organic-base additive or not in the presence of water. The invention further provides a method for preparing a sodium salt from the obtained Rabeprazole.
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Paragraph 0077; 0078; 0079; 0080

(2017/08/28)

Rabeprazole sodium crystal method for the preparation of compounds
The invention relates to the field of medicine production and in particular relates to a preparation method of a rabeprazole sodium crystal type compound. The preparation method of the rabeprazole sodium crystal type compound comprises the following steps of: by taking 2-mercapto benzimidazole and 2-chloromethyl-3-methyl-4-methoxy propoxy pyridine hydrochloride as raw materials and carrying out a condensation reaction to prepare rabeprazole thioether, and subsequently carrying out an oxidation reaction via the rabeprazole thioether and carrying out salt forming reaction via rabeprazole and sodium hydroxide to acquire the rabeprazole sodium. According to the preparation method of the rabeprazole sodium crystal type compound, the raw materials are low in cost and easy to purchase; samples are basically invariant in related substances and contents under the condition with high temperature and high humidity; the articles are stable in property and low in overall manufacturing cost; and the preparation method of the rabeprazole sodium crystal type compound has the advantages of strictly controlling the temperatures in the steps, being less in by-products, high in yield and non-toxic, and also has the advantages of being short in production period and further improving the production efficiency.
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Paragraph 0033-0036

(2017/05/06)

A process for the preparation of sodium rebeilazole for
The invention provides a preparation method of sodium rabeprazole. The preparation method comprises the following four steps of (1) adding rabeprazole into a mixed solvent of 2-fluoro-3-chloro-5-trifluoromethyl pyridines and ethanol, and regulating the temperature at 35-40 DEG C; (2) adding anhydrous sodium carbonate and anhydrous sodium sulfate into a reaction solution until the pH value of the reaction solution is 8.0-10.0, keeping the temperature at 35-40 DEG C, and reacting for 2h under stirring; (3) continuing to add n-hexane, and reacting at the temperature of 35-40 DEG C for 2h under stirring; and (4) carrying out solid-liquid separation, and drying at reduced pressure to obtain sodium rabeprazole. The method is simple in process, and sodium rabeprazole is high in purity, low in water content and good in stability.
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Paragraph 0021; 0022

(2016/10/07)

A right-handed sodium rebeilazole for method for the synthesis of
The invention relates to a method for synthesizing rabeprazole sodium. The method comprises the following steps: performing asymmetric oxidation on raw materials with cumyl hydroperoxide, extracting through a sodium hydroxide solution, neutralizing to the pH value of 9.7 by using acid, separating out high-purity white rabeprazole sodium solids, filtering without drying, directly adding a wet sample into a mixed system of sodium hydroxide and dichloromethane and alkane solvent while stirring for reacting at the temperature of 0-30 DEG C for 3-5 hours, filtering, and drying, thereby obtaining the white rabeprazole sodium solids. According to the method disclosed by the invention, the operating steps are simplified, the yield is improved, the rabeprazole is prevented from being dried and heated, unknown impurities generated by heat instability are reduced, and use of an organic solvent is reduced.
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Paragraph 0039-0040

(2017/04/11)

PROCESS FOR THE PREPARATION OF RABEPRAZOLE
The present invention provides a compound of Formula III, process of its preparation and its use as a reference marker or as a reference standard. The present invention further provides a process for the preparation of rabeprazole, a salt or a solvate thereof. The invention also provides a chromatographic method for testing the purity of rabeprazole, a salt or a solvate thereof.
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(2014/07/07)

PROCESS FOR THE PREPARATION OF 2-PYRIDINYLMETHYLSULFINYL BENZIMIDAZOLES, THEIR ANALOGS AND OPTICALLY ACTIVE ENANTIOMERS
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 20; 21

(2013/07/31)

PROCESS FOR OBTAINING AMORPHOUS RABEPRAZOLE SODIUM
The present invention relates to a new process for obtaining the amorphous form of rabeprazole sodium salt from the acetone solvate of said salt by means of the treatment in a solvent system formed by a C6-C8 alkane and water, and to the use of said process for obtaining rabeprazole sodium salt from the acetone solvate thereof.
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Page/Page column 14; 15

(2012/11/13)

A PROCESS FOR THE PREPARATION OF AMORPHOUS FORM OF RABEPRAZOLE SODIUM
The present invention relates to a process for the preparation of amorphous form of Rabeprazole sodium of formula (I).
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Page/Page column 4; 5

(2011/02/24)

NEW CRYSTALLINE FORMS OF RABEPRAZOLE SODIUM
The present invention relates to crystalline forms of rabeprazole sodium and processes for their preparation. The invention also relates to pharmaceutical compositions comprising rabeprazole sodium.
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Page/Page column 19

(2010/04/03)

PROCESS FOR PURIFICATION OF RABEPRAZOLE SODIUM
There is provided a process for preparing amorphous rabeprazole sodium. Thus, for example, sodium hydroxide was dissolved in methanol. Rabeprazole was added to the solution and stirred at 25 - 35°C for 1 hour. Methanol was distilled off from the reaction mass, dichloromethane was added to the residual mass and the contents were stirred to obtain solution. The solution was added to cyclohexane. The contents were stirred at 25 - 35°C for 30 minutes, centrifuged the material and washed at 60 - 65°C to obtain amorphous rabeprazole sodium.
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Page/Page column 3-4

(2010/04/03)

Process for the preparation of pyridine-methylsulfinyl compounds
A process for the preparation of a compound of formula (I), or a salt thereof, wherein Q is ═CR8— or ═N—; and R1-R8 are as herein defined; comprising the reaction of a compound of formula (II), or a salt thereof, wherein Q, R1-R7 are as herein defined; with a reducing agent selected from a trivalent phosphorous compound, an oxidizable solvent and a sulfonic acid chloride; and, if desired, the conversion of a compound of formula (I) to another compound of formula (I) or a salt thereof.
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Page/Page column 5-6

(2009/04/24)

An improved process for the production of rabeprazole sodium substantially free from the impurities
The present work details the journey towards development of a simple and cost-viable process for large-scale synthesis of rabeprazole sodium substantially free from the impurities. The detailed study of different parameters affecting the quality and yield percentage of the compound has been presented. Yield is increased from 40% (reported process) to 75% with the improved process at sulfoxidation stage.
Reddy, Pingili Ramchandra,Himabindu, Vurimidi,Jaydeepkumar, Lilakar,Reddy, Ganta Madhusudhan,Kumar, Jonnalagadda Vijaya,Reddy, Ghanta Mahesh
experimental part
p. 896 - 899
(2010/04/22)

PROCESS FOR PREPARATION OF PYRIDINYLMETHYLSULPHINYL BENZIMIDAZOLE COMPOUNDS AND PYRIDINE INTERMEDIATES
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 15-16

(2009/10/22)

Synthesis of metabolites and related substances of rabeprazole, an anti-ulcerative drug
Rabeprazole sodium (Aciphex) is a gastric proton pump inhibitor used for the prevention and treatment of gastric acid-related diseases. During the synthesis of bulk drug of rabeprazole sodium, we have observed metabolites rabeprazole sulfide and rabeprazole sulfone and related substances rabeprazole-N-oxide, rabeprazole sulfone-N-oxide, N-aralkyl rabeprazole, chloro rabeprazole, and methoxy rabeprazole as impurities in the drug substance. The present work describes the synthesis and characterization of these compounds. Copyright Taylor & Francis Group, LLC.
Reddy, Ganta Madhusudhan,Mukkanti, Kaga,Bhaskar, Boluggodu Vijaya,Reddy, Padi Pratap
scheme or table
p. 278 - 290
(2009/04/11)

PROCESS FOR THE PREPARATION OF AMORPHOUS RABERAZOLE SODIUM
The present invention provides a process for the preparation of amorphous rabeprazole sodium said process comprising (a) suspending rabeprazole in an organic solvent having dielectric constant ranging between 1.8 to 21, wherein at least 80 % of the organic solvent is a ketonic solvent having dielectric constant ranging between 13 to 21; (b) adding aqueous sodium hydroxide; (c) azeotropically distilling out water from the above reaction system to obtain a residue, (d) adding ketonic solvent having dielectric constant ranging between 13 to 21 to the residue of step (c) to obtain a solution; and (e) quenching the solution obtained in step (d) into an organic solvent having a dielectric constant ranging between 1.8 to 21, wherein at least 80 % of the organic solvent is an ethereal solvent having dielectric constant ranging between 1.8 to 5.
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Page/Page column 7

(2009/12/05)

IMPROVED PROCESS FOR AMORPHOUS RABEPRAZOLE SODIUM
The present invention provides an improved and efficient process for preparation of highly pure amorphous rabeprazole sodium. Thus, for example, rabeprazole is dissolved in an alcoholic sodium hydroxide solution followed by carbon treatment, the resulting filtrate is distilled under vacuum at 50 - 52°C followed by co-distillation with cyclohexane and the resulting residue is dissolved in anisole; the solution is added to cyclohexane under agitation and then collected the precipitated solid by filtration or centrifugation.
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Page/Page column 6

(2009/01/20)

Novel Processes for the Production of Amorphous Rabeprazole Sodium
The invention is directed to overcome the problems associated with the formation of rabeprazole sodium, i.e. formation of (2-({[4-(3-methoxypropoxy)-3-methylpyridin-2-yl]methyl}sulfonyl)-1H-benzimidazole side product which is achieved by a process for the preparation of amorphous rabeprazole salt, e.g. sodium, comprising the steps of: i) contacting rabeprazole salt complex, e.g. sodium acetone complex with a first solvent system;ii) filtering the solid from the solvent system used in step i) or distilling, totally or partially, the solvent system used in step i) under reduced or atmospheric pressure, to thereby obtain a residue;iii) contacting the solid or the residue of step ii) with a second solvent system;v) filtering the solid from the solvent system used in step iii) or distilling, totally or partially, the solvent system used in step iii) under reduced or atmospheric pressure to thereby obtain a solid;v) optionally repeating steps iii) and iv) one or more times;vi) optionally filtering to obtain a wet solid; andvii) drying the wet solid.
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Page/Page column 5

(2008/12/07)

A PROCESS FOR THE PREPARATION OF BENZIMIDAZOLE DERIVATIVES AND THEIR SALTS
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 32

(2008/06/13)

A process for the preparation of pyridine-methylsulfinyl compounds
A process for the preparation of a compound of formula (I), or a salt thereof, wherein Q is =CR8- or =N-; and R1-R8 are as herein defined; comprising the reaction of a compound of formula (II), or a salt thereof, wherein Q, R1-R7 are as herein defined; with a reducing agent selected from a trivalent phosphorous compound, an oxidizable solvent and a sulfonic acid chloride; and, if desired, the conversion of a compound of formula (I) to another compound of formula (I) or a salt thereof.
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Page/Page column 7

(2008/12/05)

METHOD OF PREPARATION OF AMORPHOUS RABEPRAZOLE SODIUM
The invention relates to preparation of amorphous rabeprazole sodium from rabeprazole using sodium tertiary butoxide in tertiary butyl alcohol. The preparation further avoids the use of halogenated solvents, and freeze drying.
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Page/Page column 5

(2008/06/13)

PROCESS FOR PREPARING PROTON PUMP INHIBITORS
The present application relates to a process for the preparation of proton pump inhibitors of the benzimidazole-type represented by the general Formula I, Formula I wherein R1 and R2 are the same as or different from each other and are selected from hydrogen, methoxy or difluoromethoxy, R3, R4 and R5 are the same as or different from each other and are selected from hydrogen, methyl, methoxy, methoxypropoxy or trifluoroethoxy, and their pharmaceutically acceptable salts.
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Page/Page column 23-24

(2008/06/13)

IMPROVED PROCESS FOR THE PREPARATION OF PURE RABEPRAZOLE
The present invention relates to a process for the preparation of pure Rabeprazole sulfoxide using the solvent mixture for the extraction steps and this invention further relates to the process for the preparation of amorphous Rabeprazole sodium using pure rabeprazole base in presence of aqueous NaOH and water miscible solvent and adding an anti-solvent.
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Page/Page column 11

(2009/01/23)

SALTS OF BENZIMIDAZOLE DERIVATIVE WITH AMINES AND PROCESS FOR PRODUCTION THEREOF
It is an object of the present invention to provide (1) a process for manufacturing alkali metal salts of 2-[{4-(3-methoxypropoxy)-3-methylpyridin-2-yl}methylsulfinyl]-1 H -benzimidazole which are useful as gastric acid secretion inhibitors, anti-ulcer agents and other drugs and (2) salts of 2-[{4-(3-methoxypropoxy)-3-methylpyridin-2-yl}methylsulfinyl]-1 H -benzimidazole with amines which are intermediates for the production of the alkali metal salts, and a process for manufacturing the same. According to the present invention, disclosed are salts represented by the following formula (I): (wherein A + represents an isopropylammonium ion, sec-butylammonium ion or cyclopentylammonium ion).
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Page/Page column 25

(2008/06/13)

Process for Production of Benzimidazole Derivative Salt Precipitate
The present invention provides a process for the production of a 2-[{4-(3-methoxypropoxy)-3-methylpyridin-2-yl}methylsulfinyl]-1 H-benzimidazole alkali metal salt (1), which is a drug or an intermediate for the production of a drug, the process not requiring large-scale equipment and being excellent in terms of workability, operability and energy conservation. According to the present invention, there is disclosed a process for the production of a salt precipitate represented by formula (1) (wherein B represents an alkali metal ion), the process comprising the steps of: dissolving the compound represented by formula (2) in a first organic solvent and adding an alkali metal hydroxide, or dissolving the alkali metal hydroxide in the first organic solvent and adding the compound represented by formula (2); and further adding a second organic solvent to a reaction mixture obtained.
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Page/Page column 5

(2008/06/13)

Process for the preparation of 2-[{4-(3-methoxypropoxy)-3-methylpyridin-2-yl}methylsulfinyl]-1H-benzimidazole substantially free of sulfone impurity
A process for the preparation of rabeprazole substantially free of sulfone impurity is disclosed. The method comprises reacting 2-[{4-(3-methoxypropoxy)-3-methylpyridine-2-yl}methylthio]-1H-benzimidazole with an oxidizing agent and removing the unreacted sulfide compounds and sulfone impurities from the medium by means of an extraction and two additional crystallization steps. The unreacted compounds are removed with the organic layer of said extraction step whereas the impurities are removed with the additional crystallization steps wherein rabeprazole free base and impurities are treated in the same phase. Preparation of rabeprazole sodium salt is also covered within the scope of the present invention. Product of the previous crystallization steps is dissolved in methanolic sodium hydroxide and obtained solution is concentrated. Sodium salt of rabeprazole is precipitated by way of adding the residue into diethyl ether. Both rabeprazole and its sodium salt are obtained with sulfone impurity percentage around 0.08 %.
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Page/Page column 6

(2008/06/13)

NEW PROCESS FOR SYNTHESIS OF PROTON PUMP INHIBITORS
A process for preparation of rabeprazole sodium comprising oxidation of wet or dry rabeprazole sulphide with sodium hypohalite in water or a mixture of water and water miscible solvent using alkali metal hydroxide and catalyst is disclosed herein. The present invention also discloses process for preparation of rabeprazole sulphide.
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Page/Page column 8-9

(2008/06/13)

MORPHINE SULPHATE FORMULATIONS
Described is a pellet composition comprising a core element comprising morphine sulfate, a filler and a binder, wherein the morphine sulfate, calculated as the anhydrous form, comprises about 50 wt% to about 85 wt% of the total weight of the core element; and a coating disposed on at least a portion of the core element, the coating comprising an insoluble matrix polymer which is insoluble at pH 1 to 7.5; an enteric polymer which is insoluble at pH 1 to 4 and soluble at pH 6 to 7.5; and an acid soluble polymer which is soluble at a pH of 1 to 4, wherein the ratio of the acid soluble polymer to the enteric polymer is 1.45:1 to 2.5:1 on a weight basis. Also described are dosage forms comprising the disclosed pellets.
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Page/Page column 7

(2008/06/13)

AN IMPROVED PROCESS FOR THE MANUFACTURE OF RABEPRAZOLE SODIUM
A process for manufacture of amorphous Rabeprazole sodium with mean particle diameter between 10 to 55 μm said process comprising addition of Rabeprazole to aqueous sodium hydroxide; addition of ethyl alcohol to the solution; distillation of solvents from the solution thus obtained till thick mass is obtained; addition of an organic solvent to the residue to obtain a clear solution; addition of this clear solution to an anti- solvent under agitation and isolation of the product.
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Page/Page column 5; 6

(2008/06/13)

PROCESS FOR PRODUCTION OF SULFOXIDE DERIVATIVES OR SALTS THEREOF IN THE AMORPHOUS STATE
A process for producing sulfoxide derivatives or salts thereof in the amorphous state, characterized by heat-drying solvated crystals of a sulfoxide derivative or a salt thereof represented by the general formula (I): wherein R1 represents a hydrogen atom, a methoxy group, or a difluoromethoxy group; R2 represents a methyl group or a methoxy group; R3 represents a 3-methoxypropoxy group, a methoxy group, or a 2,2,2-trifluoroethoxy group; R4 represents a hydrogen atom or a methoxy group; and B represents a hydrogen atom, an alkali metal or 1/2 alkaline earth metal.
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Page/Page column 11

(2008/06/13)

Crystalline form Z of rabeprazole sodium and process for preparation thereof
The present invention relates to novel crystalline Form Z of rabeprazole sodium and a process for the preparation of the crystalline Form Z as well as composition, pharmaceutical composition and method utilizing the crystalline Form Z.
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Page/Page column 7

(2008/06/13)

PAHARMACEUTICAL PROCESS AND COMPOUNDS PREPARED THEREBY
The present invention relates to an improved process for the preparation of a sulfinyl compound of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, from a sulfide compound of formula (II), wherein in both formulae (I) and (II) R1 and R3 are selected from the group consisting of hydrogen, methyl or C1-4alkoxy, R2 is selected from the group consisting of substituted or unsubstituted C1-4alkoxy and R4 is selected from the group consisting of hydrogen or substituted or unsubstituted C1-4alkoxy.
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Page 13

(2008/06/13)

Crystalline form Z of rabeprazole sodium and process for preparation thereof
The present invention relates to novel crystalline Form Z of rabeprazole sodium and a process for the preparation of the crystalline Form Z as well as composition, pharmaceutical composition and method utilizing the crystalline Form Z.
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Page 8

(2008/06/13)

PROCESS FOR THE PREPARATION OF HIGHLY RABEPRAZOLE SODIUM SALT
A method for the preparation of (±)-sodium-2-[[[4-(3- methoxypropoxy)-3- methyl-pyridinyl]methyl]sulfinyl]-1H-benzimidazole(Rabeprazole sodium) of formula (I), which comprises dissolving Rabeprazole of Formula (II) in aqueous sodium hydroxide until complete dissolution has taken place and thereafter subjecting the so obtained solution to lyophilization to obtain highly pure Rabeprazole sodium of Formula (I) in dry form.
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Page 2

(2008/06/13)

CRYSTALLINE FORMS OF RABEPRAZOLE SODIUM
The present invention relates to novel polymorphic forms of Rabeprazole sodium. The present invention also relates to methods of making polymorphic forms of Rabeprazole sodium. Achiphex7 (Rabeprazole sodium) is an inhibitor of the gastric proton pump. It causes dose-dependant inhibition of acid secretion and is useful as an antiulcer agent. The chemical designation of Rabeprazole sodium is 2-[[[4-(3-methoxypropoxy)-3 methyl-2-pyridinyl]-methyl] sulfinyl]-1H-benzimidazole sodium. It may be represented by Formula (1).
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Page/Page column 12-13

(2008/06/13)

Crystals of benzimidazole derivatives and their production
A substantially solvent-free and stable crystal of the compound of the formula: STR1 wherein the ring A may optionally be substituted, R1 represents hydrogen or an N-protecting group, each of R2, R3 and R4 (1) a hydrogen atom, (2) an alkyl group which may optionally be substituted with halogen atom(s) or (3) an alkoxy group which may optionally be substituted with halogen atom(s) or alkoxy; or its salt, is produced by subjecting a solvate of the compound (I) or its salt to de-solvent treatment, in an industrially advantageous method.
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(2008/06/13)