cas 134523-01-6, ATORVASTATIN SODIUM | Articles data

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PROCESS FOR THE CONTINUOUS MANUFACTURE OF STATINS
The present invention relates to process for the continuous manufacture of Statins or salts thereof. The present invention relates to process for the continuous manufacture of Atorvastatin or a salt thereof. The present invention relates to a continuous m
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(2021/06/04)

Method for purifying atorvastatin calcium intermediate
The atorvastatin calcium intermediate is subjected to hydrolysis reaction to obtain the reaction liquid of atorvastatin calcium intermediate. The reaction liquid is extracted with a stripping solvent and is separated and separated to obtain an aqueous pha
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(2021/09/01)

AN IMPROVED AND COMMERCIALLY VIABLE PROCESS FOR PREPARATION OF PYRROLE DERIVATIVES WITH IMPROVED IMPURITY PROFILE & MINIMISATION OF UNIT OPERATIONS.
The present invention relates to improved process for the preparation of a pyrrole derivative as a racemic mixture, an enantiomer, a diastereoisomer, a mixture thereof, a tautomer thereof or a pharmaceutically acceptable salt and hydrates thereof and also intermediates involved therein. Particularly invention is directed to improved processes for the preparation of pyrrole derivatives such as (4R,cis)-6-[2-[3-phenyl-4-(phenyl-carbamoyl)-2-(4-fluorophenyl)-5-(1-methyl-ethyl)-pyrrole-1-yl]-2,2-dimethyl-[1,3]dioxane-4-yl-acetic acid-tertiary butyl ester of formula IV followed by its conversion into [R-(R*, R*]-2-(4-fluorophenyl)- β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1- heptanoic acid particularly calcium salt and its hydrate represented by Formulae I/IA respectively wherein formation of the impurities is either eliminated or minimized in the corresponding intermediaries.
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(2020/02/14)

Preparation method of crystal form I atorvastatin calcium
The invention discloses a preparation method of crystal form I atorvastatin calcium. The method includes the steps of: preparation of atorvastatin ester; preparation of an atorvastatin salt; preparation of atorvastatin calcium; refining an atorvastatin ca
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(2020/02/29)

Preparing method of high-purity atorvastatin calcium
The invention discloses a preparing method of high-purity atorvastatin calcium, and belongs to the technical field of organic synthesis. The method includes the steps of making a compound V and calcium acetate react in a water and alcohol mixed solvent system, and conducting cooling crystallization and filtration after the reaction is completed to obtain an atorvastatin calcium crude product, wherein the reaction temperature is 40-70 DEG C, the volume ratio of alcohols to water in the reaction system is 1:(2-8), and the mass percentage concentration of the compound V in a mixed solvent is 5-10%; dissolving the atorvastatin calcium crude product in a recrystallization solvent A, adding I-type atorvastatin calcium crystals at 45-85 DEG C for crystal transformation, and conducting cooling crystallization, filtration, washing and drying after crystal transformation is completed to obtain a fine product, wherein the mass percentage concentration of the atorvastatin calcium crude product inthe recrystallization solvent A is 5-10%. The method has the advantages of being high in product purity, easy and safe to operate, high in yield and the like and is suitable for large-scale industrialproduction.
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(2018/10/19)

Synthesis method of atorvastatin calcium
The invention relates to a synthesis method of an atorvastatin calcium. A cheap and easy-to-get Paal-Knorr cyclization product formula-V compound is subjected to hydroxyl deprotection, esterolysis andsalinization so as to obtain a target product atorvasta
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(2018/12/02)

Enantioselective synthesis of allylboronates and allylic alcohols by copper-catalyzed 1,6-boration
Chiral secondary allylboronates are obtained in high enantioselectivities and 1,6:1,4 ratios by the copper-catalyzed 1,6-boration of electron-deficient dienes with bis(pinacolato)diboron (B2(pin)2). The reactions proceed efficiently using catalyst loadings as low as 0.0049 mol %. The allylboronates may be oxidized to the allylic alcohols, and can be used in stereoselective aldehyde allylborations. This process was applied to a concise synthesis of atorvastatin, in which the key 1,6-boration was performed using only a 0.02 mol % catalyst loading. 1,6-Borations of electron-deficient dienes with bis(pinacolato)diboron using copper catalyst loadings as low as 0.0049 mol % provided chiral allylboronates that, after oxidation, result in allylic alcohols in high enantioselectivities and 1,6:1,4 ratios. The allylboronates can also be used in stereoselective allylations of aldehydes. This process was applied to a concise synthesis of atorvastatin.
Luo, Yunfei,Roy, Iain D.,Madec, Amael G. E.,Lam, Hon Wai
p. 4186 - 4190
(2014/05/06)

Spectroscopic characterization and quantitative determination of atorvastatin calcium impurities by novel HPLC method
Seven process related impurities were identified by LC-MS in the atorvastatin calcium drug substance. These impurities were identified by LC-MS. The structure of impurities was confirmed by modern spectroscopic techniques like 1H NMR and IR and physicochemical studies conducted by using synthesized authentic reference compounds. The synthesized reference samples of the impurity compounds were used for the quantitative HPLC determination. These impurities were detected by newly developed gradient, reverse phase high performance liquid chromatographic (HPLC) method. The system suitability of HPLC analysis established the validity of the separation. The analytical method was validated according to International Conference of Harmonization (ICH) with respect to specificity, precision, accuracy, linearity, robustness and stability of analytical solutions to demonstrate the power of newly developed HPLC method.
Gupta, Lokesh Kumar
p. 495 - 501,7
(2012/12/11)

Spectroscopic characterization and quantitative determination of atorvastatin calcium impurities by novel HPLC method
Seven process related impurities were identified by LC-MS in the atorvastatin calcium drug substance. These impurities were identified by LC-MS. The structure of impurities was confirmed by modern spectroscopic techniques like 1H NMR and IR and physicochemical studies conducted by using synthesized authentic reference compounds. The synthesized reference samples of the impurity compounds were used for the quantitative HPLC determination. These impurities were detected by newly developed gradient, reverse phase high performance liquid chromatographic (HPLC) method. The system suitability of HPLC analysis established the validity of the separation. The analytical method was validated according to International Conference of Harmonization (ICH) with respect to specificity, precision, accuracy, linearity, robustness and stability of analytical solutions to demonstrate the power of newly developed HPLC method.
Gupta, Lokesh Kumar
p. 495 - 501
(2013/01/13)

A METHOD OF INDUSTRIAL PRODUCTION OF AN AMORPHOUS FORM OF ATORVASTATIN WITH A HIGH SPECIFIC SURFACE AREA AND ITS USE IN A DOSAGE FORM
The invention deals with an amorphous form of the hemicalcium salt of (3R,5R) 7-[3-phenyl- 4-phenylcarbamoyl-2-(4-fluorophenyl)-5-isopropylpyrrol-1-y1]-3,5-dihydroxyheptanoic acid (atorvastatin of formula I) with a high specific surface area, based on con
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Page/Page column 14

(2011/08/08)

A NOVEL POLYMORPHIC FORM OF ATORVASTATIN SALTS
The present invention provides an improved process for the preparation of Atorvastatin of formula (I) or its salts, preferably hemicalcium salt with purity greater than 99.5% using novel salts of Atorvastatin such as N,N- dicyclohexylethylenediamine salt of Atorvastatin and novel polymorph of Atorvastatin sodium salt. Formula (I).
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Page/Page column 23; 13

(2011/08/08)

PREPARATION PROCESS USEFUL IN SYNTHESIS OF ATORVASTATIN
The present invention relates to a preparation process useful in synthesis of atorvastatin, more particularly a process for preparing atorvastatin is effective in treating hyperlipemia, comprising protecting the dihydroxy group at C3 and C5 positions of t
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Page/Page column 9

(2011/05/16)

METHOD FOR THE PREPARATION OF ATORVASTATIN AND INTERMEDIATES USED THEREIN
The present invention relates to a novel method for preparing atorvastatin. According to the present invention, provided are a novel intermediate of the preparation of atorvastatin and a method of preparing large amounts of atorvastatin in a safe manner using the intermediate.
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Page/Page column 15-16

(2011/02/18)

PREPARATION OF NOVEL NON-CRYSTALLINE FORMS OF ATORVASTATIN CALCIUM
The invention relates to a process for producing non crystalline forms of Atorvastatin Calcium.
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Page/Page column 6-7

(2009/12/23)

PREPARATION PROCESS USEFUL IN SYNTHESIS OF ATORVASTATIN
The present invention relates to a preparation process useful in synthesis of atorvastatin, more particularly a process for preparing atorvastatin is effective in treating hyperlipemia, comprising protecting the dihydroxy group at C3 and C5 positions of t
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Page/Page column 16-17

(2009/08/14)

PROCESS FOR THE PRODUCTION OF ATORVASTATIN CALCIUM IN AMORPHOUS FORM
A process for the production of amorphous atorvastatin calcium and stabilized, amorphous atorvastatin calcium is provided.
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Page/Page column 8-9; 11

(2009/09/07)

CRYSTALLINE FORMS OF ATORVASTATIN HEMI-MAGNESIUM SALT AND A PROCESS THEREOF
The present invention relates to crystalline forms of atorvastatin hemi-magnesium salt and a process for the preparation of crystalline forms. It also relates to a pharmaceutical composition comprising these crystalline forms or combinations thereof optio
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Page/Page column 14-17; 19

(2010/01/30)

METHOD FOR THE PREPARATION OF ATORVASTATIN AND INTERMEDIATES USED THEREIN
The present invention relates to a novel method for preparing atorvastatin. According to the present invention, provided are a novel intermediate of the preparation of atorvastatin and a method of preparing large amounts of atorvastatin in a safe manner using the intermediate.
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Page/Page column 35-36

(2009/09/05)

A METHOD FOR PRODUCING STATINS IN PURE FORM
This invention provides a new method for the preparation of statins comprising hydrolyzing a mixture of compounds of the following formulas (Formula III and IV).
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Page/Page column 10

(2009/07/25)

NEW COMBINATION FOR USE IN THE TREATMENT OF INFLAMMATORY DISORDERS
There is provided combination products comprising (a) pemirolast, or a pharmaceutically-acceptable salt or solvate thereof; and (b) a statin, or a pharmaceutically-acceptable salt or solvate thereof. Such combination products find particular utility in th
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Page/Page column 41-42

(2008/12/06)

A NOVEL CRYSTALLINE FORM OF ATORVASTATIN SODIUM
A novel crystalline form of atorvastatin sodium. The said crystalline atorvastatin sodium has characteristic X-ray powder diffraction pattern and is highly pure with purity above 99.5%.
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Page/Page column 4

(2008/12/05)

Polymorphic form of atorvastatin calcium
The present invention relates to atorvastatin calcium, a useful agent for lowering serum cholesterol levels. New atorvastatin calcium Form V, processes for preparing the new form, and pharmaceutical compositions and dosage forms containing the new form are disclosed.
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Page/Page column 6

(2008/12/07)

POLYMORPHS OF ATORVASTATIN SALTS
Polymorph and amorphous forms of atorvastatin sodium and hemi-magnesium, processes for their preparation and pharmaceutical compositions comprising them are described.
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Page/Page column 20

(2008/06/13)

PHARMACEUTICAL COMBINATION COMPRISING 3- (3-DIMETHYLAMIN0-1-ETHYL-2-METHYL-PR0PYL) -PHENOL AND AN NSAID
The present invention relates to a combination comprising as components (a) the compound 3-(3-Dimethylamino-1-ethyl-2-methyl-propyl)-phenol, and (b) one or more non-steroidal anti-inflammatory drugs (NSAIDs); a pharmaceutical salt comprising said componen
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Page/Page column 15

(2008/06/13)

PROCESS FOR ATORVASTATIN CALCIUM AMORPHOUS
A novel process of the preparation of amorphous atorvastatin calcium starting from a compound of Formula (II).
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Page/Page column 4-6

(2008/06/13)

PROCESSES FOR THE PREPARATION OF PYRROLE DERIVATIVES
A process for the preparation of a pyrrole derivative or a racemic mixture, an enantiomer, a diastereoisomer, a mixture thereof, a tautomer thereof, or a pharmaceutically acceptable salt thereof comprising reacting an amino compound of the general formula (I), wherein each R is independently hydrogen or a hydrolyzable protecting group, or each R, together with the oxygen atom to which each is bonded, form a hydrolyzable cyclic protecting group, or each R is bonded to the same substituent which is bonded to each oxygen atom to form a hydrolyzable protecting group and R1 is hydrogen, a lower alkyl or a cation capable of forming a non-toxic pharmaceutically acceptable salt, with a di-oxo compound of the general formula (II), wherein R2 is 1-naphthyl, 2-naphthyl, a C3-C25 cycloalkyl group, norbornenyl, a substituted or unsubstituted aryl group, benzyl, 2-, 3-, or 4-pyridinyl, or 2-, 3-, 4-pyridinyl-N-oxide, R3 and R4 are independently hydrogen, a lower alkyl, a C3-C25 cycloalkyl group, a substituted or unsubstituted aryl group, cyano, trifluoromethyl, or -CONR6R7 wherein R6 and R7 are independently hydrogen, a lower alkyl or a substituted or unsubstituted aryl group and R5 is a lower alkyl, a C3-C25 cycloalkyl or trifluoromethyl; in the presence of a catalyst and in at least one solvent. Also disclosed is a process for hydrolyzing the pyrrole derivative to provide, for example, atorvastatin or pharmaceutically acceptable salts thereof.
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Page/Page column 12-13

(2008/06/13)

Process for the production of atorvastatin calcium un amorphous form
A process for the production of amorphous atorvastatin calcium and stabilized, amorphous atorvastatin calcium is provided.
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Page/Page column 3; 14; 18

(2010/11/30)

SALT FORMS OF [R-(R*, R*)]-2-(4-FLOUROPHENYL)-BETA, DELTA-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1-HEPTANOIC ACID
Novel salt forms of [R-(R*,R*)]-2-(4-fluorophenyl)-?,S-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.
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Page/Page column 59

(2008/06/13)

PROCESS FOR THE PREPARATION OF ATORVASTATIN
The invention relates to processes for the preparation of atorvastatin. Atorvastatin is known by the chemical name [R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid. The hemi-calcium salt of atorvastatin is useful as an inhibitor of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase). The invention also relates to pharmaceutical compositions that include the atorvastatin or a pharmaceutically acceptable salt thereof and to use of said compositions for treating hypolipidemia, hypocholesterolemia and atherosclerosis.
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Page/Page column 12

(2008/06/13)

Process for the production of atorvastatin calcium in amorphous form
A process for the production of amorphous atorvastatin calcium and stabilized, amorphous atorvastatin calcium is provided.
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Page/Page column 5; 6; 10

(2010/02/14)

CRYSTALLINE FORM OF ATORVASTATIN HEMI CALCIUM
The present invention relates to novel crystalline form R of atorvastatin hemi calcium salt and hydrates thereof useful as pharmaceutical agents, to methods for their production and isolation, to pharmaceutical compositions which include novel crystalline form R of atorvastatin hemi calcium salt and hydrates thereof and a pharmaceutically acceptable carrier, and to pharmaceutical methods of treatment.
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Page/Page column 6; 14

(2010/02/14)

SYNTHESIS OF 3,5-DIHYDROXY-7-PYRROL-1-YL HEPTANOIC ACIDS
Atorvastatin and related 3,5-dihydroxy-7-pyrrol-1-yl heptanoic acids can be made by oxidation of a 3,5-dihydroxy-7-pyrrol-1-yl heptanol precursor from novel but readily accessible starting materials. Silylether-protected 7-amino-3,5-dihydroxy heptanoic acid esters undergo Paal Knorr reaction with 1,4-diketones to give valuable silylether-diprotected 3,5-dihydroxy-7-pyrrol-1-yl heptanoic acid ester intermediates for preparing atorvastatin. The Paal Knorr reaction of ketal-proctected 7-amino-3R, 5R-dihydroxy heptanoic acid esters with 4-fluoro-α-(2-methyl-1-oxopropyl-γ-oxo-N,β-diphenylbenzenebutanamide occurs in high yield with few side products when it is conducted in a low boiling point ether.
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Page 31-32

(2010/02/07)

The convergent synthesis of CI-981, an optically active, highly potent, tissue selective inhibitor of HMG-CoA reductase
The synthesis of CI-981 is described starting from isobutyrylacetanilide (3) and the key chiral intermediate 2.
Baumann,Butler,Deering,Mennen,Millar,Nanninga,Palmer,Roth
p. 2283 - 2284
(2007/10/02)