- 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
- -
-
Paragraph 0031-0032; 0035-0043; 0045-0046; 0049; 0051;...
(2021/09/01)
-
- 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
- -
-
Page/Page column 30-31
(2021/06/04)
-
- Asymmetric synthesis of (-)-atorvastatin calcium by tandem catalysis
-
A seven-step synthesis of (-)-atorvastatin calcium, an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMGCoA) reductase, has been developed. The key transformations of the present synthesis are a tandem olefin cross-metathesis/ hemiacetalization/intramolecular oxa-Michael addition and a subsequent regioselective BaeyerVilliger oxidation for the stereocontrolled construction of the syn-3,5-dihydroxy carboxylic acid substructure.
- Fuwa, Haruhiko,Minami, Riko,Murata, Keisuke
-
p. 2028 - 2035
(2021/09/16)
-
- 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
- -
-
Paragraph 0043-0068
(2020/02/29)
-
- 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.
- -
-
Page/Page column 70; 72-73; 75
(2020/02/14)
-
- Atorvastatin calcium intermediate as well as preparation method and application thereof
-
The invention discloses an atorvastatin calcium intermediate as well as a preparation method and application thereof. A synthesis process of the intermediate is environmentally-friendly, simple to operate and low in EHS risk; raw materials are easy to obtain; a used chemical reagent is small in toxicity and low in cost; and the synthesis process is a green synthesis process suitable for the industrial production. Moreover, the intermediate provided by the invention is applied to the synthesis of atorvastatin calcium and a key intermediate thereof, the route is relatively short, the yield is high, the industrial production cost of the atorvastatin calcium is effectively reduced, and the atorvastatin calcium intermediate has a relatively high industrial application prospect.
- -
-
-
- Separating method for impurity A and impurity B and method for effectively reducing content of impurity A in atorvastatin calcium condensate
-
The invention discloses a separating method for an impurity A and an impurity B and a method for effectively reducing the content of an impurity A in an atorvastatin calcium condensate, and belongs tothe technical field of impurity separating in medicinal chemistry. The invention specifically discloses the impurity A in the atorvastatin calcium condensate, and a method for separating the impurityA from the atorvastatin calcium condensate, further studies that the impurity A of the atorvastatin calcium condensate is introduced by the impurity B in a starting material ATS-9 crude product, anddiscloses a method for separating the impurity B in the ATS-9 crude product, so as to reduce the content of impurity A in the atorvastatin calcium condensate, and further provide the basis for reducing the content of impurities in atorvastatin calcium diamine. The purity of the impurity A in the atorvastatin calcium condensate obtained by the separating method is at least 99.5%, and the purity ofthe impurity B in ATS-9 is at least 99.5%.
- -
-
Paragraph 0071; 0072; 0074
(2019/01/16)
-
- 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.
- -
-
Paragraph 0006; 0024; 0028; 0029
(2018/10/19)
-
- Low-barium vastatin calcium and preparation method thereof
-
The invention provides low-barium vastatin calcium of which the barium content is not greater than 140ppm, the barium content is a weight percentage of a barium element molecular weight of 137.33 in avastatin calcium sample, the barium content is preferab
- -
-
Paragraph 0072; 0073; 0074
(2018/11/03)
-
- AN IMPROVED PROCESS FOR PREPARATION OF ATORVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
-
The present invention provides an improved process for the preparation of Atorvastatin or pharmaceutically acceptable salts thereof in high yield and purity.
- -
-
Page/Page column 17; 18; 19; 20; 21; 22
(2017/05/07)
-
- A atorvastatin condensation the intermediate product of the resolution method (by machine translation)
-
The invention relates to a kind of atorvastatin "condensate" intermediate resolution method, the method, comprises the following steps: step 1, takes shrinks compound trans-isomer mixture, in order to isopropanol as the solvent heating and dissolves it, s
- -
-
Paragraph 0065; 0076; 0077; 0078; 0089; 0090
(2017/06/24)
-
- New chloramphenicol Schiff base ligands for the titanium-mediated asymmetric aldol reaction of α,β-unsaturated aldehydes with diketene: A short synthesis of atorvastatin calcium
-
Several novel chiral Schiff base ligands were prepared from a commercially available chloramphenicol base and applied to the titanium-mediated asymmetric aldol reaction of diketene with various α,β-unsaturated aldehydes. This reaction proceeded in good yield with high enantioselectivity. The synthetic utility of this methodology was demonstrated in the short synthesis of atorvastatin calcium.
- Wang, Haifeng,Yan, Linjie,Xiong, Fangjun,Wu, Yan,Chen, Fener
-
p. 75470 - 75477
(2016/08/24)
-
- Production technology of atorvastatin calcium
-
The invention relates to a production technology of atorvastatin calcium.The production technology comprises the steps that (4R-Cis)-2.2-dimethyl-6-(2-aminoethyl)-1,3-dioxane-4-tert-butyl acetate and 2-[2-(4-fluorophenyl)-2-oxo-1-phenylethyl]-4-methyl-3-o
- -
-
-
- Asymmetric synthesis of the HMG-CoA reductase inhibitor atorvastatin calcium: An organocatalytic anhydride desymmetrization and cyanide-free side chain elongation approach
-
An efficient asymmetric synthesis of atorvastatin calcium has been achieved from commercially available diethyl 3-hydroxyglutarate through a novel approach that involves an organocatalytic enantioselective cyclic anhydride desymmetrization to establish C(
- Chen, Xiaofei,Xiong, Fangjun,Chen, Wenxue,He, Qiuqin,Chen, Fener
-
p. 2723 - 2728
(2014/04/17)
-
- Synthetic studies on statins. Part 1: A short and cyanide-free synthesis of atorvastatin calcium via an enantioselective aldol strategy
-
A short and cyanide-free enantioselective synthesis of atorvastatin calcium has been achieved starting from a commercially available highly substituted 1,4-diketone in an overall yield of 40%. The key step in this approach is the asymmetric aldol reaction of an aldehyde with diketene in the presence of Ti(O-i-Pr)4-Schiff base complex to create the (5R)-stereochemistry of atorvastatin calcium.
- Hu, Lemeng,Xiong, Fangjun,Chen, Xiaofei,Chen, Wenxue,He, Qiuqin,Chen, Fener
-
p. 207 - 211
(2013/04/10)
-
- ESTERS OF HEXANOIC ACIDS AS INTERMEDIATES FOR THE PREPARATION OF ATORVASTATIN
-
The invention relates to compounds of general formula (3) wherein R4 is allyl, 2-butyl, cyclohexyl, 3-methyl-2-butyl or 4-methyl-2-pentyl, a method for the preparation of compounds of general formula (3) and their use in the preparation of ator
- -
-
-
- MICRONIZED CRYSTALS OF ATORVASTATIN HEMICALCIUM
-
The present invention relates to micronized crystals of atorvastatin hemi-calcium, a method for the preparation of micronized crystals of atorvastatin hemi-calcium and a pharmaceutical dosage form comprising said micronized crystals of atorvastatin hemi-c
- -
-
Page/Page column 9; 10
(2013/03/26)
-
- 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)
-
- ESTERS OF HEXANOIC ACIDS AS INTERMEDIATES FOR THE PREPARATION OF ATORVASTATIN
-
The invention relates to compounds of general formula (3) wherein R4 is allyl, 2-butyl, cyclohexyl, 3-methyl-2-butyl or 4-methyl-2-pentyl, a method for the preparation of compounds of general formula (3) and their use in the preparation of ator
- -
-
-
- SALTS OF 7-AMINO-3,5-DIHYDROXYHEPTANOIC ACID ESTERS
-
The invention relates to salts of acids with 2-propyl esters of general formula (2) The invention also relates to a method for the preparation of salts of acids with compounds of general formula (2) and to the use thereof in the preparation of atorvastati
- -
-
-
- 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
- -
-
Page/Page column 14
(2011/08/08)
-
- PRODUCTION OF ATORVASTATIN LOW IN ETHER IMPURITIES
-
The present invention relates to a method for the production of atorvastatin having decreased levels of impurities of general formulae (3) and (4) by means of a concentrating step.
- -
-
Page/Page column 7-8
(2011/11/06)
-
- PRODUCTION OF ATORVASTATIN LOW IN LACTONE IMPURITIES
-
The present invention relates to a method for the production of atorvastatin having decreased levels of impurity (3) by means of a pH-controlling step.
- -
-
Page/Page column 4-5
(2011/11/06)
-
- Amorphous Coprecipitates of Atorvastatin Pharmaceutically Acceptable Salts
-
The present invention relates to stable amorphous co-precipitates of atorvastatin pharmaceutically acceptable salts with pharmaceutically acceptable excipients, method for the preparation, pharmaceutical compositions, and method of treating thereof. Advan
- -
-
-
- Methods for predicting the response to statins
-
The invention provides methods for optimizing therapeutic efficacy for treating hypercholesterolemia in a subject having a cardiovascular disease (CVD), comprising (a) determining subject characteristics that affect the likelihood of reaching a goal level of low density lipoprotein (LDL); and (b) obtaining success probabilities of a variety of statin treatments for reaching said goal level of LDL using said subject characteristics and a multivariate model; and (c) administrating the optimal statin treatment with the highest success probability of step (b) to said subject thereby optimizing therapeutic efficacy for treating hypercholesterolemia in said subject.
- -
-
-
- AN IMPROVED PROCESS FOR THE PREPARATION OF AMORPHOUS ATORVASTATIN CALCIUM
-
The present invention relates to an improved process for the preparation of pure amorphous atorvastatin calcium comprising reaction of (3R,5R)-2-(4-fluorophenyl)- 3,5-dihydroxy-5-(1 -methylethyl)-3-phenyl-4-[(phenyl amino) carbonyl]-1 H-pyrrole-1 - heptan
- -
-
Page/Page column 7
(2011/09/19)
-
- Novel Polymorph of Atorvastatin Calcium and Use Thereof for the Preparation of Amorphous Atorvastatin Calcium
-
The present invention provides a novel polymorphic form of atorvastatin calcium, designated as form Al, process for preparation, pharmaceutical compositions, and method of treating thereof. The present invention further provides a process for the preparat
- -
-
-
- PROCESS FOR THE PREPARATION OF AMORPHOUS ATORVASTATIN CALCIUM
-
The present invention also provides the amorphous form of hemi-calcium salt of atorvastatin with high purity and processes for preparation thereof.
- -
-
Page/Page column 7
(2010/08/07)
-
- 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.
- -
-
Page/Page column 36
(2009/09/05)
-
- PREPARATION OF NOVEL NON-CRYSTALLINE FORMS OF ATORVASTATIN CALCIUM
-
The invention relates to a process for producing non crystalline forms of Atorvastatin Calcium.
- -
-
Page/Page column 6-7
(2009/12/23)
-
- 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.
- -
-
Page/Page column 9; 11
(2009/09/07)
-
- METHOD FOR THE PREPARATION OF 4-FLUORO-ALPHA-[2-METHYL-1-OXOPROPYL]-y-OXO-N-BETA-DIPHENYLBENZENEBUTANAMIDE AND PRODUCTS THEREFROM
-
A method for the preparation of 4-fluoro-α-[2-methyl-1-oxopropyl]-y-oxo-N-β-diphenylbenzenebutanamide also known as 2-[2-(4-fluorophenyl)-2-oxo-1-phenylethyl]-4-methyl-3-oxo-pentanoic acid phenylamide of the formula I containing about 0.1% or less of α-[2-methyl-1-oxopropyl]-γ-oxo-N-p-diphenylbenzene butanamide, about 0.05% or less of difluoro-α-[2-methyl-1-oxopropyl]-y-oxo-N-β-diphenylbenzene butanamide and about 0.1% or less of 3-[2-(4-Fluorophenyl)-2-oxo-1-phenyl-ethoxy]-4-methyl-pent-2-enoic acid phenylamide.
- -
-
Page/Page column 7
(2009/12/23)
-
- PROCESS FOR THE PREPARATION OF ATORVASTATIN
-
The present invention relates to a process for preparing the cholesterol biosynthesis inhibitor atorvastatin, (3R,5R)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4- (phenylcarbamoyl)-lH-pyrrol-l-yl]-3,5-dihydroxyheptanoic acid calcium salt, which comprises
- -
-
Page/Page column 25
(2009/05/30)
-
- PROCESS FOR THE MODIFICATION OF THE SOLID STATE OF A COMPOUND AND CO-AMORPHOUS COMPOSITIONS PRODUCED WITH SAME
-
The invention provides a process for preparing non-crystalline organic compositions and non-crystalline, co-amorphous blends of organic compounds.
- -
-
Page/Page column 30-32
(2009/05/28)
-
- A process for preparation of amorphous form of atorvastatin hemi-calcium salt
-
The present invention relates to a process for preparation of atorvastatin hemi-calcium salt in its amorphous form.
- -
-
Page/Page column 16; 17
(2009/08/13)
-
- PROCESS FOR PRODUCING AMORPHOUS ATORVASTATIN CALCIUM
-
Disclosed herein is an improved process for producing amorphous atorvastatin calcium and a method of packaging thereof.
- -
-
Page/Page column 5
(2009/08/16)
-
- NOVEL PROCESS FOR THE PREPARATION OF 4-FLUORO-ALPHA-[2-METHYL -1-OXOPROPYL]-GAMMA-OXO-N-?-DIPHENYLBENZENEBUTANAMIDE AND PRODUCTS THEREFROM
-
A novel process for the preparation of 4-fluoro-α-[2-methyl-1-oxopropyl]-γ-oxo-N-β-diphenylbenzenebutanamide also known as 2-[2-(4-fluorophenyl)-2-oxo-1-phenylethyl]-4-methyl-3-oxo-pentanoic acid phenylamide of the formula (I) containing about 0.1% or less of α-[2-methyl-1-oxopropyl]-γ-oxo-N-β-diphenylbenzene butanamide, about 0.05 % or less of difluoro -α-[2-methyl-1-oxopropyl]-γ-oxo-N-β-diphenylbenzene butanamide and about 0.1% or less of 3-[2-(4-Fluorophenyl)-2-oxo-1-phenyl-ethoxy]-4-methyl-pent-2-enoic acid phenylamide.
- -
-
Page/Page column 18-19
(2009/12/27)
-
- 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.
- -
-
Page/Page column 7
(2008/12/07)
-
- Atorvastatin calcium propylene glycol solvates
-
Atorvastatin calcium propylene glycol solvates and processes to prepare these novel solvates which are particularly useful and suitable for pharmaceutical applications.
- -
-
Page/Page column 6
(2008/12/07)
-
- AN IMPROVED PROCESS FOR THE PREPARATION OF STABLE AMORPHOUS ATORVASTATIN HEMI CALCIUM AND THEIR SALTS THEREOF
-
The present invention describes the preparation of highly pure (i.e. filling in ICH quality parameters with respect to related substances) stable amorphous Atorvastatin calcium salt comprising (a) hydrolysis of 1,3-dioxane ring of (4R-Cis)-1,1-dimethyleth
- -
-
Page/Page column 7; 11
(2008/12/08)
-
- CRYSTALLINE FORMS OF ATORVASTATIN
-
Novel forms of atorvastatin hemi-calcium have been prepared and characterized. These novel forms are particularly useful in pharmaceutical compositions.
- -
-
Page/Page column 15
(2008/06/13)
-
- NOVEL PROCESS FOR THE SYNTHESIS OF [R-(R*, R*)]-2-(4-FLUOROPHENYL)-BETA, DELTA-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1-HEPTANOIC ACID OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
-
An improved synthesis for the preparation of [R-(R*, R*)]-2-(4-fluorophenyl)- β, δ-dihydroxy-5-(1- methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1 H-pyrrole-1-heptanoic acid or a pharmaceutically acceptable salt thereof, as well as other valuable interm
- -
-
Page/Page column 17; 21
(2008/12/06)
-
- PREPARATION OF ATORVASTATIN CALCIUM FORM VI AND COMPOSITIONS THEREOF
-
The present invention provides processes to prepare atorvastatin calcium Form VI, pharmaceutical compositions comprising atorvastatin calcium Form VI, and processes to prepare said compositions. An aspect of the invention relates to atorvastatin calcium F
- -
-
Page/Page column 5
(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
- -
-
Page/Page column 16
(2008/06/13)
-
- A PROCESS OF PREPARING AMORPHOUS ATORVASTATIN CALCIUM
-
A simple and economical process for the preparation of amorphous atorvastatin calcium in high purity and good yield from crystalline atorvastatin sodium without forming crystalline atorvastatin calcium is disclosed.
- -
-
Page/Page column 9-11; 13-14
(2008/06/13)
-
- PROCESS FOR THE PREPARATION OF AMORPHOUS ATORVASTATIN CALCIUM SALT
-
Disclosed is a novel process for preparing pure amorphous form of Atorvastatin employing a suitable solvent system selected from water, water miscible solvents or water immiscible solvents or mixture thereof.
- -
-
Page/Page column 9;
(2008/06/13)
-
- Novel crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms
-
The present invention provides novel forms of atorvastatin designated Forms VI, VIII, IX, X, XI and XII and novel processes for their preparation as well as processes for preparing atorvastatin Forms I, II, IV, V and amorphous atorvastatin. Also provided
- -
-
Page/Page column 12
(2008/06/13)
-
- PROCESS FOR ANNEALING AMORPHOUS ATORVASTATIN
-
Processes for annealing amorphous atorvastatin is described. Pharmaceutical compositions and formulations containing annealed amorphous atorvastatin are also described.
- -
-
Page/Page column 13-17
(2008/06/13)
-
- PROCESS FOR THE PREPARATION OF ATORVASTATIN CALCIUM
-
The present invention relates to process for the preparation of atorvastatin calcium. The process provides the novel approach for the synthesis of an important intermediate atorvastatin protected diol chemically (4R-cis)-6-[-2-[3-phenyl-4-(phenyl- carbamoyl)-2-(4-flourophenyl)-5-(1-methyl-ethyl)-pyrrol-1-yl]-ethyl]-2,2-dimethyl- [1,3]dioxane-4-yl-acetic acid-tertriay butyl ester for atorvastatin calcium i.e. [R- (R*,R*)]-2-(4-fluorophenyl-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4- [(phenylamino) carbonyl]-1H-pyrrole-1-heptanoic acid calcium salt (2:1). The present invention relates the use of amino side chain i.e [6-(2-aminoethyl)-2,2,-dimethyl- [1,3]dioxan-4-yl]-acetic acid tert-butyl ester and stetter compound i.e. 4-(4- Fluoroρhenyl)-2-isobutryl-4-oxo-N-phenyl butryl amide as an important starting materials for the preparation of atorvastatin protected diol in the high yield and thereby the recovery of amino side chain with an industrially applicable process.
- -
-
Page/Page column 8
(2008/06/13)
-
