- PROCESS FOR MANUFACTURE OF ROSUVASTATIN CALCIUM AMORPHOUS
-
Disclosed here is a process for the preparation of amorphous Rosuvastatin calcium hydrate with high purity.
- -
-
Page/Page column 7; 8
(2019/01/22)
-
- Purification method of rosuvastatin calcium key intermediate
-
The invention provides a purification method of a rosuvastatin calcium intermediate. The rosuvastatin calcium intermediate has a structure of a compound (4). The purification method comprises following steps: adding an alcohol solvent and water into a crude product containing the compound (4), then adding an ether solvent, cooling, and crystallizing to obtain the compound (4). The structure of thecompound (4) is represented in the description. The provided purification method has the advantages of simple operation, high yield, and good selectivity, can obtain high purity rosuvastatin calciumkey intermediate, which is used to prepare high quality rosuvastatin calcium, and improves the drug quality.
- -
-
Paragraph 0053-0055
(2019/05/08)
-
- INTERMEDIATE COMPOUND FOR PREPARING ROSUVASTATIN CALCIUM AND METHOD FOR PREPARING ROSUVASTATIN CALCIUM THEREFROM
-
Provided are an intermediate compound for preparing rosuvastatin calcium and a preparation method of the rosuvastatin calcium. The method comprises: using the foregoing intermediate compound as a raw material, and subjecting the raw material to a step of Wittig reaction, a step of protecting group removal and hydrolysis and a step of calcium salt formation, so as to obtain the rosuvastatin calcium. The product, which is prepared from the intermediate compound, can be substantially enhanced in stereoselectivity and also notably improved in purity and yield; in addition, the method for preparing rosuvastatin calcium from the intermediate compound is simple, convenient and low in cost.
- -
-
Paragraph 0048
(2017/02/24)
-
- Synthesis method of chiral isomer impurities of rosuvastatin calcium
-
The invention relates to a synthesis method of chiral isomer impurities of rosuvastatin calcium. The invention finds that meso compounds IV (3R, 5R) and (3R, 5S), which are obtained after a compound III is reduced by sodium borohydride, differ greatly in chemical properties, (3R, 5S) compounds, adopting hydroxyl cis-structures, on C-3 and C-5 can be hydrolyzed in a very low-temperature alkaline environment, while (3R, 5R) compounds, adopting hydroxyl trans-structures, on the C-3 and the C-5 can be hydrolyzed at a relatively high temperature and cannot be hydrolyzed at a low temperature, and by virtue of a peculiar phenomenon, two chiral isomers of the meso compound IV are separated to obtain a target compound. The synthesis method is short in route; chiral carbon is not required to be introduced from a side chain source; the synthesis method is simple in process and easy to operate; the purity and the yield of the obtained target product are high, the purity can reach 98.8%, the yield can reach 75%, and the purity and the yield are much higher than those in the prior art; a reference substance is provided for the (3R, 5S) chiral isomer impurities of the rosuvastatin calcium; the synthesis method is of a great significance in researching the quality of the rosuvastatin calcium.
- -
-
Paragraph 0034-0036; 0042
(2017/12/27)
-
- Ruishufatatinggan known method for the preparation of impurity
-
The invention relates to a preparation method of known impurities of rosuvastatin. The preparation method comprises the following step: by taking 4-(4-fluorophenyl)-5-triphenyl phosphine bromine-6-isopropyl-2-[(N-methyl-N-methanesulfonamido)]-pyrimidine as a raw material, preparing (bis-[E-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl) amino]-pyrimidine-yl]-3R-3-hydroxyl-5-oxo-6-heptenoic acid] calcium salt through witting reaction, acidification, oxidization, alkaline hydrolysis and salt forming reaction to obtain the known impurities of rosuvastatin. The preparation method is short in synthetic line and simple to operate, and the product obtained is high in purity and can be applied to research of reference substances.
- -
-
Paragraph 0030; 0032; 0038; 0040; 0046; 0048; 0054; 0056
(2019/02/02)
-
- PROCESSES FOR THE PREPARATION OF ROSUVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
-
The present invention relates to processes for the preparation of rosuvastatin calcium of formula I and pharmaceutically acceptable salts thereof using novel intermediates, and to a pharmaceutical composition containing the same.
- -
-
Page/Page column 30
(2016/09/22)
-
- New Statin intermediate, the preparation of the same and the preparation of Rosuvastatin using the same
-
The present invention provides a novel producing method for producing a core intermediate (chemical formula IV) of rosuvastatin, a novel intermediate used therefor and a producing method of rosuvastatin hemi-calcium salts using the same. The novel intermediate of the present invention can be prepared with high purity and in high yields in mild conditions, and thus the rosuvastatin intermediate and rosuvastatin hemi-calcium salts can be conveniently and efficiently mass-produced without complicated processes.
- -
-
-
- Method for preparing of chiral intermediate and method for the preparing of HMG-CoA reductase inhibitor using chiral intermadiate
-
Chiral compounds and manufacturing method of the present invention refers to using the same manufacturing method relates to number of HMG-COa reduction inhibitors, more specifically an HMG-COa-reduction inhibitors number jaws statin compound in number of chiral intermediates that can be used a reaction steps, mild, and endangering a simple method and in high yield and purity can be under trillion number, purity statin compound is mirror number under trillion number on a commercial scale in can manufacturing method and [...] compounds using the same number of HMG-COa reduction inhibitors relates to manufacturing method. (by machine translation)
- -
-
-
- Ruishufatatinggan and wherein the intermediate preparation method
-
The invention relates to preparation methods for rosuvastatin calcium and intermediates thereof. Specifically, the invention discloses intermediate compounds for preparing rosuvastatin calcium and a preparation method of the intermediate compounds, and the intermediates are the compounds shown as formula V and formula VI. The invention also discloses a preparation method of rosuvastatin calcium or salts thereof, and the preparation method is based on the two intermediate compounds and the preparation method thereof. The preparation is simple and safe in operation, low in production cost and applicable to industrialized production.
- -
-
-
- Ruishufatatinggan and wherein the intermediate preparation method (by machine translation)
-
This invention involves a kind of Ruishufatatinggan and wherein the intermediate preparation method. In particular, the invention discloses used for preparing rosuvastatin calcium and its method for preparing intermediate compounds, the structure of the specification are as intermediates for Chinese II, formula III, formula IV, formula VI or formula VII is shown in. The invention also discloses switzerland extends down his sandbank or its salt preparation method, the method is based on the aforesaid five intermediate compound and its preparation method, the operation is simple, safe, and the production cost is low, is suitable for industrial production. (by machine translation)
- -
-
-
- Ruishufatatinggan intermediate and preparing rosuvastatin calcium intermediate and Ruishufatatinggan method (by machine translation)
-
Ruishufatatinggan intermediate and preparing rosuvastatin calcium intermediate and Ruishufatatinggan method, which belongs to the technical field of pharmaceutical organic synthesis. The present invention includes the intermediate compound rosuvastatin D, rosuvastatin F method for the preparation of intermediate compound and the use of these compounds for preparing rosuvastatin calcium method. In the invention, by adopting the above-mentioned technical means, improving the preparing rosuvastatin calcium the overall yield, greatly reduces the cost, and enhance the quality of rosuvastatin calcium. (by machine translation)
- -
-
-
- Method for the preparation of high purity Rosuvastatin Calcium salt
-
The present invention relates to a method for manufacturing a Rosuvastatin calcium salt by using a Rosuvastatin tert-butyl amine salt, and to a method for manufacturing a high purity Rosuvastatin calcium salt, which has impurities less than 0.1% of a diastereomer. The manufacturing method of a high purity Rosuvastatin calcium salt comprises the steps of: 1) manufacturing a compound represented by chemical formula III by reducing a compound represented by chemical formula IV; 2) manufacturing a compound represented by chemical formula II by adding t-butyl amine; and 3) manufacturing a compound represented by chemical formula I by adding a calcium ion to the compound represented by chemical formula II.COPYRIGHT KIPO 2016
- -
-
Paragraph 0043; 0044
(2017/01/17)
-
- NOVEL BORONATE ETHER INTERMEDIATES FOR PREPARATION OF STATIN COMPOUNDS, PREPARATION METHOD THEREOF AND PREPARATION METHOD OF STATIN COMPOUNDS USING SAID BORONATE ETHER INTERMEDIATES
-
The present invention relates to a novel boronate ether compound and a manufacturing method thereof. Provided is a novel boronate ether compound denoted by chemical formula 1 or chemical formula 2 as an intermediate to manufacture rosuvastatin calcium or pitavastatin calcium which is one of the statin based compounds to reduce the level of low density lipoprotein (LDL) of patients who have hyperlipidemia and are accordingly cured, and statin compounds with high purity are easily manufactured and separated compared with an existing patented method and are easily provided in a method of mass production.
- -
-
-
- PROCESS FOR THE PREPARATION OF ROSUVASTATIN CALCIUM AND PREPARATION OF ITS NOVEL INTERMEDIATES
-
The present invention relates to process for the preparation of 7-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidin-5-yl]-(3R,5S)-dihydroxy-(E)-6-heptenoic acid calcium having formula (I). The compound of formula (I) has adopted name "Rosuvastatin Calcium". The present invention is also related to novel intermediates of formula (4) and formula (5) used in preparation of formula (I), and process of their preparation.
- -
-
-
- AN IMPROVED PROCESS FOR THE PREPARATION OF CHIRAL DIOL SULFONES AND STATINS
-
The present invention relates to an improved process to prepare chiral diol sulfones of formula (I), wherein R1 and R2 each independently represent group selected from C1-4 alkyl, C1-4 alkenyl, C3-6 cycloalkyl, C6-10 aryl or C7-12 aralkyl, each of R1 and R2 may be substituted and wherein R1 and R2 may form a ring together with the C-atom; R3 represents group selected from C1-5 alkyl, aryl or aralkyl.
- -
-
Page/Page column 18
(2014/07/23)
-
- PROCESS FOR PREPARATION OF ROSUVASTATIN CALCIUM
-
Disclosed is the process for the preparation of 4-(fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)-5-formyl-pyrimidine of formula (I), which is the intermediate of rosuvastatin calcium. Purification of substantially pure acetonide protected tert-butyl ester of rosuvastatin (II) and its use for the preparation of substantially pure amorphous rosuvastatin calcium are also disclosed.
- -
-
Page/Page column 22-23
(2013/02/28)
-
- PROCESS FOR THE PREPARATION OF ROSUVASTATIN
-
The invention relates to a process for the preparation of a HMG - CoA reductase inhibitor such as rosuvastatin, as well as intermediates useful in such process. The invention also relates to salts of HMG-CoA reductase inhibitors and processes for preparing same as well as processes for preparing pharmaceutically acceptable salts of HMG-CoA reductase inhibitors.
- -
-
Page/Page column 41
(2010/08/08)
-
- PROCESS FOR PREPARING ROSUVASTATIN CALCIUM
-
The present invention relates to an improved process for preparing Rosuvastatin calcium of Formula I.
- -
-
Page/Page column 12-13
(2010/03/31)
-
- PROCESS FOR PREPARATION OF ROSUVASTATIN ZINC SALT
-
The subject of the present invention is an improved process for the preparation of (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3i-,55)-dihydroxy-hept-6-enoic acid zinc salt (2:1), which allows the reproducible manufacture of said compound on industrial scale in high purity. The compound of the Formula (I) can be used for the treatment of diseases related to lipid metabolism.
- -
-
Page/Page column 35-36; 38-39
(2009/05/30)
-
- PROCESS FOR PREPARATION OF PHARMACEUTICAL INTERMEDIATES
-
The present invention provides an improved process for the preparation of (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3R,5S)- dihydroxy-hept-6-enoic acid and sodium salt thereof. A further subject of the present invention is high purity (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3R,5S)-dihydroxy-hept-6-enoic acid sodium salt and process for the preparation thereof. The compound of the general Formula (I) and sodium salt thereof are valuable pharmaceutical intermediates during the production of high purity pharmaceutically active ingredients suitable for the regulation of lipid metabolism.
- -
-
Page/Page column 21-23
(2009/05/30)
-
- ROSUVASTATIN INTERMEDIATES AND THEIR PREPARATION
-
Provided are processes and intermediates for preparation of rosuvastatin.
- -
-
Page/Page column 23
(2009/03/07)
-
- AN IMPROVED PROCESS FOR PREPARATION OF ROSUVASTATIN CALCIUM
-
The present invention relates to an improved process for preparing (E)-7-[4-(4-fluorophenyl)- 6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6- enoic acid calcium of Formula (I).
- -
-
Page/Page column 21
(2008/12/08)
-
- PROCESS FOR PREPARING ROSUVASTATIN CALCIUM
-
A process for preparing amorphous rosuvastatin calcium having purity greater than 99.65% substantially free of impurities determined by area percentage of HPLC at RRT 1.26, 1.31, 1.41, 1.56, 1.71 and 3.99.
- -
-
Page/Page column 8; 9
(2008/06/13)
-
- PROCESS FOR THE SYNTHESIS OF ROSUVASTATIN CALCIUM
-
Present invention represents process for the preparation of HMG-CoA reductsase inhibitors, in particular rosuvastatin calcium introducing L-malic acid as the source of chirality for the side chain
- -
-
Page/Page column 30
(2010/11/25)
-
- PROCESS FOR PREPARATION OF ROSUVASTATIN
-
The invention relates to commercially viable process for the preparation of Rosuvastatin by an early introduction of the correct absolute stereochemistry at C-5 (S) of Rosuvastatin side chain followed by regioselective chain extension using novel side chain building blocks. It is yet another object of the invention is to provide novel intermediates that may be used for the preparation of Rosuvastatin. Formula (I).
- -
-
Page/Page column 15-16
(2008/06/13)
-
- PROCESS FOR PREPARATION OF CALCIUM SALT OF ROSUVASTATIN
-
The invention relates to commercially viable process for the preparation of Rosuvastatin by an early introduction of correct absolute stereochemistry at C-5 (S) of Rosuvastatin side chain followed by regioselective chain extension using novel side chain building blocks and less expensive reagents. It is yet another object of the invention is to provide novel intermediates that may be used for the preparation of Calcium salt of Rosuvastatin.Formula (I).
- -
-
Page/Page column 19; 20
(2010/11/24)
-
- PREPARATION OF ROSUVASTATIN
-
Provided are processes for preparing intermediates of rosuvastatin and their use in preparation of rosuvastatin and rosuvastatin salts thereof.
- -
-
Page/Page column 27-28
(2008/06/13)
-
- PROCESS FOR THE MANUFACTURE OF THE CALCIUM SALT OF ROSUVATATIN (E)-7-`4- (4-FLUOROPHENYL) -6-ISOPROPYL-2-`METHYL (METHYLSULFONYL) AMINO ! PYRIMIDIN -5-YL ! (3R, 5S) -3, 5-DIHYDROXYHEPT-6-ENOIC ACID AND CRYSTALLINE INTERMEDIATES THEREOF
-
A process for the manufacture of the calcium salt of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl (methylsulfonyl) amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid, useful as an HMGCoA reductase inhibitor, from a compound of the formula (7) wherein A is an acetal or ketal protecting group and R is alkyl, via isolated crystalline compounds of the formula (8) or of formula (10) is described. Crystalline intermediates of formulae 7, 8 and 10 are also described.
- -
-
Page/Page column 20-21
(2010/02/11)
-
- PROCESS FOR THE PREPARATION OF PYRIMIDINE DERIVATIVES
-
There is described a process for the preparation of compounds of formula (1) starting from the reaction of the compounds of formulae (24), (25) and (26) to form the compound of formula (23), wherein in each case R1, R2 and R3 are each independently of the others an unsubstituted or substituted organic radical; R4 is hydrogen, unsubstituted or substituted C1-C8alkyl, C1-C8alkoxy, phenoxy or benzyloxy, or halogen; Y1 and Y2 are each independently of the other hydrogen or a protecting group, or Y1 and Y2 together are a protecting bridge; and X1 is hydrogen, an organic radical or a cation; and also novel intermediates.
- -
-
-
