503610-43-3Relevant articles and documents
Preparation method of rosuvastatin calcium
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, (2019/07/05)
The invention provides a preparation method of rosuvastatin calcium. A rosuvastatin calcium side chain is prepared by using allene as a raw material and is used to synthesize rosuvastatin calcium. According to the method, a hydrogen peroxide-heteropoly acid oxidation system is used to oxidize the side chain from olefin to aldehyde, thereby avoiding harsh conditions of low-temperature reaction in the prior art and being more beneficial to industrial production.
Synthesis method of rosuvastatin calcium
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Paragraph 0056-0058, (2019/06/30)
The invention provides a synthesis method of rosuvastatin calcium. Allene is taken as the raw material to prepare a bi-molecular rosuvastatin calcium side-chain intermediate. Bi-molecular allene and cyclohexanedione carry out reactions to form the bi-molecular side chain intermediate. Due to steric hindrance, in Wittig reactions, the conversion of the intermediate into cis-rosuvastatin calcium isprevented, thus the optical purity of rosuvastatin calcium is increase effectively, the product barely contains cis-rosuvastatin calcium, and moreover, the synthesis method does not a severe low temperature condition and is more suitable for industrial production.
Palladium-Catalyzed Stereoselective Cyclization of in Situ Formed Allenyl Hemiacetals: Synthesis of Rosuvastatin and Pitavastatin
Spreider, Pierre A.,Breit, Bernhard
, p. 3286 - 3290 (2018/06/11)
A diastereoselective palladium-catalyzed cyclization of allenyl hemiacetals is described. It permits the selective synthesis of 1,3-dioxane derivatives, precursors for syn-configured 1,3-diols which make an appearance in all of the statin representatives. The reaction allows the total synthesis of Rosuvastatin and Pitavastatin in a straightforward fashion.
NOVEL CLASS OF COMPOUNDS FOR THE TREATMENT OF CARDIOVASCULAR DISEASE
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Page/Page column 41, (2017/09/05)
The present invention relates to the field of medicine, specifically the field of treatment and prevention of cardiovascular diseases.
ROSUVASTATIN CALCIUM AND PROCESS FOR PRODUCING INTERMEDIATE THEREOF
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Paragraph 0490; 0491, (2016/12/22)
An object of the present invention is to provide a novel method capable of producing rosuvastatin calcium and intermediates therefor efficiently, inexpensively and with high purity. The present invention provides a method of efficiently producing rosuvastatin calcium and intermediates therefor having a high purity at an industrial scale, without using an extremely low temperature reaction or a special asymmetric catalyst.
PROCESS FOR THE PREPARATION OF STATINS IN THE PRESENCE OF BASE
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, (2013/11/19)
The present invention relates to a process for the preparation of statins by means of a Julia-Kocienski reaction between an aldehyde and a sulfone derivative in the presence of an alkaline metal alkoxy base. The resulting derivatives are suitable as building blocks for statin type compounds such as cerivastatin, fluvastatin, pitavastatin and rosuvastatin.
PROCESS FOR THE PREPARATION OF HMG-COA REDUCTASE INHIBITORS AND INTERMEDIATES THEREOF
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, (2012/01/14)
The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvasatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2-N-O-R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof.
PROCESS FOR THE PREPARATION OF STATINS IN THE PRESENCE OF BASE
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, (2012/08/07)
The present invention relates to a process for the preparation of statins by means of a Julia-Kocienski reaction between an aldehyde and a sulfone derivative in the presence of an alkaline metal alkoxy base. The resulting derivatives are suitable as building blocks for statin type compounds such as cerivastatin, fluvastatin, pitavastatin and rosuvastatin.
Process for the preparation of key intermediates for the synthesis of rosuvastatin or pharmaceutically acceptable salts thereof
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Page/Page column 12, (2011/07/06)
The present invention relates in general to the field of organic chemistry and in particular to a process for the preparation of 5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVL) as well as a process for preparing crystalline 5-((E)-2-((2S,4R)-4-(tert-butyldimethylsilyloxy)-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVLTBS) useful as key intermediates for the preparation of rosuvastatin or pharmaceutically acceptable salts thereof.
PROCESS FOR THE PREPARATION OF KEY INTERMEDIATES FOR THE SYNTHESIS OF ROSUVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
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Page/Page column 19; 20, (2011/07/07)
The present invention relates in general to the field of organic chemistry and in particular to a process for the preparation of 5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVL) as well as a process for preparing crystalline 5-((E)-2-((2S,4R)-4-(tert-butyldimethylsilyloxy)-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVLTBS) useful as key intermediates for the preparation of rosuvastatin or pharmaceutically acceptable salts thereof.