- A process for preparing rosuvastatin calcium intermediate method
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The invention relates to a method for preparing a rosuvastatin calcium intermediate, in particular to a preparation method for a compound shown in the formula 3. According to the method, ethyl (R)-(-)-4-cyano-3-hydroxybutyate is mainly used as an initial material for performing a hydroxyl protecting reaction and then the esterification reaction is performed, so that the target product is prepared. The preparation method provided by the invention is simple in operation, less in reaction steps and greatly reduces production cost; moreover, the rosuvastatin calcium intermediate is high in purity and yield, and stable in quality and has a wide prospect in the industrial application.(shown in the specification).
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Paragraph 0039-0040; 0045-0046
(2017/08/15)
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- DOSY NMR for monitoring self aggregation of bifunctional organocatalysts: Increasing enantioselectivity with decreasing catalyst concentration
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In this report, we demonstrate that self-aggregation is an intrinsic problem of bifunctional organocatalysts, especially in the case when the substrates do not have functional groups which are able to bind strongly with catalyst. Due to their self-associa
- Jang, Hyeong Bin,Rho, Ho Sik,Oh, Joong Suk,Nam, Eun Hye,Park, Sang Eun,Bae, Han Yong,Song, Choong Eui
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scheme or table
p. 3918 - 3922
(2010/09/17)
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- PROCESS AND INTERMEDIATES FOR THE SELECTIVE SYNTHESIS OF FLUVASTATIN
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The invention relates to process for the selective preparation of 3-hydroxy-6-dialkoxyphosphoryl-5-oxo-hexanoic acid esters, comprising a first step, in which a methylphosphonic acid dialkylester is treated with a base, and a second step, in which the pro
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Page/Page column 7
(2010/10/20)
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- Optical resolution of 3-(silyloxy)glutaric acid half esters and their utilization for enantioconvergent synthesis of a HMG-CoA reductase inhibitor
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Useful chiral synthons, (3R)- and (3S)-[(tert- butyldimethylsilyl)oxy]pentanedioic acid monomethyl ester, (R)-1 and (S)-1, were obtained by optical resolution of a racemic mixture of 1. Sulfoxide 8 has been developed from (S)-1 as a new building block for preparing HMG-CoA reductase inhibitors. Two alternate chiral synthons 2 and 8, synthesized from (R)-1 and (S)-1, respectively, were employed for enantioconvergent synthesis of potent inhibitor 15 containing a pyrrole moiety.
- Konoike, Toshiro,Okada, Tetsuo,Araki, Yoshitaka
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p. 3037 - 3040
(2007/10/03)
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- 3-Hydroxyglutarate and β,γ-Epoxy Esters as Substrates for Pig Liver Esterase (PLE) and α-Chymotrypsin
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The pH dependence of the α-chymotrypsin-catalyzed hydrolysis of dimethyl 3-hydroxyglutarate (3) has been studied.The e.e. was determined by HPLC analysis of diastereoisomeric camphanoic-acid derivatives.Kinetic resolution of the β,γ-epoxy esters 10 and 24 by pig liver esterase has been shown to provide an alternative access to chiral β-hydroxy esters and acids of high optical purity.By this latter method, the unnatural enantiomer of γ-amino-β-hydroxybutyric acid (GABOB) has been sinthesized.Finally, dimethyl meso-3,4-epoxyadipate (19) was hydrolyzed by pig liver esterase with almost 100 percent selectivity.
- Mohr, Peter,Roesslein, Lukas,Tamm, Christoph
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p. 142 - 152
(2007/10/02)
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