- New Statin intermediate, the preparation of the same and the preparation of Rosuvastatin using the same
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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.
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Paragraph 0139; 0145-0147
(2017/04/20)
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- PROCESS FOR THE PREPARATION OF ROSUVASTATIN
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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.
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Page/Page column 38
(2010/08/08)
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- NOVEL PROCESS FOR STEREOSELECTIVE REDUCTION OF ?-KETOESTERS
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A novel process for the preparation of compounds of formula (I): R1 = CN, OP (P=any suitable protecting group), alkyl, aryl or hetroaryl, R2 = Alkyl or aryl by reacting a compound of formula (II): R1 = CN, OP (P=any suitable protecting group), alkyl, aryl or hetroaryl, R2 = Alkyl or aryl with a reducing agent, sodium borohydride in presence of metal halides, preferably CeC13 or metal alkoxides, preferably Ti(OiPr)4.
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- 2,4,6-substituted phenol derivatives
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A 2,4,6-substituted phenol having the formula (I): STR1 wherein X is S or CH2 ; R1 and R2 are the same or different from each other and each is a lower alkyl group; R3 is a group of the formula: STR2 in which R4 is hydrogen atom or a lower alkyl group; R5 and R6 are the same or different from each other and each is hydrogen atom, a lower alkyl group, or a phenyl group which may be substituted, or a pharmaceutically acceptable salt thereof is useful as an active agent in a pharmaceutical composition. The pharmaceutical composition comprises a therapeutically effective amount of a compound having the formula (I), as an effective ingredient, in association with a pharmaceutically acceptable substantially nontoxic carrier or excipient. The pharmaceutical composition can be useful in the treatment of lipemia of mammals. Additionally the compounds can be used as antiatherosclerotic agents and antilipenic agents.
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- Stereoselective synthesis of HR 780 a new highly potent HMG-CoA reductase inhibitor
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HR 780 (1) a new HMG-CoA reductase inhibitor has been synthesized stereoselectively starting from L-malic acid. Wittig olefination employing phosphonium halides, phosphonates and phosphane oxides have been investigated.
- Wess,Kesseler,Baader,Bartmann,Beck,Bergmann,Jendralla,Bock,Holzstein,Kleine,Schnierer
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p. 2545 - 2548
(2007/10/02)
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