- Palladium-Catalyzed Stereoselective Cyclization of in Situ Formed Allenyl Hemiacetals: Synthesis of Rosuvastatin and Pitavastatin
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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.
- Spreider, Pierre A.,Breit, Bernhard
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supporting information
p. 3286 - 3290
(2018/06/11)
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- A method for preparing a rosuvastatin calcium intermediate
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The invention relates to the technical field of pharmaceutical chemistry, particularly the field of process optimization and cost control for pharmaceutical intermediate preparation, and more particularly relates to an impurity in preparation of a rosuvastatin calcium intermediate and a method for synthesizing the intermediate from the impurity. A compound I' is reacted with ozone and a reductantto obtain a compound IV and an important intermediate III, the compound IV is further subjected to reduction and substitution to prepare another intermediate II important in preparation of the rosuvastatin calcium intermediate, and the compound II and the compound III are adopted to prepare an intermediate compound I. Through recovery and utilization of the impurity compound I', the preparation cost of the compound I is significantly reduced. The method is simple in process and suitable for industrial large-scale production.
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Paragraph 0025
(2019/01/08)
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- PROCESS FOR THE PREPARATION OF HMG-COA REDUCTASE INHIBITORS AND INTERMEDIATES THEREOF
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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.
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Page/Page column 20
(2012/01/14)
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- PROCESS FOR THE PREPARATION OF PYRIMIDINE DERIVATIVES
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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.
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- Process for the production of tert-butyl (E)-(6-[2-[4-(-flourophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]vinyl](4R,6S)-2, 2-dimethyl[1, 3]oioxan-4yl)acetace
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The invention concerns a process for the manufacture of tert-butyl (E)-(6-[2-4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]vinyl}-(4R, 6S)-2,2-dimethyl[1,3-dioxan-4-yl) acetate, the novel starting material used in said process and the use of the process in the manufacture of a pharmaceutical.
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- Crystalline salts of 7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]-(3r,5s)-3,5-dihydroxyhept-6-enoic acid
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The invention relates to crystalline salts of the compound (E)-7-[4-(4-fluorophenyl)-6-iso-propyl-2-[methyl(methyl-sulfonyl)amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid of formula (I),as well as processes for their manufacture, pharmaceutical compositions containing them, and their uses.
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- Process for preparing N-[5-(diphenylphosphinoylmethyl)-4-(4-fluorophenyl)-6-isopropylpyrimidin-2-yl]-N-methylmethanesulfonamide
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N-[5-(Diphenylphosphinoylmethyl)-4-(4-fluorophenyl)-6-isopropylpyrimidin-2-yl]-N-methylmethanesulfonamide of the formula: is prepared by reaction of [4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidin-5-yl]methanol with chlorodiphe
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