ChemicalBook CAS DataBase List (Intermediates of Rosuvastatin Calcium R-4

(Intermediates of Rosuvastatin Calcium R-4 synthesis

7synthesis methods

Product Name:(Intermediates of Rosuvastatin Calcium R-4
CAS Number:851440-19-2
Molecular formula:C26H34FN3O6S
Molecular Weight:535.63

tert-Butyl 6-[(1E)-2-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]ethenyl]-2,2-dimethyl-1,3-dioxane-4-acetate

289042-12-2
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(Intermediates of Rosuvastatin Calcium R-4

851440-19-2
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Yield:851440-19-2 87%

Reaction Conditions:

with titanium(IV) isopropylate in methanol; for 32 h;Reflux;

Steps:

2 The second step, and then esterification of (E) - ({2- [4- (fluorophenyl) -6-isopropyl-2- [methyl (methanesulfonyl) amino] pyrimidin-5-yl] vinyl yl} (4R, 6S) -2,2- dimethyl [1,3] dioxane-4-yl) methyl ester

Previous to give 108 g (0.1867 mol) of the product was added 1L of methanol and 5 grams of tetraisopropyl titanate was heated to reflux for 16 hours, the methanol was removed by vacuum distillation. 1L fresh methanol and then added 5g tetraisopropyl titanate was heated under reflux for 8 hours, distilling off methanol, 1L fresh methanol and 5g tetraisopropyl titanate was heated under reflux for 8 hours, so you can get the conversion rate of over 98% . Methanol was distilled off, 300ml of isopropanol was added and the distillation continued directly from the residue crystallized fresh isopropanol, 87g of the finally obtained (theoretical yield 87%) of product, the HPLC purity was 98.9%.

References:

CN105461636,2016,A Location in patent:Paragraph 0054;0055