Patent ID: 8049010

Claim:
A method for synthesizing an intermediate of rosuvastatin calcium, using 4-4′-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidine-5-formaldehyde as raw material, comprising: a) reacting the raw material with a nitrilized reagent in an organic solvent to produce an intermediate I, 4-4′-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidine-5-acrylonitrile; b) reacting the intermediate I with a reductant to produce an intermediate II, 4-4′-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidine-5-acraldehyde; c) reacting the intermediate II with 1,3-bis(trimethyl siloxane)-1-ethoxy-1,3-butadiene to produce an intermediate III, 7-[4-4′-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidine-5-yl]-3-oxo-(5R)-5-hydroxy-(E)-6-ethyl heptenoate, wherein the reaction comprises: dissolving the intermediate II in tetrahydrofuran, protecting the intermediate II with an inert gas; adding dinaphthol, isopropyl titanate, and tetramethyl ethylene diamine as catalysts; adding 1,3-bis(trimethyl siloxane)-1-ethoxy-1,3-butadiene after agitating to uniformity, and reacting for 2-4 hours at 20-35° C.; and d) reacting the intermediate III with an reductant to produce an intermediate IV, 7-[4-4′-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidine-5-yl]-(3R,5S)-dihydroxy-(E)-6-ethyl heptenoate.