Improvement in Synthesis Method of the Intermediate of Rosuvastatin
Fei Shao · Fain kemikaru · 2006
Applying the Biginelli reaction,reacting 4-fluorobenzaldehyde with methyl isobutyrylacetate and thiourea in the presence of a protonic compound,then through methylation,oxidation,necleophilic substitution,reduction and oxidation,the pyrimidine aldehyde intermediate of Rosuvatatin(for reduction of cholesterol levels in patients with hypercholesterolaemia)was synthesized in 32.5% yield.Compared with the literatures,not only the synthesis step was shorten,but also the yield was improved by 14.5%.Structures of the compounds were confirmed by ~1HNMR,IR and MS.