The Research On The Synthesis And Quality Of Rosuvastatin Calcium

Rosuvastatin calcium,which chemical name is(+)-(3R,5S)-bis{7-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulphonylamino)-pyrimidin-5-yl]-3,5-dihydroxy-6-(e)-heptenoic acid} calcium,and the trader name as crestor,is a drug used to treat cardiovascular diseases.Crestor was developed by Shionogi in Japan,and was first marketed in United States in 2003.Rosuvastatin calcium is synthesized from raw material(4R-cis)-6-[(acetyloxy)methyl]-2,2_dimethyl-1,3_dioxane-4_acetic acid-1,1-dimethylethyl ester through the reaction of esterolysis and Swern oxidation to obtain the side chain aldehyde.The side chain aldehyde was reacted through Wittig condensation,deprotection and esterolysis,and finally transformed into calcium salt.The work of characterization of Rosuvastatin calcium has been performed.This work covered the optimization of the synthesis technology and the research work on quality with the requirements from regulatory affairs.The optimization of the parameters has been conducted with each step.The specification and impurity profile has been established.And the analytical method has been fully validated with the comply of the reuirements of regulatory affairs.