Rosuvastatin, one of the two new statins launched for the treatment of hypercholesterolemia, has high hepato-selectivity and more potent inhibitory effect on HMG-CoA reductase than the previously marketed statins. In rat hepatocytes, it inhibits cholesterol biosynthesis with an IC50 of 1.12 nM, which is ~100-fold higher potency than pravastatin. Rosuvastatin is synthesized in a 12-step sequence, entailing the construction of a pyrimidinyl aldehyde intermediate in eight steps and subsequent introduction of the dihydroxyheptenoate side chain via Wittig reaction with a bketophosphorane reagent and stereoselective carbonyl reduction of the resultant enone.
A selective, competitive HMG-CoA reductase inhibitor. Antilipemic.
White or almost white crystalline powder
White crystalline powder
Infrared absorption spectrum should be consistent with the standard spectrum