Description
INTRODUCTION
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.
FUNCTION:
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.
FUNCTION:
A selective, competitive HMG-CoA reductase inhibitor. Antilipemic.
Product Name | Rosuvastatin calcium | |
Item | Specification | Testing result |
Appearance | White or almost white crystalline powder | White crystalline powder |
CAS# | 147098-20-2 | Conforms |
Identify | Infrared absorption spectrum should be consistent with the standard spectrum | Associated with the standard spectrum |
Water | NMT 3.0% | 2.00% |
Specific rotation | +16 - +20° | +18.5° |
Calcium | 3.5% - 4.5% | 3.80% |
Heavy metal | ≤20ppm | Conforms |
Single impurity | NMT 0.5% | 0.40% |
Total impurities | NMT 1.0% | 0.80% |
Purity | ≥99.0% | 99.20% |
Conclusion | Conformed with EP standard |