| Commonly used cholesterol-lowering drugs |
Fluvastatin sodium salt is commonly used as a cholesterol-lowering drug, cholesterol-lowering effect is very good, the trade name of the commercially available products is Lescol,which is produced by Novartis. Fluvastatin sodium salt is a fully synthetic cholesterol-lowering drug, it belongs to methylglutaryl coenzyme A (HMC-CoA) reductase inhibitors, the main function is performed in the liver ,it can transform HMG-CoA into 3-methyl-3,5-dihydroxy acid, it can inhibit the synthesis of endogenous cholesterol ,and reduce cholesterol content in liver cells, it can stimulate the synthesis of low density lipoprotein (LDL) receptors,and enhance the uptake of LDL particles, reduce the plasma total cholesterol concentration.it can significantly reduce total cholesterol, LDL cholesterol, triglycerides, and increase high-density lipoprotein cholesterol.
The above information is edited by the chemicalbook of Tian Ye. |
| Chemical Properties |
Melting point 194~197 ℃. |
| Uses |
HMG-CoA reductase inhibitors. |
| production method |
1. After condensation of (chloroacetyl) fluorobenzeneand N-isopropyl aniline , the compound (I) is obtained. Then in acetonitrile, under the presence of phosphorus oxychloride, react with N, N-dimethylamino acrolein , the compound (Ⅱ) is obtained. Compound (Ⅱ) in the role of a strong base, after condensation with methyl acetoacetate , and then splitting ,the compound (Ⅲ) is produced. At-77 ~-74 ℃, the compound (Ⅲ) is added dropwise into a mixture of boron sodium borohydride , methanol, tetrahydrofuran and diethyl methoxy ,stir 30min; cyclic boronic ester obtained in ethyl acetate is treated with 30% hydrogen peroxide; then it is hydrolyzed to obtain fluvastatin sodium.
2. the compound (Ⅳ)is obtained by catalytic hydrogenation of Phloroglucinol . React it With tert-butyldiphenylsilyl chloride to produce the compound (V), and then oxidize it to generate (Ⅵ). After oxidation of chloroperbenzoic acid to obtain (Ⅶ), (Ⅷ) is produced through ring-opening . And then it is oxidized to (IX) . (Ⅺ) is obtained through condensation of (Ⅸ) and intermediate x , after deprotection and hydrolysis, obtain fluvastatin sodium. Intermediate (X) can be made through starting from the compound (I), via formylation, reduction, chlorination, and then reacting with triphenylphosphine . |
| Chemical Properties |
Yellow Powder |
| Uses |
A synthetic HMG-CoA reductase inhibitor. Antilipemic |
| Uses |
Anti- hyperlipoproteinemic;'HMG CoA reductase inhibitor |
| Biological Activity |
Orally active, potent and competitive HMG-CoA reductase inhibitor (IC 50 = 40 -100 nM at human liver microsomes). Inhibits vascular smooth muscle proliferation in vitro (IC 50 = 70 nM) and exhibits antihypercholesterolemic and antioxidant activity in vivo . |
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