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Novel method for preparing rosuvastatin calcium

A technology of rosuvastatin calcium and a new method, applied in the direction of organic chemistry, etc., can solve the problems of different lipid-lowering properties, and achieve the effects of simple synthesis, simple three-waste treatment, and strong operability

Inactive Publication Date: 2011-01-19
刘璟凌
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  • Summary
  • Abstract
  • Description
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  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although this product has the dihydroxyheptanoic acid part of the pharmacophore shared by statins, the rest of the structure in the molecule is quite different from other similar drugs, so the lipid-lowering performance is also different.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0009] Further describe the total synthesis of rosuvastatin calcium by the following examples

[0010] 1. Synthesis of 4-(4-fluorophenyl)-6-isopropyl-5-methoxycarbonyl-3,4-2(1H)-dihydropyrimidinone (L)

[0011] Add p-fluorobenzaldehyde (500g), methyl isobutyrylacetate (860g), urea 200g, cuprous chloride, methanol, sulfuric acid into the reaction kettle, and heat to reflux. Cool in an ice-water bath, continue to stir, and then filter with suction. The obtained solid is rinsed with methanol and dried in a drying oven to obtain 1460.17 g of white crystals, with a yield of 98.7%.

[0012] 2. Synthesis of [4-(4-fluorophenyl)-2-hydroxyl-6-isopropyl-5-methoxycarbonylpyrimidine (II)

[0013] Add 65-68% nitric acid and sodium nitrite into the reaction kettle, add intermediate I in batches at 10-25°C, and continue to react at 10-20°C, and the reaction is complete by TLC detection. Add water to the reaction solution, then add dropwise sodium hydroxide solution to adjust the pH, and pay...

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PUM

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Abstract

The invention discloses a novel method for preparing rosuvastatin calcium, which is characterized by comprising the following steps of: performing a series of reactions such as condensation, oxidation, reduction and substitution on fluorobenzaldehydes, methyl isobutyrylacetate, urea and cuprous chloride serving as raw materials to finally obtain the final product rosuvastatin calcium. The method is an economic, safe, high-purity and high-yield route, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a new method for preparing rosuvastatin calcium. Background technique [0002] Background technology of the present invention is as follows: [0003] Rosuvastatin calcium is a third-generation statin drug with a fully synthesized single enantiomer, which belongs to HMG-CoA reductase inhibitors, and can reduce elevated low-density cholesterol, total cholesterol, triglycerides and aposthesia Protein B concentration, while increasing the concentration of high-density cholesterol. It can be used for comprehensive treatment of primary hypercholesterolemia, mixed lipodystrophy and homozygous familial hypercholesterolemia. [0004] Although this product has the dihydroxyheptanoic acid part of the pharmacophore shared by statins, the rest of the structure in the molecule is quite different from other similar drugs, so the lipid-lowering performance is also different. A la...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/42
Inventor 刘璟凌朱华荣
Owner 刘璟凌