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Preparation method of atorvastatin calcium

A technology of atorvastatin calcium and atorvastatin method, which is applied in the field of preparation of atorvastatin calcium, can solve the problems of expensive raw materials and high synthesis costs, and achieve the advantages of easy-to-obtain raw materials, high synthesis yield, and low-cost raw materials Effect

Inactive Publication Date: 2010-08-18
SHAOXING MINSHENG PHARMA +1
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Problems solved by technology

[0005] The synthetic route of atorvastatin calcium disclosed in U.S. Patent No. 5,273,995 is to introduce the first chiral center through raw materials, and the second chiral center is obtained through substrate induction, see Chemical Equation 1, but the patent introduces chiral The raw material is not a natural product, and the synthesis cost is high because the price of the raw material is very expensive

Method used

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  • Preparation method of atorvastatin calcium
  • Preparation method of atorvastatin calcium
  • Preparation method of atorvastatin calcium

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Embodiment Construction

[0033] In this example, in order to overcome the deficiencies of the prior art, atorvastatin calcium was synthesized using cheap and easily available natural products as raw materials. The preparation method of atorvastatin calcium is: synthesize the main ring fragment and the side chain fragment respectively, and then concatenate them to form the target product. The difference in chain fragments makes the process of connecting side chains and main rings and then synthesizing atorvastatin calcium different from the existing methods. The specific method is:

[0034] Synthesis of A main loop fragment

[0035] 1) Synthesis of methyl isobutyryl acetate (compound of formula 2) (see chemical equation 6),

[0036]

[0037] Chemical Equation 6

[0038] In a dry 250mL round bottom flask, add 0.20mol sodium hydride, add 150mL benzene, 16.6mL (0.12mol) dimethyl carbonate, and heat until the reaction liquid is refluxed. Add 50mL of benzene solution containing 5.727g (75mmol) of met...

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Abstract

The invention discloses a preparation method of atorvastatin calcium, which comprises the steps of: firstly, synthesizing a primary ring segment compound of the atorvastatin calcium in the formula 5, and simultaneously synthesizing a side chain segment compound in the formula 16; carrying out pyrrole cyclization reaction on the primary ring segment compound in the formula 5and the side chain segment compound in the formula 16 to obtain a connecting intermediate compound in the formula 17; removing protective groups of the compound in the formula 17, carrying out saponification on ester groups of the compound in the formula 17 to obtain sodium salt compound in the formula 18 of the atorvastatin; and adding a calcium chloride water solution in a water solution of the compound in the formula 18 to be filtered to obtain the atorvastatin calcium. The invention has easy obtaining and low cost of the raw materials and higher synthesis yield, and can overcome the defects of the prior art.

Description

technical field [0001] The invention relates to a preparation method of atorvastatin calcium. Background technique [0002] Statins are hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitors, which block the endogenous cholesterol synthesis rate-limiting enzyme (HMG-CoA) reductase by competitively inhibiting The metabolic pathway of intracellular valonate reduces the synthesis of cholesterol in the cell, thereby stimulating the increase in the number and activity of low-density lipoprotein (LDL) receptors on the surface of the cell membrane (mainly liver cells) and clearing serum cholesterol. increase, decrease in level. Statins can also inhibit the synthesis of apolipoprotein B-100 in the liver, thereby reducing the synthesis and secretion of triglyceride-rich AV and lipoproteins. Statins are known as "miracle drugs" in the medical world. Medical experts agree that the role of statins in the prevention and treatment of coronary heart disease is no less than that...

Claims

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Application Information

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IPC IPC(8): C07D207/34
CPCY02P20/55
Inventor 李瀛程文张宪恕薛吉军张涛
Owner SHAOXING MINSHENG PHARMA
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