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Preparation method of atorvastatin calcium

A technology of atorvastatin calcium and methyl group, applied in the field of pharmaceutical preparation, can solve problems such as inability to realize industrial application, complicated operation, etc., achieve good practical value and promotion and application significance, good repeatability, and good industrial application prospect Effect

Active Publication Date: 2018-06-29
TOPFOND PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The purpose of this application is to provide a relatively new method for the preparation of atorvastatin calcium, so as to partially solve the disadvantages of the existing preparation technology, such as complex operation or inability to realize industrial application

Method used

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  • Preparation method of atorvastatin calcium

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Experimental program
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Effect test

Embodiment

[0043] The preparation method of atorvastatin calcium provided in this embodiment, the specific process is introduced as follows.

[0044] (1) Preparation of 2-methyl-3-carbonyl-pentanoic acid methyl ester

[0045] Using dimethyl carbonate and 3-methyl-2-butanone (methyl isopropyl ketone) as raw materials, 2-methyl-3-carbonyl-pentanoic acid methyl ester (first intermediate); the reaction scheme is as follows:

[0046] .

[0047] in particular:

[0048] Use a 500mL reaction flask with a thermometer and a stirrer as a reaction vessel, add 30g (0.333mol) of dimethyl carbonate (0.333mol) and 3-methyl-2-butanone (0.35mol), add 200mL of solvent THF, and then add the 1. Catalyst: Potassium tert-butoxide 38g (0.34mol), under nitrogen atmosphere, react at 60°C for 8h;

[0049] After the reaction, cool down to room temperature, adjust to neutral with dilute hydrochloric acid, concentrate under reduced pressure, add 300 mL of saturated sodium chloride solution, and extract three ti...

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Abstract

The invention belongs to the technical field of medicine preparation and particularly relates to a patent application about a novel preparation method of atorvastatin calcium. The method includes steps of preparing intermediates including: 2-methyl-3-carbonyl-methyl pentanoate, 2-methyl-3,5-dicarbonyl-5-anilino-butane, 4-methyl-3-oxo-N-phenyl-2-benzylidene pentanamide, 4-(4-fluorophenyl)-2-(2-methylpropionyl)-4-oxo-N-beta-diphenyl butyrylamide. The preparation method employs cheap and easy-to-obtained raw materials, has simple reactions and operations, and has great industrial application prospect. In conclusion, the preparation method has high reaction efficiency and product yield, is good in repeatability, is suitable for industrial production and has great application value and promotion and application significance.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and specifically relates to a patent application for a novel preparation method of atorvastatin calcium. Background technique [0002] Atorvastatin calcium is a powerful lipid-lowering drug launched by Pfizer in 1997. It is a drug that can simultaneously reduce total cholesterol and triglycerides. It belongs to 3-hydroxy-3-methyl - glutaryl-coenzyme A (HMG-CoA) reductase inhibitors. Since atorvastatin calcium is suitable for the simultaneous treatment of the increase of total cholesterol and triglycerides, in 2008, the American College of Cardiology and the Stroke Society recommended in the Guidelines for the Secondary Prevention of Ischemic Stroke and Transient Ischemic Attack The use of statins to strengthen lipid-lowering, and atorvastatin is recommended emphatically, which further establishes its status as a major drug with a large variety and a long market cycle. Since 2002, a...

Claims

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Application Information

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IPC IPC(8): C07D207/34
CPCC07D207/34
Inventor 樊振刘玮周新建吴相永刘宁宇任真王俊臣张忠理吕兰亭李青丽卢廷贵
Owner TOPFOND PHARMA CO LTD
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