Method for preparing atorvastatin calcium

A technology of atorvastatin calcium and compounds, which is applied in the field of preparation of atorvastatin calcium, can solve the problems of high cost of atorvastatin calcium, high cost of compound 3, and difficult synthesis, and achieves cheap raw materials, mild reaction conditions, and easy separation simple effect

Active Publication Date: 2012-08-01
湖南欧亚药业有限公司
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Problems solved by technology

Due to the presence of two chiral centers in the synthesis of compound 3, ultra-low temperature -78°C and a very active strong base n-butyllithium are often used in the synthesis, so the synthesis of compound 3 is difficult and expensive
The biggest problem of this type of method is that the yield of Paal-Knorr reaction is generally 50-80%, and the cost of compound 3 is high, so the cost of atorvastatin calcium will also be high by using this type of route

Method used

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  • Method for preparing atorvastatin calcium
  • Method for preparing atorvastatin calcium
  • Method for preparing atorvastatin calcium

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Embodiment Construction

[0043]In order to make the technical means, creative features, work flow, and use methods of the present invention achieve the purpose and effect easily understood, the present invention will be further described below in conjunction with specific embodiments.

[0044] Synthesis of Compound II:

[0045] Add 608 grams of benzene (8.00mol) into the reaction flask, stir, cool to 0°C, add 160.2 grams of anhydrous aluminum trichloride (1.20mol), and slowly add 172.5 grams of 4-fluorophenylethyl Acyl chloride (1.00mol), after the dropwise addition, return to room temperature and react for 1 hour, then raise the temperature to 50°C and react for 10 hours. After the reaction, the reaction solution is cooled to room temperature, poured into 1200 ml of ice water, and added with 200 ml of 3N hydrochloric acid while stirring , the reaction solution was separated, the aqueous layer was extracted with benzene, the organic layers were combined, washed successively with 3N hydrochloric acid, ...

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Abstract

The invention discloses a method for preparing atorvastatin calcium. According to the method, a pyrrole ring is synthesized by performing Hantzsch reaction on a compound III and ethyl isobutyrylacetate; reaction conditions of a compound VI and a compound VII are mild; and a methanol-anhydrous calcium chloride system is adopted when calcium salt is generated, and atorvastatin calcium is generated finally. A product is high in purity and safety factor, energy consumption is low, yield is high, the reaction conditions are relatively mild, and separation is easy to realize.

Description

technical field [0001] The invention relates to a synthesis method of a compound, in particular to a preparation method of atorvastatin calcium. Background technique [0002] Statins are currently the world's best-selling blood lipid-lowering drugs and are HMG-CoA reductase inhibitors. Atorvastatin Calcium (Atorvastatin Calcium) is the drug with the fastest growth and the highest sales among blood lipid-lowering drugs in the world. The Chinese chemical name of atorvastatin calcium is: 7-[2-(4-fluorophenyl)-3-phenyl-4-(anilinoformyl)-5-(2-propyl)pyrrol-1-yl Calcium ]-3,5-dihydroxyheptanoate; [R,(R*,R*)]-2-(4-fluorophenyl)-β,α-dihydroxy-5-(1-methylethyl )-3-phenyl-[(anilino)-hydroxyl]-1H-pyrrole-1-heptanoic acid calcium salt, its structural formula is: [0003] [0004] I [0005] The synthesis of atorvastatin calcium reported in the literature can be represented by the following reaction equation: [0006] [0007] 3 [0008] [0009] 4 Ⅰ [0010] P1 and P2 a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/34
Inventor 林开朝
Owner 湖南欧亚药业有限公司
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