Preparation method of rosuvastatin calcium

A technology of rosuvastatin calcium and general formula, which is applied in the field of preparation of rosuvastatin calcium, can solve the problems of long process flow, low conversion rate and high cost, and achieves simplified operation procedures, high conversion rate and less impurities. Effect

Inactive Publication Date: 2015-01-21
常州金隆生物医药有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0057] From (S)-3-hydroxyl-4-chloro-butyronitrile as the starting material, although through the Reformatsky reaction, a simple method has been realized to obtain the dicarbonyl compound containing chiral hydrocarbon group, but because it belongs to the halogenated compound, the cost is still high
[0058] Therefore, in order to solve the problems of long technological process, low conversion rate and heavy pollution in the existing process, it is necessary to improve the existing preparation method of rosuvastatin calcium

Method used

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  • Preparation method of rosuvastatin calcium
  • Preparation method of rosuvastatin calcium
  • Preparation method of rosuvastatin calcium

Examples

Experimental program
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Embodiment 1

[0096] Synthesis of compound I:

[0097] Tetrahydrofuran was added to the reactor, under N 2 For protection, add NaH (60%) at room temperature under stirring; slowly add benzyl alcohol into the reactor, complete the addition within 0.5h to 1h, and stir at room temperature for 2h. At room temperature, dissolve bromoacetic acid in THF and slowly add it dropwise to the reactor, and react at 20-60°C for 16 hours after dropping. Add water to extract sodium benzyl alkoxide; add toluene to wash the water phase twice; add 5mol / L HCl to the water layer to acidify until the pH value is 3; separate the organic acid after acidification, and add toluene to the water layer to extract. The combined organic acid and toluene layers were dried, and the content was detected.

[0098] Synthesis of compound II:

[0099] The reaction process is to add 200g of benzyloxyacetic acid and 2.4L of toluene to a 5L reactor; at 20-40°C, add carbonylimidazole in one batch and stir for 0.5h. Add 100g of N...

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Abstract

The invention discloses a preparation method of rosuvastatin calcium. The preparation method comprises the following steps: 1, carrying out microbial fermentation to prepare chiral diol; 2, preparing a target chiral side chain; and 3, carrying out condensation Witting condensation on the target chiral side chain and a mother nucleus to synthesize the above calcium salt. The preparation method has the advantages of preparation flow shortening, preparation efficiency improvement, convenient quality control, convenient industrialization, raw material and energy investment reduction, cost reduction, avoiding of toxic substances, and environmental protection level improvement.

Description

technical field [0001] The invention relates to a preparation method of a calcium salt compound, in particular to a preparation method of rosuvastatin calcium. Background technique [0002] Rosuvastatin calcium is an aminopyrimidine derivative developed and screened by Shionogi Pharmaceutical Co., Ltd. in Japan in the late 1980s. After that, As-traZeneca developed a new generation of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors worldwide except Japan and other East Asian countries. It was launched in February 2003 Launched in Canada for the first time, the general name is Rosuvastatin calcium. According to the homonym of INN, it is named Rosuvastatin calcium, and the product name is Crestor. This product has the effect of lowering LDC-C and raising HDL-C, which is better than other statins on the market. It has good tolerance and safety, and is known as "super statin". Recently, AstraZeneca's rosuvastatin calcium has been approved by the FDA for new...

Claims

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Application Information

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IPC IPC(8): C12P17/12C12P7/62C07D239/42
Inventor 杨敏
Owner 常州金隆生物医药有限公司
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