A kind of synthetic method of rosuvastatin tert-butyl ester

A technology for rosuvastatin tert-butyl ester and a synthesis method, which is applied in the field of synthesis of rosuvastatin tert-butyl ester, can solve problems such as difficulty in obtaining raw materials, difficulty in realizing industrialized production, complicated routes, etc., and achieves broad prospects and industrial application. Value, reduce waste pollution problems, easy to operate and simple effect
CN110483412BActive Publication Date: 2020-06-26ANHUI QINGYUN PHARMA & CHEM
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ANHUI QINGYUN PHARMA & CHEM
Publication Date
2020-06-26

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Abstract

The invention discloses a synthesis method of rosuvastatin tert-butyl ester. The synthesis method comprises the following steps: reacting 5-bromomethyl-4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methanesulfonyl)amino]pyrimidine with a substance A under the action of a first base catalyst to obtain a substance B; oxidizing the substance B with an oxidizing agent to obtain a substance C; then, reacting the substance C with tert-butyl (4R-Cis)-6-formyl-2,2-dimethyl-1,3-dioxane-4-acetate under the action of a second base catalyst to obtain a substance D; and finally, performing acid deprotection toobtain the rosuvastatin tert-butyl ester. The method disclosed by the invention is green and environment-friendly, mild and controllable in reaction condition, convenient and simple to operate, good in stereoselectivity and high in yield, and the prepared rosuvastatin tert-butyl ester is good in purity.
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Description

technical field

[0001] The invention relates to the technical field of chemical synthesis, in particular to a method for synthesizing rosuvastatin tert-butyl ester. Background technique

[0002] Rosuvastatin Calcium (Rosuvastatin CalciumL), a statin drug of Astra Zeneca Company, was launched in the United States in 2003 under the trade name Crestor. It has powerful HMG-CoA reductase inhibitory activity, which reduces LDL-C, increases The effect of HDL-C is better than that of other statins on the market, and it is well tolerated and safe. It is known as a "super statin".

[0003] Rosuvastatin tert-butyl ester can be hydrolyzed and salt-formed to obtain rosuvastatin calcium, so it is the key intermediate of rosuvastatin calcium, and it is of great significance to study its synthetic route. The structure of rosuvastatin tert-butyl ester is as follows Shown:

[0004]

[0005] Summarizing the existing literature reports, the current synthetic routes of rosuvastatin tert-but...

Claims

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