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Preparation method of rosuvastatin intermediate

A technology for rosuvastatin and intermediates, applied in the field of intermediate synthesis, can solve the problems of harsh reaction conditions, complicated separation, low temperature, etc., and achieve the effects of easy-to-obtain raw materials, high yield, and mild reaction conditions

Inactive Publication Date: 2017-02-15
HUBEI XIANGYUN GROUP CHEM
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Problems solved by technology

The reaction conditions of the two are harsh, both are under low temperature conditions and both need nitrogen protection; Z7 reacts with phosphorus tribromide to synthesize Z8.1. (below 0°C), complicated separation and low yield (91.2%); then Z8.1 was reacted with diphenylethoxyphosphine to synthesize Z9, the mother nucleus of rosuvastatin

Method used

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  • Preparation method of rosuvastatin intermediate
  • Preparation method of rosuvastatin intermediate

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Embodiment Construction

[0020] In order to make the object, technical solution and advantages of the present invention clearer, the present invention will be further described in detail below.

[0021] This embodiment provides the preparation method of rosuvastatin intermediate z9, comprising the following steps:

[0022] One: Synthesis of Z7

[0023]

[0024] The average single batch is 94.3g, the HPLC content is 99.6%, and the yield is 85.7%.

[0025] Two: Synthesis of Z8.1

[0026]

[0027] The reaction time is 6 hours, the reaction temperature is 10-50°C, and the solvent is CHCl 3 .

[0028] Three: Synthesis of Z9

[0029]

[0030] The reaction time is 10 hours, the reaction temperature is 40-100° C., and the solvent is toluene.

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Abstract

The invention discloses a preparation method of a rosuvastatin intermediate, and belongs to the technical field of intermediates. The method comprises the following steps: carrying out a reduction reaction on Z6, KBH4 and a Lewis acid in an organic solvent at 60-100 DEG C to obtain Z7, wherein a mass ratio of the Z6 to KBH4 to the Lewis acid is (105-130):(50-60):(50-70); carrying out a reaction on the Z7 and phosphorous tribromide in an organic solvent at 10-50 DEG C to obtain Z8.1, wherein a mass ratio of the Z7 to phosphorous tribromide is 1:(1-1.3), and the organic solvent is C1-C3 halogenated hydrocarbon; and carrying out a reaction on the Z8.1 and ethyl diphenylphosphinite in an organic solvent at 40-100 DEG C to obtain Z9, wherein a mass ratio of the Z8.1 to ethyl diphenylphosphinite is (1.5-1.8):1. The method has the advantages of easily available raw materials, mild reaction conditions, easy realization of industrial production, high yield, and easiness in separation of the solvents.

Description

technical field [0001] The invention belongs to the technical field of intermediate synthesis, and in particular relates to a method for preparing a rosuvastatin intermediate, in particular to a method for synthesizing a rosuvastatin intermediate Z9 by using the rosuvastatin intermediate Z6 as a raw material. Background technique [0002] Cardiovascular disease is a kind of disease that seriously endangers the health. In recent years, the morbidity and mortality of such diseases have been on the rise in both eastern and western countries. According to the statistics of the World Health Organization, about 15 million people die of cardiovascular diseases in the world every year. In my country, the incidence of cardiovascular and cerebrovascular diseases is as high as 8%, and the mortality rate is close to 50% of the total mortality. Cardiovascular and cerebrovascular diseases are mainly caused by atherosclerosis, and more than 80% of atherosclerosis is caused by hyperlipidem...

Claims

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Application Information

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IPC IPC(8): C07D239/42
CPCC07D239/42
Inventor 冯春生何俊胡挺查炎华胡玉峰
Owner HUBEI XIANGYUN GROUP CHEM
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