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
View PDF6 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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 synthesi

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Preparation method of rosuvastatin intermediate
  • Preparation method of rosuvastatin intermediate
  • Preparation method of rosuvastatin intermediate

Examples

Experimental program
Comparison scheme
Effect test

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.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap