Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Rosuvastatin lactone

A technology of rosuvastatin lactone and methyl isobutyrylacetate, applied in the field of medicine, can solve problems such as different lipid-lowering properties, and achieve the effects of simple synthesis, strong operability, and simple three-waste treatment

Inactive Publication Date: 2014-03-05
成都摩尔生物医药有限公司
View PDF8 Cites 8 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although this product has the dihydroxyheptanoic acid part of the pharmacophore shared by statins, the rest of the structure in the molecule is quite different from other similar drugs, so the lipid-lowering performance is also different.

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
  • Rosuvastatin lactone
  • Rosuvastatin lactone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0011] The following examples further describe the total synthesis of rosuvastatin lactone.

[0012] 1. Synthesis of 4-(4-fluorophenyl)-6-isopropyl-5-methoxycarbonyl-3,4-2(1H)-dihydropyrimidinone (L)

[0013] Add p-fluorobenzaldehyde (500g), methyl isobutyrylacetate (860g), urea 200g, cuprous chloride, methanol, sulfuric acid into the reaction kettle, and heat to reflux. Cool in an ice-water bath, continue to stir, and then filter with suction. The resulting solid is rinsed with methanol and dried in a drying oven to obtain 1460.17 g of white crystals, with a yield of 98.7%.

[0014] 2. Synthesis of [4-(4-fluorophenyl)-2-hydroxyl-6-isopropyl-5-methoxycarbonylpyrimidine (II)

[0015] Add 65-68% nitric acid and sodium nitrite into the reaction kettle, add intermediate I in batches at 10-25°C, and continue to react at 10-20°C, and the reaction is complete as detected by TLC. Add water to the reaction solution, then add dropwise sodium hydroxide solution to adjust the pH, and pa...

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 kind of rosuvastatin lactone. The chemical formula of the rosuvastatin lactone is C22H26FN3O5S; the rosuvastatin lactone is prepared by taking fluorobenzaldehyde, methyl isobutyrylacetate, urea and cuprous chloride as raw materials through a series of reactions such as condensation, oxidation, reduction, substitution, and the like, so that a final product rosuvastatin lactone is obtained. The rosuvastatin lactone disclosed by the invention is an economic, security, high-purity and high-yield route, and suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a new method for preparing rosuvastatin lactone. Background technique [0002] Rosuvastatin lactone is a third-generation statin drug with a fully synthesized single enantiomer, which belongs to HMG-CoA reductase inhibitors, and can reduce elevated low-density cholesterol, total cholesterol, triglycerides and Base protein B concentration, while increasing the concentration of high-density cholesterol. It can be used for comprehensive treatment of primary hypercholesterolemia, mixed lipodystrophy and homozygous familial hypercholesterolemia. [0003] Although this product has the dihydroxyheptanoic acid part of the pharmacophore shared by statins, the rest of the structure in the molecule is quite different from other similar drugs, so the lipid-lowering performance is also different. A large number of clinical trials have confirmed that the effect of this product o...

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): C07D405/06
CPCC07D405/06
Inventor 李智勇
Owner 成都摩尔生物医药有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com