Synthesis of product prepared from imidazole acted with halogenated acetate ethyl ester

A technology of zoledronic acid and a new method, which is applied in the field of medicine, can solve the problems of high requirements for production personnel protection, three wastes treatment, and high equipment requirements, and achieve the effects of low cost, environmental protection, and mild reaction conditions

Inactive Publication Date: 2004-02-04
MAILIN HIGH TECH DEVING WUHAN CITY
View PDF0 Cites 9 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this route requires high-pressure reaction, high equipment requirements, and highly toxic cyanide will be produced during hydrolysis, which has high requirements for the protection of production personnel and the treatment of three wastes

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
  • Synthesis of product prepared from imidazole acted with halogenated acetate ethyl ester
  • Synthesis of product prepared from imidazole acted with halogenated acetate ethyl ester
  • Synthesis of product prepared from imidazole acted with halogenated acetate ethyl ester

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0018] according to figure 1 Shown, the preparation of imidazole acetic acid:

[0019] Add 300 grams of imidazole and 450 milliliters of ethyl chloroacetate, 360 grams of anhydrous potassium carbonate, and 1500 milliliters of acetone into a 3000 milliliter three-necked reaction flask with stirring, condenser and thermometer, heat up to reflux, keep the reflux reaction for 6 hours, and cool to Filtrate at room temperature, recover acetone at normal pressure to dryness, add 600 ml of water to the residual oil, extract with dichloromethane, dry over anhydrous magnesium sulfate, recover the solvent at normal pressure to dryness, distill the residue under reduced pressure, collect 135-140 ° C / 5mmHg cut, obtains 220 grams of light yellow oily imidazole ethyl acetate.

[0020] Its reaction formula is:

[0021] The obtained imidazole ethyl acetate is directly put into a 2000 ml three-neck reaction flask with a stirring and condenser tube without refining, and 900 ml of 4N hydroc...

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

A process for snthesizing azolyphosphonic acid includes such steps as reacting of imidazo on ethyl thioacetate, hydrolyzing with acid to obtain imidazoleacetic acid, and preparing azolyphosphonic acid. Its advantages are easily available raw materials, low cost, short process, high productivity and no environmental pollution.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a new method for synthesizing zoledronic acid. Background technique [0002] Zoledronic acid, (1-hydroxy-2-imidazol-1-ylethylidene) diphosphonic acid monohydrate, see (I) for the chemical structure. It is the strongest new-generation bisphosphonate drug discovered in current clinical research for the treatment of tumor-induced hypercalcemia (TIH or HCM), the most common life-threatening metabolic complication associated with cancer. [0003] It is reported in the literature that the synthesis of zoledronic acid takes imidazole as the starting material, reacts with acetonitrile under pressure, and then hydrolyzes with acid to obtain the intermediate imidazole acetic acid, and then reacts with phosphorous acid to obtain the finished product. However, this route requires high-pressure reaction, high equipment requirements, and highly toxic cyanide will be pr...

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
Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6506
Inventor 胡文倩张玉张耕
Owner MAILIN HIGH TECH DEVING WUHAN CITY
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