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

Synthetic method for 2-chloro-4-amino-6,7-dimethoxy quinazoline

A technology of dimethoxyquinazoline and synthesis method, which is applied in the synthesis field of 2-chloro-4-amino-6,7-dimethoxyquinazoline, can solve the problem of insufficient reaction of reactants and target product Instability, complex synthesis method and other problems, to achieve the effect of complete reaction, stable yield and simplified reaction steps

Inactive Publication Date: 2017-09-01
浙江逸都生物科技有限公司
View PDF2 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The synthesis method of 2-chloro-4-amino-6,7-dimethoxyquinazoline in the prior art is relatively complicated, and the reaction of the reactants is not sufficient, which easily causes waste of raw materials, and the obtained target product is unstable

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
  • Synthetic method for 2-chloro-4-amino-6,7-dimethoxy quinazoline
  • Synthetic method for 2-chloro-4-amino-6,7-dimethoxy quinazoline

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0037] The synthetic method of 2-chloro-4-amino-6,7-dimethoxyquinazoline of the present invention comprises the steps:

[0038] 1) Preparation of 3,4-dimethoxyphenyl isocyanate

[0039] (1) First dissolve 3,4-dimethoxyaniline and dichloroethane and then heat to generate 3,4-dimethoxyaniline solution, the quality of 3,4-dimethoxyaniline and dichloroethane The ratio is 3:10, mixing in this ratio can improve the reaction efficiency of 3,4-dimethoxyaniline and dichloroethane, make the reaction of reactants more thorough, and reduce the waste of raw materials;

[0040] (2) Then add triphosgene and dichloroethane into the first reaction flask, stir and dissolve, lower the temperature to within 10°C, add 3,4-dimethoxyaniline solution dropwise into the first reaction flask, ~ 2 hours to finish dripping;

[0041] (3) heating and refluxing for 3h, reclaiming ethylene dichloride to obtain 3,4-dimethoxyphenyl isocyanate;

[0042] 2) Preparation of 3,4-dimethoxyphenylcyanuria

[0043] ...

Embodiment 1

[0060] 1) Preparation of 3,4-dimethoxyphenyl isocyanate

[0061] (1) At first 124g of 3,4-dimethoxyaniline and 400ml of ethylene dichloride were dissolved and then heated to generate 3,4-dimethoxyaniline solution;

[0062] (2) Then add triphosgene and 400ml of dichloroethane into the first reaction flask, stir and dissolve, lower the temperature to within 10°C, add the 3,4-dimethoxyaniline solution dropwise into the first reaction flask, Finish dripping within 1 to 2 hours;

[0063] (3) warming up and refluxing for 3h, reclaiming ethylene dichloride to obtain 3,4-dimethoxyphenyl isocyanate with a yield of 0.94;

[0064] 2) Preparation of 3,4-dimethoxyphenylcyanuria

[0065] (1) at first concentration is that 50% cyanamide 150g and concentration are 50% lye 200g to add in the second reaction bottle, reduce temperature to within 3 ℃;

[0066] (2) Add 3,4-dimethoxyphenyl isocyanate dropwise to the second reaction flask, and raise the temperature to 30° C. after the dropwise ad...

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 synthetic method for 2-chloro-4-amino-6,7-dimethoxy quinazoline. The synthetic method comprises the following steps: 1) preparing 3,4-dimethoxyphenyl isocyanate; 2) preparing 3,4-dimethoxyphenyl cyanourea; 3) preparing a 2-chloro-4-amino-6,7-dimethoxy quinazoline crude product; and 4) preparing a 2-chloro-4-amino-6,7-dimethoxy quinazoline fine product. The synthetic method disclosed by the invention simplifies reaction steps and increases the product yield; reaction conditions are optimized, so that reactants react more sufficiently, and therefore, generation of byproducts is reduced, production efficiency is improved, reactants are prevented from being oxidized, reaction is more complete, the target object can be obtained by direct filtering and drying during post-treatment, and the yield is stable.

Description

technical field [0001] The invention relates to a synthesis method of 2-chloro-4-amino-6,7-dimethoxyquinazoline. Background technique [0002] 2-Chloro-4-amino-6,7-dimethoxyquinazoline is an important intermediate for the synthesis of prazosin hydrochloride, terazosin hydrochloride, alfuzosin hydrochloride, doxazosin mesylate and other drugs body. This class of drugs is selective epinephrine alfa 1 —Receptor blockers, which can reduce peripheral vascular resistance, and have lowering effects on systolic and diastolic blood pressure; have the effect of relaxing bladder and prostate smooth muscle, and can relieve symptoms of dysuria caused by prostatic hypertrophy. [0003] The synthesis method of 2-chloro-4-amino-6,7-dimethoxyquinazoline in the prior art is relatively complicated, and the reaction of the reactants is not sufficient, which easily causes waste of raw materials, and the obtained target product is unstable . Contents of the invention [0004] The object of ...

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): C07D239/94
Inventor 钱伟成王新霖
Owner 浙江逸都生物科技有限公司
Features
  • Generate Ideas
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

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

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com