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

7-amino-tetrazole[1,5-a] pyrimidine-5-alcohol(compound ii) and its synthetic route

A technology of aminotetrazole and synthetic route, which is applied in the field of medicine and can solve the problems of high toxicity, toxicity, and poor selectivity of systemic drugs

Inactive Publication Date: 2013-08-21
INNER MONGOLIA MEDICAL UNIV
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] At present, most of the antineoplastic drugs used clinically are not highly selective for tumor cell inhibition, systemic administration is highly toxic, and most of them have immunosuppressive effects
In theory, anti-metabolite drugs can kill tumor cells without affecting normal cells, but in fact, anti-metabolite drugs also show certain toxicity to some normal tissues with rapid proliferation

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
  • 7-amino-tetrazole[1,5-a] pyrimidine-5-alcohol(compound ii) and its synthetic route
  • 7-amino-tetrazole[1,5-a] pyrimidine-5-alcohol(compound ii) and its synthetic route
  • 7-amino-tetrazole[1,5-a] pyrimidine-5-alcohol(compound ii) and its synthetic route

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0038] 1. Preparation of 7-amino-tetrazol[1,5-a]pyrimidin-5-ol (compound II) (Route 1)

[0039] (1) Add 3g of 5-aminotetrazole, 3.7g of malonic acid and 45mL of chloroform into a round bottom flask, heat to reflux, and after the solids are uniformly dispersed, add 10.8g of phosphorus oxychloride, heat to reflux and stir overnight. Evaporate the solvent in a water bath, add ice water, stir well, and filter with suction to obtain a solid. The obtained solid was heated with water, refluxed, and then an appropriate amount of ethanol was added. After the solid was completely dissolved, it was filtered while it was hot. 4.3g, m.p.>300℃, yield 79.63%, elemental analysis C 4 h 3 N 5 o 2 . Found: C31.06, H2.12, N45.61; Calculated: C31.38, H1.98, N45.74.

[0040] (2) Add 4g of tetrazo[1,5-a]pyrimidine-5,7-diol (compound I) and 20mL of phosphorus oxychloride into a round bottom flask, heat to 100°C, and keep the temperature. The reaction was stirred for 4 hours to obtain a clear s...

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 novel purine analogue 7-amino-tetrazole[1,5-a]pyrimidine-5-alcohol(compound II) and its synthetic route. It shows through a pharmacological experiment that the compound II has an effect of inhibiting cell division cycle phosphoesterase CDC25. The compound II can be used as an antimetabolic medicine with high biological activity, good selectivity and little toxicity, and can be widely used in clinic.

Description

technical field [0001] The present invention belongs to the technical field of medicine, relates to an anti-metabolite and its synthesis route, and specifically relates to performing ring equivalent substitution on the basic mother nucleus of a purine base, designing and synthesizing a new purine analogue and 7-amino-tetra Azozo[1,5-a]pyrimidin-5-ol (compound II). Background technique [0002] Purine analogues not only have antibacterial, antiviral, antihypertensive, antiarrhythmic, immunosuppressive and many other activities. And it has strong biological activity in anti-tumor. In theory, anti-metabolite drugs can kill tumor cells without affecting normal cells, but in fact, anti-metabolite drugs also show certain toxicity to some normal tissues with rapid proliferation. Therefore, it is of great practical significance to search for anti-metabolites with high biological activity, good selectivity and low toxicity. [0003] CDC25B (cell devision cycle B) phosphatase is a ...

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): C07D487/04A61P35/00A61P31/18
Inventor 鲁源
Owner INNER MONGOLIA MEDICAL UNIV
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