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
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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

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  • 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

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Experimental program
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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...

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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

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04A61P35/00A61P31/18
Inventor 鲁源
Owner INNER MONGOLIA MEDICAL UNIV
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