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Compound I tetrazole (1, 5-a) pyrimidine-5, 7-diol and synthetic route thereof

A synthetic route and compound technology, applied in organic chemistry, drug combination, antiviral agents, etc., can solve problems such as poor selectivity, toxicity, and high toxicity of systemic drugs

Inactive Publication Date: 2013-07-17
INNER MONGOLIA MEDICAL UNIV
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  • Description
  • Claims
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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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  • Compound I tetrazole (1, 5-a) pyrimidine-5, 7-diol and synthetic route thereof
  • Compound I tetrazole (1, 5-a) pyrimidine-5, 7-diol and synthetic route thereof
  • Compound I tetrazole (1, 5-a) pyrimidine-5, 7-diol and synthetic route thereof

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Embodiment Construction

[0022] 1. Preparation of tetrazo[1,5-a]pyrimidine-5,7-diol (compound I) (Route 1)

[0023] Add 3g of 5-aminotetrazole, 3.7g of malonic acid and 45mL of chloroform into a round-bottomed flask, heat to reflux, and after the solid is 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.

[0024] 2. Test report on inhibition of cell division cycle phosphatase CDC25B by tetrazo[1,5-a]pyrimidine-5,7-diol (compound I)

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Abstract

The invention discloses novel purine analogue tetrazole (1, 5-a) pyrimidine-5, 7-diol (compound I) and a synthetic route thereof. Pharmacological experiments show that the compound I is inhibitory for cell division cycle phosphoesterase CDC25. The compound I can be made into anti-metabolites high in bioactivity, fine in selectivity and low in toxicity, and is widely applicable to the 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 analog tetrazole [1 ,5-a] pyrimidine-5,7-diol (compound I), and pharmacological experiments have confirmed that compound I has an inhibitory effect on cell division cycle phosphatase CDC25. 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 wit...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K31/519A61P35/00A61P31/18
Inventor 鲁源
Owner INNER MONGOLIA MEDICAL UNIV
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