2H-pyrazolo [3, 4-d] pyrimidine derivative and synthetic method thereof

A technology of pyrimidine derivatives and synthesis methods, applied in the field of 2H-pyrazolo[3,4-d]pyrimidine derivatives and synthesis
CN102115476AInactive Publication Date: 2011-07-06CHANGZHOU UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
CHANGZHOU UNIV
Publication Date
2011-07-06
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention belongs to the field of organic synthesis and relates to a 2H-pyrazolo [3, 4-d] pyrimidine derivative (i.e., 2-(4-substituted phenyl)-4-chloro-2H-pyrazolo [3, 4-d] pyrimidine) and a synthetic method thereof. In the general structural formula of 2-(4-substituted phenyl)-4-chloro-2H-pyrazolo [3, 4-d] pyrimidine, R refers to hydrogen, alkyl, alkoxyl, halogen, cyan, nitro, carboxyl, ester group and the like; and tetrahydrofuran is adopts as solvent, 4-substituted phenylhydrazine reacts with 4, 6-(dichloro-pyrimidine)-5-methanal under the action of triethylamine, most solvent is vaporized after reaction completion, a crude product precipitates out as a solid by adding water, the crude product filtered out is recrystallized with absolute methanol, and then isomer is removed by a column separation method to obtain corresponding 2-(4-substituted phenyl)-4-chloro-2H-pyrazolo [3, 4-d] pyrimidine. The 2H-pyrazolo [3, 4-d] pyrimidine derivative is synthesized for the first time by selecting reasonable reaction conditions.
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Description

Technical field

[0001] The present invention involves a 2H-pyrazole and [3,4-D] pyrimidine derivatives, namely 2- (4-replace the phenyl) -4-clotic-2H-pyrazoleThe synthetic method is to replace the phenylhol and 4,6-dichloropyamine -5-formaldehyde as the raw material, and the tetrahydrocarbufu as the solvent.Azoli [3,4-D] pyrimidine. Background technique

[0002] As an important biomolecular DNA and ATP structure unit, pyrazole and its pyrazole derivatives have a wide range of biological activity. They are the advantage structure in the design of new drugs and have been highly valued by drug chemical workers.At present, many anti-cancer drugs have been developed based on 1H-pyrazole [3,4-D] pyrimidine derivatives.treat.For example, allopurinol, which has been used for clinical, can treat primary and secondary hyperuricemia, repeated attacks or chronic gout, gout, uric acid renal, and uric acid nephropathy, and high uric acid and bloodMany other pyrine derivatives have also been pr...

Claims

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