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Title: Synthesis and alkylation of 1-aryl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin4-ones as possible anticonvulsant agents
Other Titles: Синтез и алкилирование 1-арил-1,5-дигидро-4Н-пиразоло [3,4-d] пиримидин-4-онов в качестве возможных противосудорожных средств
Синтез і алкілування 1-арил-1,5-дигідро-4H-піразоло [3,4-D] піримідин-4-они в якості можливих протисудомних засобів
Authors: Severina, A. I.
Georgiyants, V. А.
Shtrygol, S. Yu.
Kavraiskyi, D. P.
Северина, А. И.
Георгиянц, В. А.
Штрыголь, С. Ю.
Каврайский, Д. П.
Северіна, А. І.
Георгіянц, В. А.
Штриголь, С. Ю.
Каврайський, Д. П.
Keywords: synthesis;pyrimidine;pyrazole;alkylation;acetamides;activity prediction;синтез;піримідин;піразол;алкілування;ацетаміди;прогнозування активності;пиразол;алкилирование;пиримидин;ацетамиды;прогнозирование активности
Issue Date: 2015
Publisher: Der Pharma Chemica
Bibliographic description (Ukraine): Synthesis and alkylation of 1-aryl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-ones as possible anticonvulsant agents / A. I. Severina, V. А. Georgiyants, S. Yu. Shtrygol, D. P. Kavraiskyi // Der Pharma Chemica. - 2015. - № 7(11). - С. 43-48.
Abstract: The synthesis of 1-(4-bromophenyl)- and 1-(2-chlorophenyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one as possible anticonvulsant agents was planned. It was carried out by the interaction of the corresponding phenylhydrazine hydrochloride with ethyletoxymethylencyanocetate with a further heating of obtained 5-аmino-1аryl-1H-pyrazole-4-carboxylate in excess of formamide. The direction of reaction of 1-aryl-1,5-dihydro-4Hpyrazolo[3,4-d] pyrimidine-4-one with N-arylsubstituted α-chloracetamides, 2-chloro-1-(4-arylpiperazine-1-yl)ethanone and 2-chloro-N-(4-chlorobenzyl)acetamide in the presence of DMFA-NaHCO3 had been investigated. Using the data of NMR and NOESY spectroscopy it was found out that reaction is selectively performed at 5 position of pyrazolo[3,4-d]pyrimidine system. Due to preliminary prognosis of biological activity pharmacological screening of substances synthesized as possible anticonvulsant agents on the penthyltetrazole seizures was planned
Appears in Collections:Наукові публікації кафедри фармацевтичної хімії

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