Synthesis of acyclic nucleoside analogues based on 1,2,4-triazolo[1,5-a]pyrimidine-7-ones by one-step Vorbrüggen glycosylation

New analogues of acyclovir have been prepared by reacting 1,2,4-triazolo[1,5-a]pyrimidin-7-ones 1а-i and (2-acetoxyethoxy)methyl acetate 2 in the presence of trimethylsilyl trifluoromethanesulfonate as a catalyst. Thei nteraction between the compounds 1а-е and 2 has led to a mixture of N3 and N4 iso...

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Main Authors: I. A. Khalymbadzha, S. L. Deev, T. S. Shestakova, V. L. Rusinov, O. N. Chupakhin
Format: Article
Language:English
Published: Ural Federal University 2015-05-01
Series:Chimica Techno Acta
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Online Access:https://chimicatechnoacta.ru/article/view/1126
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author I. A. Khalymbadzha
S. L. Deev
T. S. Shestakova
V. L. Rusinov
O. N. Chupakhin
author_facet I. A. Khalymbadzha
S. L. Deev
T. S. Shestakova
V. L. Rusinov
O. N. Chupakhin
author_sort I. A. Khalymbadzha
collection DOAJ
description New analogues of acyclovir have been prepared by reacting 1,2,4-triazolo[1,5-a]pyrimidin-7-ones 1а-i and (2-acetoxyethoxy)methyl acetate 2 in the presence of trimethylsilyl trifluoromethanesulfonate as a catalyst. Thei nteraction between the compounds 1а-е and 2 has led to a mixture of N3 and N4 isomers. In contrast, the reaction of compounds 1g-i and 2 proceeded selectively to form N3 isomers. In the case of compounds 1a-c the predominant product is the one with the acyclic moiety in azine ring (N4 isomer). Interaction between 1d-f and 2 has led to mixtures comprising mainly N3 isomer. It has been found that the ratio of glycosylation products 1 and 2 are thermodynamically controlled. The structure of the obtained compounds has been proved by 1Н, 13С, two-dimensional 1Н-13С NMR spectroscopy and X-ray analysis.
format Article
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institution Kabale University
issn 2411-1414
language English
publishDate 2015-05-01
publisher Ural Federal University
record_format Article
series Chimica Techno Acta
spelling doaj-art-417bf516e5d54639ab869d7f7d88b5ed2025-08-20T03:55:40ZengUral Federal UniversityChimica Techno Acta2411-14142015-05-012215816310.15826/chimtech.2015.2.2.0171242Synthesis of acyclic nucleoside analogues based on 1,2,4-triazolo[1,5-a]pyrimidine-7-ones by one-step Vorbrüggen glycosylationI. A. Khalymbadzha0S. L. Deev1T. S. Shestakova2V. L. Rusinov3O. N. Chupakhin4Институт органического синтеза УрО РАН, ЕкатеринбургИнститут органического синтеза УрО РАН, ЕкатеринбургИнститут органического синтеза УрО РАН, ЕкатеринбургИнститут органического синтеза УрО РАН, ЕкатеринбургИнститут органического синтеза УрО РАН, ЕкатеринбургNew analogues of acyclovir have been prepared by reacting 1,2,4-triazolo[1,5-a]pyrimidin-7-ones 1а-i and (2-acetoxyethoxy)methyl acetate 2 in the presence of trimethylsilyl trifluoromethanesulfonate as a catalyst. Thei nteraction between the compounds 1а-е and 2 has led to a mixture of N3 and N4 isomers. In contrast, the reaction of compounds 1g-i and 2 proceeded selectively to form N3 isomers. In the case of compounds 1a-c the predominant product is the one with the acyclic moiety in azine ring (N4 isomer). Interaction between 1d-f and 2 has led to mixtures comprising mainly N3 isomer. It has been found that the ratio of glycosylation products 1 and 2 are thermodynamically controlled. The structure of the obtained compounds has been proved by 1Н, 13С, two-dimensional 1Н-13С NMR spectroscopy and X-ray analysis.https://chimicatechnoacta.ru/article/view/1126аналоги ацикловира
spellingShingle I. A. Khalymbadzha
S. L. Deev
T. S. Shestakova
V. L. Rusinov
O. N. Chupakhin
Synthesis of acyclic nucleoside analogues based on 1,2,4-triazolo[1,5-a]pyrimidine-7-ones by one-step Vorbrüggen glycosylation
Chimica Techno Acta
аналоги ацикловира
title Synthesis of acyclic nucleoside analogues based on 1,2,4-triazolo[1,5-a]pyrimidine-7-ones by one-step Vorbrüggen glycosylation
title_full Synthesis of acyclic nucleoside analogues based on 1,2,4-triazolo[1,5-a]pyrimidine-7-ones by one-step Vorbrüggen glycosylation
title_fullStr Synthesis of acyclic nucleoside analogues based on 1,2,4-triazolo[1,5-a]pyrimidine-7-ones by one-step Vorbrüggen glycosylation
title_full_unstemmed Synthesis of acyclic nucleoside analogues based on 1,2,4-triazolo[1,5-a]pyrimidine-7-ones by one-step Vorbrüggen glycosylation
title_short Synthesis of acyclic nucleoside analogues based on 1,2,4-triazolo[1,5-a]pyrimidine-7-ones by one-step Vorbrüggen glycosylation
title_sort synthesis of acyclic nucleoside analogues based on 1 2 4 triazolo 1 5 a pyrimidine 7 ones by one step vorbruggen glycosylation
topic аналоги ацикловира
url https://chimicatechnoacta.ru/article/view/1126
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