Formylation of 2-Methylpyrimidine-4,6-diol Under the Conditions of the Vilsmeier–Haack Reaction

In the course of this work, we explored the influence of the conditions of the Vilsmeier–Haack reaction for 2-methylpyrimidine-4,6-diol (<b>1</b>). We conducted a comparative analysis of approaches using various solvents (o-xylene, N,N-dimethylformamide (DMF), benzene, and dichloroethane...

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Main Authors: Aleksandr V. Dambaev, Denis A. Kolesnik, Igor P. Yakovlev, Tamara L. Semakova
Format: Article
Language:English
Published: MDPI AG 2024-11-01
Series:Chemistry Proceedings
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Online Access:https://www.mdpi.com/2673-4583/16/1/104
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author Aleksandr V. Dambaev
Denis A. Kolesnik
Igor P. Yakovlev
Tamara L. Semakova
author_facet Aleksandr V. Dambaev
Denis A. Kolesnik
Igor P. Yakovlev
Tamara L. Semakova
author_sort Aleksandr V. Dambaev
collection DOAJ
description In the course of this work, we explored the influence of the conditions of the Vilsmeier–Haack reaction for 2-methylpyrimidine-4,6-diol (<b>1</b>). We conducted a comparative analysis of approaches using various solvents (o-xylene, N,N-dimethylformamide (DMF), benzene, and dichloroethane) as the reaction medium, and the optimal one was selected. During the formylation of substrate 1 in these conditions, only 4,6-dihydroxy-2-methylpyrimidine-5-carbaldehyde (<b>2</b>) was successful. It should be noted that there was no substitution of hydroxyl groups for chlorine atoms observed in reactions with similar substrates. The structure of the resulting product <b>2</b> was proven using NMR spectroscopy on <sup>1</sup>H and <sup>13</sup>C nuclei and by mass spectrometry.
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institution Kabale University
issn 2673-4583
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publishDate 2024-11-01
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series Chemistry Proceedings
spelling doaj-art-398b3d07c2b246439cbadc1dee4b70eb2025-08-20T03:26:20ZengMDPI AGChemistry Proceedings2673-45832024-11-0116110410.3390/ecsoc-28-20128Formylation of 2-Methylpyrimidine-4,6-diol Under the Conditions of the Vilsmeier–Haack ReactionAleksandr V. Dambaev0Denis A. Kolesnik1Igor P. Yakovlev2Tamara L. Semakova3State Federal-Funded Educational Institution of Higher Education, Saint Petersburg State Chemical and Pharmaceutical University, Ministry of Healthcare of the Russian Federation, Professor Popov Str., 14, Lit. A, St. Petersburg 197022, RussiaState Federal-Funded Educational Institution of Higher Education, Saint Petersburg State Chemical and Pharmaceutical University, Ministry of Healthcare of the Russian Federation, Professor Popov Str., 14, Lit. A, St. Petersburg 197022, RussiaState Federal-Funded Educational Institution of Higher Education, Saint Petersburg State Chemical and Pharmaceutical University, Ministry of Healthcare of the Russian Federation, Professor Popov Str., 14, Lit. A, St. Petersburg 197022, RussiaState Federal-Funded Educational Institution of Higher Education, Saint Petersburg State Chemical and Pharmaceutical University, Ministry of Healthcare of the Russian Federation, Professor Popov Str., 14, Lit. A, St. Petersburg 197022, RussiaIn the course of this work, we explored the influence of the conditions of the Vilsmeier–Haack reaction for 2-methylpyrimidine-4,6-diol (<b>1</b>). We conducted a comparative analysis of approaches using various solvents (o-xylene, N,N-dimethylformamide (DMF), benzene, and dichloroethane) as the reaction medium, and the optimal one was selected. During the formylation of substrate 1 in these conditions, only 4,6-dihydroxy-2-methylpyrimidine-5-carbaldehyde (<b>2</b>) was successful. It should be noted that there was no substitution of hydroxyl groups for chlorine atoms observed in reactions with similar substrates. The structure of the resulting product <b>2</b> was proven using NMR spectroscopy on <sup>1</sup>H and <sup>13</sup>C nuclei and by mass spectrometry.https://www.mdpi.com/2673-4583/16/1/104formylationpyrimidine-4,6-diolsVilsmeier–Haack reactionelectrophilic substitution
spellingShingle Aleksandr V. Dambaev
Denis A. Kolesnik
Igor P. Yakovlev
Tamara L. Semakova
Formylation of 2-Methylpyrimidine-4,6-diol Under the Conditions of the Vilsmeier–Haack Reaction
Chemistry Proceedings
formylation
pyrimidine-4,6-diols
Vilsmeier–Haack reaction
electrophilic substitution
title Formylation of 2-Methylpyrimidine-4,6-diol Under the Conditions of the Vilsmeier–Haack Reaction
title_full Formylation of 2-Methylpyrimidine-4,6-diol Under the Conditions of the Vilsmeier–Haack Reaction
title_fullStr Formylation of 2-Methylpyrimidine-4,6-diol Under the Conditions of the Vilsmeier–Haack Reaction
title_full_unstemmed Formylation of 2-Methylpyrimidine-4,6-diol Under the Conditions of the Vilsmeier–Haack Reaction
title_short Formylation of 2-Methylpyrimidine-4,6-diol Under the Conditions of the Vilsmeier–Haack Reaction
title_sort formylation of 2 methylpyrimidine 4 6 diol under the conditions of the vilsmeier haack reaction
topic formylation
pyrimidine-4,6-diols
Vilsmeier–Haack reaction
electrophilic substitution
url https://www.mdpi.com/2673-4583/16/1/104
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AT denisakolesnik formylationof2methylpyrimidine46diolundertheconditionsofthevilsmeierhaackreaction
AT igorpyakovlev formylationof2methylpyrimidine46diolundertheconditionsofthevilsmeierhaackreaction
AT tamaralsemakova formylationof2methylpyrimidine46diolundertheconditionsofthevilsmeierhaackreaction