N-Acetylation of Amines in Continuous-Flow with Acetonitrile—No Need for Hazardous and Toxic Carboxylic Acid Derivatives

A continuous-flow acetylation reaction was developed, applying cheap and safe reagent, acetonitrile as acetylation agent and alumina as catalyst. The method developed utilizes milder reagent than those used conventionally. The reaction was tested on various aromatic and aliphatic amines with good co...

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Detalles Bibliográficos
Autores principales: Orsy, György, Fülöp, Ferenc, Mándity, István M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7221708/
https://www.ncbi.nlm.nih.gov/pubmed/32340371
http://dx.doi.org/10.3390/molecules25081985
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author Orsy, György
Fülöp, Ferenc
Mándity, István M.
author_facet Orsy, György
Fülöp, Ferenc
Mándity, István M.
author_sort Orsy, György
collection PubMed
description A continuous-flow acetylation reaction was developed, applying cheap and safe reagent, acetonitrile as acetylation agent and alumina as catalyst. The method developed utilizes milder reagent than those used conventionally. The reaction was tested on various aromatic and aliphatic amines with good conversion. The catalyst showed excellent reusability and a scale-up was also carried out. Furthermore, a drug substance (paracetamol) was also synthesized with good conversion and yield.
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spelling pubmed-72217082020-05-21 N-Acetylation of Amines in Continuous-Flow with Acetonitrile—No Need for Hazardous and Toxic Carboxylic Acid Derivatives Orsy, György Fülöp, Ferenc Mándity, István M. Molecules Article A continuous-flow acetylation reaction was developed, applying cheap and safe reagent, acetonitrile as acetylation agent and alumina as catalyst. The method developed utilizes milder reagent than those used conventionally. The reaction was tested on various aromatic and aliphatic amines with good conversion. The catalyst showed excellent reusability and a scale-up was also carried out. Furthermore, a drug substance (paracetamol) was also synthesized with good conversion and yield. MDPI 2020-04-23 /pmc/articles/PMC7221708/ /pubmed/32340371 http://dx.doi.org/10.3390/molecules25081985 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Orsy, György
Fülöp, Ferenc
Mándity, István M.
N-Acetylation of Amines in Continuous-Flow with Acetonitrile—No Need for Hazardous and Toxic Carboxylic Acid Derivatives
title N-Acetylation of Amines in Continuous-Flow with Acetonitrile—No Need for Hazardous and Toxic Carboxylic Acid Derivatives
title_full N-Acetylation of Amines in Continuous-Flow with Acetonitrile—No Need for Hazardous and Toxic Carboxylic Acid Derivatives
title_fullStr N-Acetylation of Amines in Continuous-Flow with Acetonitrile—No Need for Hazardous and Toxic Carboxylic Acid Derivatives
title_full_unstemmed N-Acetylation of Amines in Continuous-Flow with Acetonitrile—No Need for Hazardous and Toxic Carboxylic Acid Derivatives
title_short N-Acetylation of Amines in Continuous-Flow with Acetonitrile—No Need for Hazardous and Toxic Carboxylic Acid Derivatives
title_sort n-acetylation of amines in continuous-flow with acetonitrile—no need for hazardous and toxic carboxylic acid derivatives
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7221708/
https://www.ncbi.nlm.nih.gov/pubmed/32340371
http://dx.doi.org/10.3390/molecules25081985
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AT mandityistvanm nacetylationofaminesincontinuousflowwithacetonitrilenoneedforhazardousandtoxiccarboxylicacidderivatives

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