Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Efficient and Selective Acetylation of Biomolecules with 1-Acetylimidazole Catalyzed by Er(OTf)3.

Monica Nardi
* ORCID logo ,
Maria Luisa Di Gioia
* ,
Paola Costanzo
ORCID logo ,
Antonio De Nino
,
Loredana Maiuolo
,
Manuela Oliverio
ORCID logo ,
Fabrizio Olivito
,
Antonio Procopio
Version 1 : Received: 21 July 2017 / Approved: 21 July 2017 / Online: 21 July 2017 (18:28:33 CEST)

A peer-reviewed article of this Preprint also exists.

Nardi, M.; Gioia, M.L.D.; Costanzo, P.; Nino, A.D.; Maiuolo, L.; Oliverio, M.; Olivito, F.; Procopio, A. Selective Acetylation of Small Biomolecules and Their Derivatives Catalyzed by Er(OTf)3. Catalysts 2017, 7, 269. Nardi, M.; Gioia, M.L.D.; Costanzo, P.; Nino, A.D.; Maiuolo, L.; Oliverio, M.; Olivito, F.; Procopio, A. Selective Acetylation of Small Biomolecules and Their Derivatives Catalyzed by Er(OTf)3. Catalysts 2017, 7, 269.

Abstract

It is of great significance to develop sustainable processes of catalytic reaction. We report an efficient and selective procedure for the synthesis of acetylated bioactive compounds in water. The use of 1-acetylimidazole combined with Er(OTf)3 as Lewis acid catalyst gives high regioselectivity and good to excellent yields for the acetylation of primary hydroxyl groups as well as amino groups. The protection is achieved in short reaction times under microwave irradiation and is successful even in the case of base-sensitive substrates.

Keywords

catalysis; acetylation; biomolecules

Subject

Chemistry and Materials Science, Organic Chemistry

Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Comments (4)

Comment 1
Received: 28 July 2017
Commenter:
Ana Santiago

The commenter has declared there is no conflict of interests.
Comment: Very interesting your job!
A fast efficient and regioselective acetylation using MW.
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Comment 2
Received: 28 July 2017
Commenter: Natividad Herrera Cano
The commenter has declared there is no conflict of interests.
Comment: How interesting!
An eco-friendly method of protection of glycals avoiding the formation of by-products.
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Comment 3
Received: 31 July 2017
Commenter: Cariati
The commenter has declared there is no conflict of interests.
Comment: Very Good Job. Congratulation
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Comment 4
Received: 31 July 2017
Commenter: Mohamed Attya
The commenter has declared there is no conflict of interests.
Comment: Very interesting work
A fast efficient and regioselective acetylation using water for the synthesis of bio active compounds decrease purification problems and also using MW decrease the reactions times
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