Issue 57, 2021
From the journal:

RSC Advances

Conversion of N-acyl amidines to amidoximes: a convenient synthetic approach to molnupiravir (EIDD-2801) from ribose†

Ajaz Ahmed,ab   Qazi Naveed Ahmed ORCID logo ab  and  Debaraj Mukherjee ORCID logo *ab  

* Corresponding authors

a Natural Product and Medicinal Chemistry Division, Indian Institute of Integrative Medicine (IIIM), Jammu 180001, India
E-mail: dmukherjee@iiim.ac.in, dmukherje@iiim.res.in

b Academy of Scientific and Innovative Research (AcSIR-IIIM), Jammu-180001, India

Abstract

An efficient method is described for the preparation of molnupiravir (EIDD-2801) an antiviral agent via regioselective conversion of an N-acyl-nucleoside intermediate, generated through stereo and regioselective glycosylation of protected ribose and N4-acetyl cytosine, to an amidoxime. This method avoids use of expensive starting materials, enzymes, complex reagents, and cumbersome purification procedures.

Graphical abstract: Conversion of N-acyl amidines to amidoximes: a convenient synthetic approach to molnupiravir (EIDD-2801) from ribose

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Article information

DOI
https://doi.org/10.1039/D1RA06912H
Article type
Paper
Submitted
15 Sep 2021
Accepted
27 Oct 2021
First published
10 Nov 2021
This article is Open Access
Creative Commons BY-NC license

RSC Adv., 2021,11, 36143-36147

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Conversion of N-acyl amidines to amidoximes: a convenient synthetic approach to molnupiravir (EIDD-2801) from ribose

A. Ahmed, Q. N. Ahmed and D. Mukherjee, RSC Adv., 2021, 11, 36143 DOI: 10.1039/D1RA06912H

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