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

RSC Adv. 2021 Nov 10;11(57):36143-36147. doi: 10.1039/d1ra06912h. eCollection 2021 Nov 4.

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 N 4-acetyl cytosine, to an amidoxime. This method avoids use of expensive starting materials, enzymes, complex reagents, and cumbersome purification procedures.