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Issue 87, 2020
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A concise route to MK-4482 (EIDD-2801) from cytidine

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Abstract

A two-step route to MK-4482 (EIDD-2801, 1) was developed consisting of an esterification and hydroxamination of cytidine. The selective acylation and direct amination eliminate the need for protecting and activating groups and proceed in overall yield of 75%, a significant advancement over the reported yield of 17%. The step count is reduced from five transformations to two, and expensive uridine is replaced with the more available cytidine.

Graphical abstract: A concise route to MK-4482 (EIDD-2801) from cytidine

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Article information


Submitted
03 Sep 2020
Accepted
01 Oct 2020
First published
02 Oct 2020

This article is Open Access

Chem. Commun., 2020,56, 13363-13364
Article type
Communication

A concise route to MK-4482 (EIDD-2801) from cytidine

N. Vasudevan, G. P. Ahlqvist, C. P. McGeough, D. J. Paymode, F. S. P. Cardoso, T. Lucas, J. Dietz, T. Opatz, T. F. Jamison, F. B. Gupton and D. R. Snead, Chem. Commun., 2020, 56, 13363
DOI: 10.1039/D0CC05944G

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