A concise route to MK-4482 (EIDD-2801) from cytidine
Name
d0cc05944g.pdf
Description
Published version
Size
1.66 MB
Format
Unknown
Checksum (MD5)
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Author(s)
Vasudevan, N.
Ahlqvist, Grace P.
McGeough, Catherine P.
Paymode, Dinesh J.
Cardoso, Flavio S. P.
Lucas, Tobias
Dietz, Jule-Phillip
Opatz, Till
Jamison, Timothy F.
Gupton, Frank B.
Date Issued
October 2020
Journal
Chemical Communications
Publisher
Royal Society of Chemistry (RSC)
Citation
Vasudevan, N, Ahlqvist, Grace P, McGeough, Catherine P, Paymode, Dinesh J, Cardoso, Flavio SP et al. 2020. "A concise route to MK-4482 (EIDD-2801) from cytidine." Chemical Communications, 56 (87).
Version
Final published version
Abstract
© The Royal Society of Chemistry. 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. This journal is
MIT Department
Massachusetts Institute of Technology. Department of Chemistry
Terms of Use
Creative Commons Attribution NonCommercial License 3.0
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DOI of Published Version
https://doi.org/10.1039/d0cc05944g
