A concise route to MK-4482 (EIDD-2801) from cytidine
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.; Snead, David R.; ... Show more Show less
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© 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
Date issued
2020-10Department
Massachusetts Institute of Technology. Department of ChemistryJournal
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
ISSN
1359-7345
1364-548X