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

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

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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 sign...

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Bibliographic Details
Main Authors: Vasudevan, N (Author), Ahlqvist, Grace P (Author), McGeough, Catherine P (Author), Paymode, Dinesh J (Author), Cardoso, Flavio SP (Author), Lucas, Tobias (Author), Dietz, Jule-Phillip (Author), Opatz, Till (Author), Jamison, Timothy F (Author), Gupton, Frank B (Author), Snead, David R (Author)
Format: Article
Language:English
Published: Royal Society of Chemistry (RSC), 2022-03-09T15:25:53Z.
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Summary:© 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

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