一条从胞苷出发合成MK-4482（EIDD-2801）的简洁路线。
A concise route to MK-4482 (EIDD-2801) from cytidine.
作者信息
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
机构信息
Medicines for All Institute, 737 N. 5th St., Box 980100, Richmond, VA 23298-0100, USA.
出版信息
Chem Commun (Camb). 2020 Nov 11;56(87):13363-13364. doi: 10.1039/d0cc05944g. Epub 2020 Oct 8.
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.
开发了一条合成MK-4482（EIDD-2801，1）的两步路线，该路线由胞苷的酯化和羟胺化反应组成。选择性酰化和直接胺化反应无需使用保护基和活化基，总产率为75%，相较于报道的17%的产率有显著提高。反应步骤从五步减少到两步，并且用更易获得的胞苷替代了昂贵的尿苷。
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