A concise route to MK-4482 (EIDD-2801) from cytidine
A concise route to MK-4482 (EIDD-2801) from cytidine
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DOI：
10.1039/d0cc05944g
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发表时间：
2020-11-11
影响因子：
4.9
通讯作者：
Snead, David R.
中科院分区：
文献类型：
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作者：
Vasudevan, N.;Ahlqvist, Grace P.;Snead, David R.
以胞苷为原料，经酯化和羟胺化两步反应合成MK-4482(EIDD-2801，1)。选择性酰化和直接胺化消除了保护和活化基团的需要，总收率为75%，比报道的17%的产率有了显著的提高。步骤数从五次转化减少到两次，昂贵的尿苷被更可用的胞苷取代。
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.