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

被引：39

作者：

Vasudevan, N. ^{[1
]}

Ahlqvist, Grace P. ^{[2
]}

McGeough, Catherine P. ^{[2
]}

Paymode, Dinesh J. ^{[1
]}

Cardoso, Flavio S. P. ^{[1
]}

Lucas, Tobias ^{[3
]}

Dietz, Jule-Phillip ^{[3
]}

Opatz, Till ^{[3
]}

Jamison, Timothy F. ^{[2
]}

Gupton, Frank B. ^{[1
]}

Snead, David R. ^{[1
]}

机构：

[1] Med All Inst, 737 N 5th St,Box 980100, Richmond, VA 23298 USA

[2] MIT, Dept Chem, 77 Massachusetts Ave, Cambridge, MA 02139 USA

[3] Johannes Gutenberg Univ Mainz, Dept Chem, Duesbergweg 10-14, D-55128 Mainz, Germany

来源：

CHEMICAL COMMUNICATIONS | 2020年 / 56卷 / 87期

基金：

美国国家科学基金会;

关键词：

REGIOSELECTIVE ACYLATION;

D O I：

10.1039/d0cc05944g

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

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.

引用

页码：13363 / 13364

页数：2

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