Two short approaches to the COVID-19 drug β-<sc>d</sc>-N4-hydroxycytidine and its prodrug molnupiravir

被引:1
作者
Persaud, Kevin E. [1 ]
Sahu, Rajesh R. [2 ]
Neary, Michelle C. [3 ]
Kapdi, Anant R. [2 ]
Lakshman, Mahesh K. [1 ]
机构
[1] CUNY City Coll, Dept Chem & Biochem, 160 Convent Ave, New York, NY 10031 USA
[2] Inst Chem Technol, Dept Chem, Nathalal Parekh Rd, Mumbai 400019, India
[3] Hunter Coll, Dept Chem, 695 Pk Ave, New York, NY 10065 USA
关键词
SCALE SYNTHESIS; EIDD-2801; FACILE; NUCLEOSIDE; MK-4482; ROUTE;
D O I
10.1039/d3ob02039h
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Molnupiravir, the prodrug for beta-d-N-4-hydroxycytidine (NHC), is marketed by Merck as Lagevrio (TM) against mild-moderate COVID-19, under FDA emergency use authorization. It is the first oral drug against the disease. This work describes two synthetic approaches to NHC and molnupiravir by amide activation in uridine with a peptide-coupling agent and with a 4-chloropyrimidinone nucleoside intermediate.
引用
收藏
页码:735 / 740
页数:6
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