Department of Chemistry and Biochemistry, The City College of New York, 160 Convent Avenue, New York, NY 10031, USA.
Department of Chemistry, Institute of Chemical Technology, Nathalal Parekh Road, Matunga, Mumbai 400019, India.
Org Biomol Chem. 2024 Jan 24;22(4):735-740. doi: 10.1039/d3ob02039h.
Molnupiravir, the prodrug for β-D--hydroxycytidine (NHC), is marketed by Merck as Lagevrio™ 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.
莫努匹韦，β-D--羟基胞苷（NHC）的前药，由默克公司以 Lagevrio™商品名上市，用于治疗轻度至中度 COVID-19，获得 FDA 紧急使用授权。它是首款针对该疾病的口服药物。本工作描述了两种通过酰胺活化尿苷的方法来合成 NHC 和莫努匹韦，使用的试剂分别为肽偶联试剂和 4-氯嘧啶核苷中间体。
