Concise synthesis of antiviral drug, molnupiravir by direct coupling of fully protected D-Ribose with cytosine
Sahoo, Tanmoy 1Reddy, B. V. Subba1
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作者信息
1. Indian Inst Chem Technol
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Abstract
A four step synthetic process has been developed for the synthesis of orally active ribonucleoside molnupiravir (MK-4482 & EIDDD-2801), starting from a readily available D-ribose. The synthesis involves the formation of acetonide from secondary hydroxy groups of the ribose, isobutrylation of primary and anomeric hydroxy groups, ribosylation of cytosine and one-pot hydroxyamination of cytosine ring along with the hydrolysis of acetonide. It is an effective process that can replace the high cost starting materials like uridine or cytidine that are being used in previous synthetic routes for MK-4482. The use of low cost starting materials with less number of synthetic steps is expected to expand access to molnupiravir. (c) 2022 Elsevier Ltd. All rights reserved.
NSTL
Elsevier