Improvement of the C-glycosylation Step for the Synthesis of Remdesivir
ORGANIC PROCESS RESEARCH & DEVELOPMENT(2020)
摘要
The bulk supply of the antiviral C-nucleoside analogue remdesivir is largely hampered by a low-yielding Cglycosylation step in which the base is coupled to the pentose unit. Here, we disclose a significantly improved methodology for this critical transformation. By utilizing diisopropylamine as a cost-effective additive, the addition reaction furnishes an optimal yield of 75% of the desired ribofuranoside adduct, representing the highest yield obtained thus far for this key step. The method proved suitable for hectogram scale synthesis without column chromatographic operations.
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关键词
diisopropylamine,C-glycosylation,remdesivir,COVID-19
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