ENZYMATIC SYNTHESIS OF 4'-ETHYNYL NUCLEOSIDE ANALOGS

The present invention relates to an enzymatic synthesis of 4′-ethynyl-2′-deoxy nucleosides and analogs thereof, for example EFdA, that eliminates the use of protecting groups on the intermediates, improves the stereoselectivity of glycosylation and reduces the number of process steps needed to make...

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Bibliographische Detailangaben
Hauptverfasser: Truppo, Matthew, Huffman, Mark A, Campos, Kevin R, Fryszkowska, Anna, Kolev, Joshua N, Devine, Paul N, Nawrat, Christopher C
Format: Patent
Sprache:eng
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Zusammenfassung:The present invention relates to an enzymatic synthesis of 4′-ethynyl-2′-deoxy nucleosides and analogs thereof, for example EFdA, that eliminates the use of protecting groups on the intermediates, improves the stereoselectivity of glycosylation and reduces the number of process steps needed to make said compounds. It also relates to the novel intermediates employed in the process.