STEREOSELECTIVE SYNTHESIS AND PROCESS FOR THE MANUFACTURING OF 2'-DEOXYNUCLEOSIDES

STEREOSELECTIVE SYNTHESIS AND PROCESS FOR THE MANUFACTURING OF 2'-DEOXYNUCLEOSIDES

Methods for stereoselective synthesis and manufacturing of 2'-deoxynucleosides, such as 2'-ribonucleosides, are disclosed. In some embodiments, the 2'-deoxynucleoside is a ß-anomer of 2'-deoxynucleoside having a 3' a hydroxyl, 4' ß hydroxymethyl configuration. Nonlimiti...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: DENYSENKO, SERGIY M, BAHDE, ROBERT, ZHANG, LIANHAO, MORRIS, JOEL, VISHNUVAJJALA, BABURAO, LOPEZ, OMAR DIEGO, WISHKA, DONN GREGORY
Format: Patent
Sprache:eng ; fre
Schlagworte:
CHEMISTRY
DERIVATIVES THEREOF
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
SUGARS
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Beschreibung
Zusammenfassung:Methods for stereoselective synthesis and manufacturing of 2'-deoxynucleosides, such as 2'-ribonucleosides, are disclosed. In some embodiments, the 2'-deoxynucleoside is a ß-anomer of 2'-deoxynucleoside having a 3' a hydroxyl, 4' ß hydroxymethyl configuration. Nonlimiting examples of compounds prepared by the disclosed methods include 4'-thio-2'-deoxycytidine (T-dCyd) and 5-aza-4'-thio-2'-deoxycytidine (5-aza-T-dCyd; aza-T-dCyd; aza-T-dC). L'invention concerne des procédés de synthèse stéréosélective et de fabrication de 2'-désoxynucléosides, tels que des 2'-ribonucléosides. Dans certains modes de réalisation, le 2'-désoxynucléoside est un ß-anomère de 2'-désoxynucléoside ayant une configuration 3'a hydroxyle, 4'ß hydroxyméthyle. Des exemples donnés à titre non limitatif de composés préparés par les procédés selon l'invention comprennent 4'-thio-2'-désoxycytidine (T-dCyd) et 5-aza-4'-thio-2'-désoxycytidine (5-aza-T-dCyd ; aza-T-dCyd ; aza-T-dC).