Process for the preparation of 2′-O-alkyl-guanosine, cytidine, and uridine phosphoramidites
First Claim
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1. A process for preparing an oligonucleotide that comprises at least one 2′
- -O-alkylated cytidine nucleotide comprising;
alkylating a cytidine to form a 2′
-O-alkylated cytidine;
blocking the 5′
-hydroxyl moiety of said 2′
-O-alkylated cytidine;
phosphitylating the 3′
-position of said 5′
-blocked 2′
′
-alkylated cytidine to form a 2′
-O-alkylated cytidine 3′
-O-phosphoramidite; and
coupling said 2′
-O-alkylated cytidine 3′
-O-phosphoramidite with a 5′
-hydroxyl moiety on an oligonucleotide utilizing phosphoramidite coupling conditions.
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Abstract
Processes for preparing 2′-O-alkylated guanosine, uridine, cytidine, and 2,6-diaminopurine 3′-O-phosphoramidites include the steps of alkylating nucleoside precursors, adding suitable blocking groups and phosphitylating. For the guanosine 2′-O-alkylated 3′-O-phosphoramidites, alkylation is effected on 2,6-diamino-9-(β-D-ribofuranosyl) purine followed by deamination. For uridine 2′-O-alkylated 3′-O-phosphoramidites, alkylation is effect on a dialkyl stannylene derivative of uridine. For cytidine 2′-O-alkylated 3′-O-phosphoramidites, alkylation is effected directly on cytidine. Alkylation is effected directly upon 2,6-diaminopurine.
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1 Claim
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1. A process for preparing an oligonucleotide that comprises at least one 2′
- -O-alkylated cytidine nucleotide comprising;
alkylating a cytidine to form a 2′
-O-alkylated cytidine;
blocking the 5′
-hydroxyl moiety of said 2′
-O-alkylated cytidine;
phosphitylating the 3′
-position of said 5′
-blocked 2′
′
-alkylated cytidine to form a 2′
-O-alkylated cytidine 3′
-O-phosphoramidite; and
coupling said 2′
-O-alkylated cytidine 3′
-O-phosphoramidite with a 5′
-hydroxyl moiety on an oligonucleotide utilizing phosphoramidite coupling conditions.
- -O-alkylated cytidine nucleotide comprising;
Specification