Process for the preparation of 2'-O-alkyl purine phosphoramidite

Details Process for the preparation of 2'-O-alkyl purine phosphoramidite Process for the preparation of 2'-O-alkyl purine phosphoramidite

1998-10-02

2000-10-17

Wilson, James O.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

536 2671, 536 2672, 536 2781, 536 285, 536 2851, C07H 2100, C07H 1906

Patent

active

061334383

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-(.beta.-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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