2'-Fluorofuranosyl derivatives and methods for preparing 2'-fluo

Details 2'-Fluorofuranosyl derivatives and methods for preparing 2'-fluo 2'-Fluorofuranosyl derivatives and methods for preparing 2'-fluo

1990-07-23

1998-10-06

Wilson, James O.

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

Organic compounds

Carbohydrates or derivatives

536 271, 536 2711, 536 2713, 536 2721, 536 276, 536 278, 536 2781, 536 281, 536 285, 536 2853, 536 2854, C07H 100

Patent

active

058177990

ABSTRACT:
A method of preparing a 2'-fluoro compound of the formula ##STR1## where B is selected from the group consisting of purines and pyrimidines, both of which may be substituted, comprises reacting a compound of the formula II(a) or II(b) ##STR2## where R and R' are as defined in the specification with an acid halide under conditions effective to obtain a halide of the formula ##STR3## where X is a halogen. A silane of the formula B-Si (R").sub.3 where R" is as defined in the specification, is added to this product (III) under conditions effective to obtain a compound of the formula (IV) ##STR4## The compound of formula (IV) is reacted with a reagent selected from the group consisting of ammonia, BCl.sub.3 and ((C.sub.1 -C.sub.10)alkyl).sub.4 NF, under conditions effective to obtain the compound of formula (I). The compounds of formula (I) resulting from these methods exhibit anti-HIV activities and are useful for therapy against the HIV virus.

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