Process for the preparation of 2,2'-anhydro- and 2'...

C - Chemistry – Metallurgy – 07 – H

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C07H 19/06 (2006.01) C07H 19/04 (2006.01) C07H 19/12 (2006.01)

Patent

CA 2171518

A process for the preparation of compounds of the formula: Image wherein -Pg and R are protecting groups and B is a nucleobase. The process uses protected nucleobases to form 2,2'-anhydro nucleosides having the formula Image which are hydrolyzed to 2'-hydroxy intermediates which are then oxidized to the desired 2'-keto compounds. The compounds and intermediates are useful as antiviral and antitumor agents and as intermediates to 2,2'-anhydro-1-(.beta.-D- arabinofuranosyl)cytosine (anhydro-ara-C) and 1-.beta.-D- arabinofuranosylcytosine (Ara-C).

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