Process for the preparation of 1-(2'-deoxy-2',2'-difluoro-...

C - Chemistry – Metallurgy – 07 – H

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C07H 19/073 (2006.01) C07H 7/04 (2006.01) C07H 13/00 (2006.01) C07H 15/18 (2006.01) C07H 19/06 (2006.01)

Patent

CA 2168080

A process for the preparation of 1-(21-deoxy- 2',2'-difluoro-D-ribo-pentofuranosyl)-cytosine (VI) from 2-deoxy-2,2-difluoro-.beta.-D-ribo-pentopyranose (I). The process uses a tritylation reaction (Step 3) for preparing 2-deoxy-2,2-difluoro-5-O-triphenylmethyl-ribo- pentofuranose (II) as a key intermediate. The 1-(2'- deoxy-2',21-difluoro-D-ribo-pentofuranosyl)-cytosine (VI) is an antiviral and anti-cancer agent.

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