C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 19/167 (2006.01) C07D 473/00 (2006.01) C07H 19/16 (2006.01) C07H 23/00 (2006.01)
Patent
CA 2266089
Novel intermediates of nucleoside derivatives, of which the 6-position of the nucleic acid base moiety is substituted with a halogen atom, are produced. Using those novel intermediates, even substrates, of which the 3'-position of the saccharide moiety is deoxylated, can be substituted at the 2'-position at an extremely high yield. Specifically, by subjecting a 3'-deoxy derivative of inosine to 6-halogenation to give a 6-halide of the derivative, and then subjecting it to 2'-deoxylation/substitution with a fluorine atom or the like, followed by further subjecting it to substitution with an amino group, a hydroxyl group or any other intended substituent at the 6-positioned halogen atom, nucleoside derivatives are produced at a high yield. Methods for producing nucleoside derivatives including 9-(2,3-dideoxy-2-fluoro-.beta.-D-threo- pentofuranosyl)adenine (FddA) and their related compounds, in a simplified manner, at a high yield and at low costs , and especially Economical methods for substituting substrates, of which the 3'-position of the saccharide moiety is deoxylated, at the 2'-position to produce those nucleoside derivatives on an industrial scale are also provided.
Hirose Naoko
Izawa Kunisuke
Katayama Satoshi
Maruyama Tokumi
Takamatsu Satoshi
Ajinomoto Co. Inc.
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
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