Cytosine compounds and a process for the production thereof

Details Cytosine compounds and a process for the production thereof Cytosine compounds and a process for the production thereof

C - Chemistry, Metallurgy

07

H

C07H 19/06 (2006.01) C07H 19/24 (2006.01)

Patent

CA 2012096

Compounds of Formula I: (see fig. I) wherein R1 is selected from the group comprising a trifluoromethyl group, a C1-C6 alkyl group and a C6-C9 aryl group, and R2 is selected from the group comprising hydrogen, trityl, methoxytrityl, dimethoxytrityl, acetyl, a C2-C6 alkylacyl group, a C6-C9 arylacyl group, allyl, 2,2,2-trichloroethyl, phosphates and salts thereof, tosyl and mesyl, and a process for the production thereof are provided. The compound of Formula I or the corresponding pharmaceutically acceptable salt (or the neutral form of the compound of Formula I) may then be converted to the corresponding compound of Formula V, or pharmaceutically acceptable salts thereof: (see fig. V) wherein R2 is as defined above. Compounds of Formula I and V are useful for inhibition of DNA synthesis.

Composés de formule I (voir fig. I) (I), où R1 est choisi parmi le groupe comprenant un trifluorométhyle, un alkyle C1-C6 et un aryle C6-C9, R2 est choisi parmi le groupe comprenant de l'hydrogène, du trityle, du méthoxytrityle, du diméthoxytrityle, de l'acétyle, un alkylacyle C2-C6, un arylacyle C6-C9, un allyle, un 2,2,2-trichloroéthyle, leurs phosphates et sels, le tosyle et le mésyle; méthode pour préparer ces composés. Le composé de formule I ou le sel correspondant acceptable en pharmacie (ou la forme neutre du composé de formule I) peuvent ensuite être convertis en composés correspondant de formule V, ou en leurs sels acceptables en pharmacie : (voir fig. I) (V) avec R2 défini comme ci-dessus. Les composés de formules I et V sont utiles pour l'inhibition de la synthèse de l'ADN.

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