Phosphoramidate analogs of 5-fluoro-2'-deoxyuridine

Details Phosphoramidate analogs of 5-fluoro-2'-deoxyuridine Phosphoramidate analogs of 5-fluoro-2'-deoxyuridine

C - Chemistry, Metallurgy

07

H

C07H 19/10 (2006.01)

Patent

CA 2119351

The present invention provides a series of cytotoxic phosphoramidate analogs of 5-fluoro-2'-deoxyrudine of general for- mula (I), wherein R1 is H, F or (C1-C4)alkyl; R2 is CH2CH2X wherein X is Cl, Br, I or p-toluenesulfonyl; R3 is (C1-C4)alkyl or CH2CH2X wherein X is Cl, Br, I or p-toluenesulfonyl; or wherein R2 and R3, taken together with the N atom, can be 5- or 6-membered heterocyclic ring which is aliphatic or aliphatic interrupted by a ring oxygen or a second ring nitrogen; R4 is H, one equivalent of a pharmaceutically-acceptable cation or (4,4,6- trimethyltetrahydro-1,3-oxazin-2-yl)ethyl, and the pharma- ceutically acceptable salts thereof.

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