| abstract |
The present invention provides a series of cytotoxic phosphoramidate analogs of 5-fluoro-2'-deoxyrudine of general formula (I), wherein R1 is H, F or (C¿1?-C4)alkyl; R?2¿ is CH¿2?CH2X wherein X is Cl, Br, I or p-toluenesulfonyl; R?3¿ is (C¿1?-C4)alkyl or CH2CH2X wherein X is Cl, Br, I or p-toluenesulfonyl; or wherein R?2 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 pharmaceutically acceptable salts thereof. |