Chemical compounds

摘要

Aryl substituted phosphoryl derivatives of the formula In which Ar is phenyl, naphthyl, or pyridyl, Y is O or S, X¹ is O, NR³, S, CR³R⁴, CR³W¹ or CW¹W², X² and X⁶ are a bond or X⁶ is CH₂ and X² is O, NR³, S, CR³R⁴, CR³W¹ or CW¹W², R³ and R⁴ are H, alkyl or phenyl, groups, W¹ and W² are heteroatoms, X³ is alkylene, X⁴ is oxygen or CH₂, X⁵ is a bond or CH₂, Z is O, NR⁵, S, alkyl or phenyl, R⁵ is H, alkyl or phenyl, J is H, alkyl, phenyl, or a heterocyclic or polycyclic group, Q is O, NR⁶, S, CR⁶R⁷, CR⁶W³ or CW³W⁴, R⁶ and R⁷ are H, alkyl or phenyl, and W³ and W⁴ are hetero atoms, T¹ and T² are H or CH₂R⁸, R⁸ is H, OH or F, or T¹ and T² together are -CH-CH- or -C(R⁹)(R¹⁰)C(R¹¹)(R¹²)-, R⁹ is H, halogeno, CN, NH₂, CO-alkyl, or alkyl, R¹⁰, R¹¹, and R¹² are H, N₃, halogen, CN, NH₂, CO-alkyl, or alkyl, and B is a purine or pyrimidine base, have antiviral activity, as for example against HIV. Particularly preferred are thymine and adenine derivatives of amino acid phenoxyphosphoroamidates. A typical embodiment is 2',3'-dideoxy-2',3'-didehydrothymidine 5'-(phenyl methoxy alaninyl) phosphoroamidate which can be prepared from phenyl methoxy alaninyl phosphorochloridate and 2',3'-dideoxy-2',3'-didehydrothymidine.