Importance

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Abstract

Aryl substituted phosphoryl derivatives of the formula ##STR1## In which Ar is phenyl, naphthyl, or pyridyl, Y is O or S, X.sup.1 is O, NR.sup.3, S, CR.sup.3 R.sup.4, CR.sup.3 W.sup.1 or CW.sup.1 W.sup.2, X.sup.2 and X.sup.6 are a bond or X.sup.6 is CH.sub.2 and X.sup.2 is O, NR.sup.3, S, CR.sup.3 R.sup.4, CR.sup.3 W.sup.1 or CW.sup.1 W.sup.2, R.sup.3 and R.sup.4 are H, alkyl or phenyl, groups, W.sup.1 and W.sup.2 are heteroatoms, X.sup.3 is alkylene, X.sup.4 is oxygen or CH.sub.2, X.sup.5 is a bond or CH.sub.2, Z is O, NR.sup.5, S, alkyl or phenyl, R.sup.5 is H, alkyl or phenyl, J is H, alkyl, phenyl, or a heterocyclic or polycyclic group, Q is O, NR.sup.6, S, CR.sup.6 R.sup.7, CR.sup.6 W.sup.3 or CW.sup.3 W.sup.4, R.sup.6 and R.sup.7 are H, alkyl, or phenyl, and W.sup.3 and W.sup.4 are hetero atoms, T.sup.1 and T.sup.2 are H or CH.sub.2 R.sup.8, R.sup.8 is H, OH or F, or T.sup.1 and T.sup.2 together are --CH.dbd.CH-- or --C(R.sup.9)(R.sup.10)C(R.sup.11)(R.sup.12)--, R.sup.9 is H, halogeno, CN, NH.sub.2, CO-alkyl, or alkyl, R.sup.10, R.sup.11, and R.sup.12 are H, N.sub.3, halogen, CN, NH.sub.2, 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 phenoxyphosphoroamides. 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.

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First Claim