New carbocyclic phosphonate-nucleotide analogues - are effective antiviral agents against retroviral infections, e.g. HIV

摘要

1-(4-Phosphonylmethoxycyclopentyl)- thymine esters of formula (I) and their salts are new; where R1 and R2 are H or 1-6C alkyl, but not both H. Cpds. (I) and 1-(4-phosphonylmethoxycyclopentyl)- thymine (II) and their salts are also claimed as medicaments. USE - (I) and (II), which is described in J. Chem. Soc. Chem. Commun., 312 (1991), are antiviral agents esp. useful for treating retroviral (esp. HIV) infections. In an example, a soln. of 4.63g 1-((IRS,4SR)- 4-diisopropylphosphonylmethoxy-2-cyclopentenyl)- thymine in 100 ml i-PrOH was treated with 500 mg Pd/C (10%), hydrogenated at room temp., and worked up to give 4.64g (99.7%) of 1-((IRS,4SR)-4-diisopropylphosphonylmethoxy- cyclopentyl)- thymine, m.pt. 82 deg.C.