2-Nitrophenol (88-75-5)

The condensation of 2-nitrophenol (I) with 2,2,2-trrifluoroethyl p-toluenesulfonate (II) by means of K₂CO₃ in DMF gives 2-(2,2,2-trifluoroethoxy) nitrobenzene (III), which isreduced with H₂ over PtO₂ in ethanol yiedling the aniline (IV). The cyclization of (IV) with bis (2-chloroethyl)amine (V) and K₂CO₃ affords the piperazine (VI), which is condensed with 1-benzyl-3-(3-chloro-propyl)-5-methylpyrimidine-2,4(1H,3H)-dione (VII) by means of K₂CO₃ in refluxing acetonitrile to give the benzylated target compound (VIII). Finally, this compound is deprotected by hydrogenation with ammonium formate and Pd/C. The intermediate pyrimidine (VII) has been obtained by benzylation of thymine (IX) with benzyl bromide and K₂CO₃ to give the 1-benzylthymine (X), which is alkylated with 1-bromo-3-chloropropane and K₂CO₃ to the target intemediate (VII).