Synthesis of 4-Amino-8-(2, 2-Difluoro-2-deoxy-β-d-ribo Furanosyl Amino)Pyrimido [5, 4-D]pyrimidine (dfarpp). Stability and Cellular Cytotoxicity

The synthesis of beta-dFARPP was accomplished by Mitsunobu coupling of 6-cyanopurine with 2-deoxy-2,2-difluororibose followed by purine ring-expansion under the action of methanolic ammonia. The title compound inhibited the growth of proliferating human leukemic CCRF-CEM cells at 6.1 mu g/ml but had no effect on plaque formation by a variety of DNA and RNA viruses.