Synthesis of 1-(phosphonomethoxyalkoxy)pyrimidines, a novel series of acyclonucleotide analogues

A convenient synthesis of 1-(2-phosphonomethoxyalkoxy)uracil and -thymine derivatives, 4-7 by Mitsunobu coupling of 1-hydroxypyrimidines with suitably functionalized alcohols is described. The uracil analogues were converted to the corresponding 1-(phosphonomethoxyalkoxy)cytosines 8, 9 via intermediate 4-(1,2,4-triazol-1-yl) derivatives. The antiviral activity of this series of compounds is reported