SONOGASHIRA CROSS-COUPLING IN THE SYNTHESIS OF ACYCLIC NUCLEOSIDE PHOSPHONATES:PREPARATION OF 6-[(PHOSPHONOMETHOXY)ALKYNYL]-AND 6-[(PHOSPHONOMETHOXY)ALKYL]PYRIMIDINES

摘要

Several 6-[(phosphonomethoxy)alkyl]pyrimidines and 6-[(phosphonomethoxy)alkynyl]-pyrimidines were prepared as saturated and unsaturated carba-analogues of antivirally active 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]pyrimidine.As the key step of their synthesis the Sonogashira cross-coupling reaction was successfully applied.The replacement of the C-O moiety_by the C-C bond resulted in the loss of biological activity.