Karel Pomeisl, R. Pohl, A. Holý
2005
Citations
0
Influential Citations
16
Citations
Journal
Collection of Czechoslovak Chemical Communications
Abstract
A novel method of transformation of HOCH 2 group to FCH 2 was successfully applied to the preparation of fluorine-containing pyrimidine acyclic nucleoside phosphonates (FPMP compounds) such as ( S )- and ( R )-1-[3-fluoro-2-(phosphonomethoxy)propyl]thymine ( 7a , 7b ) (FPMPT). The key displacement of hydroxy group with fluorine in 1-{2-[(diisopropoxyphosphoryl)- methoxy]-3-hydroxypropyl}-4-methoxy-5-methylpyrimidin-2(1 H )-one ( 5a , 5b ) was performed using perfluorobutane-1-sulfonyl fluoride in the presence of DBU. Novel pyrimidine acyclic nucleoside phosphonates were investigated as inhibitors of thymidine phosphorylase.