Abstract 5-Chlorouracil-linked-pyrazolo [1, 5-a][1, 3, 5] triazines were designed as new thymidine phosphorylase inhibitors based on the fragment based drug design approach. Multiple-step convergent synthetic schemes were devised to generate the target compounds. The intermediate 5-chloro-6-chloromethyluracil was synthesized by a 4-step reaction. A series of the second bicyclic intermediates, namely pyrazolo [1, 5-a][1, 3, 5] ...
