Diarylthiopyrimidines and pyridines: Synthesis and biological activity

Abstract

Prior work with diarylethers of pyrimidine, pyridine, and benzene showed encouraging antitumor results. As an extension of that work the synthesis of diarylthio derivatives of pyrimidine and pyridine has been accomplished. The synthetic scheme employed the nucleophilic displacement of chlorines from trichloropyrimidine, 1, dichloropyrimidines 4 and 6, and 2,6-dichloropyridine 8 using the anion of thiophenols 2. Antitumor evaluation by the National Cancer Institute showed no useful activity.