Synthesis and Biological Profiling of Benzofuro‐Fused 7‐Deazapurine Nucleosides

A series of benzofuro‐fused 7‐deazapurine (6H‐furo[2,3‐e]pyrimido[4,5‐b]indole) 2’‐deoxyribo‐ and ribonucleosides was designed synthesized. The synthesis key 10‐chloro‐6H‐furo[2,3‐e]pyrimido[4,5‐b]indole based on the Negishi cross‐coupling iodobenzofurane with zincated 4,6‐dichloropyrimidine followed by azidation photochemical cyclization. Glycosylation heterocycle either Hoffer’s chlorodeoxyribose or protected ribose substitution reactions at position 10 gave desired two sets final nucleosides that showed moderate to weak cytostatic activity interesting fluorescence properties.