Direct Access to Unique C?5’?Acyl Modified Nucleosides through Liebeskind–Srogl Cross?Coupling Reaction

The chemical functionalization at C-5’ position of nucleosides has been significantly less studied compared to the C-1’, C-2’ and C-3’ sugar positions in spite its potential important role for biological activity. We describe here synthesis new carbothioate which were then engaged a Liebeskind-Srogl reaction with various boronic acids preparation diversely modified C-5’-acyl nucleosides. Applied pyrimidine DNA RNA series, showed broad substrate scope more than 25 examples synthesized good-to-excellent isolated yields. This general efficient Pd-catalyzed Cu(I)-mediated cross-coupling represents convenient method prepare diverse set 5’-modified paves way further transformation into variety potentially bioactive compounds via possible conversion C-5’-ketone.