Synthesis of tyrosyl-DNA phosphodiesterase I inhibitors

[Display omitted] •Efficient glycosylation.•Synthesis of tyrosyl inhibitors using cheap and readily available starting materials.•Simple and efficient synthesis of compounds 3 and 5 with good overall yield. The first report for the synthesis of tyrosyl-DNA phosphodiesterase I inhibitors 3,4-dimethoxyphenol-1-β-d-(6′-O-galloyl)glucopyranoside 3 and 3-(4-hydroxy-3-methoxyphenyl)propane-1,2-diol 2-β-d-(6′-O-galloyl) glucopyranoside 5 has been accomplished starting from readily available d-glucose as a starting material. An efficient and general approach has been reported for the synthesis of compounds 3 and 5 with an overall yield of 26% and 27%, respectively.