A General Method for the Synthesis of 2′‐O‐Modified Ribonucleosides

A general way for the functionalization of ribonucleosides is described. The method involves the synthesis of the methyl‐ribofuranoside derivative 6 equipped with a linker at the 2‐hydroxy group ( Scheme 2 ). After introduction of the nucleic‐acid bases under standard conditions ( Scheme 3 ), the resulting β‐ D ‐ribonucleosides 8 and 10 are further transformed to derivatives with lipophilic, intercalating, and aminoalkyl residues at the linker moiety. In this way, 2′‐modified 5‐methyluridines 12 , adenosines 13 , and 5‐methylcytidines 15 and 16 were prepared ( Scheme 4 ).