SOLID-PHASE PREPARATION OF 5', 3'-HETEROBIFUNCTIONAL OLIGODEOXYRIBONUCLEOTIDES USING MODIFIED SOLID SUPPORTS

The solid-phase preparation of oligodeoxyribonucleotides attached to intercalator or reactive groups through their 5'- and (or) 3'-ends is reported. These syntheses implicate the introduction of suitable masked functional groups at the 5'-end of the oligonucleotide by the intermediate of their phosphoramidite derivatives or at the 3'-end of the oligonucleotide using modified solid supports. After full deblocking, the functional groups (phosphate, thiophosphate, primary amine or thiol) can be reacted with the suitable reactive group involved in the chosen ligand. These methods allow the preparation of heterobifunctional derivatized oligodeoxyribonucleotides.