ULTRAFAST CLEAVAGE AND DEPROTECTION OF OLIGONUCLEOTIDES SYNTHESIS ANDUSE OF C-AC DERIVATIVES

We have investigated the use of alkylamines as fast cleavage and depro tection reagents for the solid phase synthesis of oligonucleotides and found methylamine/ammonium hydroxide (or methylamine) as an efficient reagent. The transamination side product formed with the commonly use d dC(bz) has been eliminated by the use of dC(Ac) phosphoramidite. Thi s system has successfully been used in the synthesis of oligonucleotid es and oligonucleoside phosphorothioates. DMT dC(Ac) hydrogen phosphon ate and DMT ribo C-Ac-2'-OMe phosphoramidite also have been prepared a nd used in the synthesis of oligonucleotides.