Synthesis and biophysical characterization of R-6'-Me-α-L-LNA modified oligonucleotides.

Abstract The synthesis and biophysical properties of R -6′-Me-α- l -LNA, which has a methyl group in the ( R ) configuration on the 2′,4′-bridging substituent of α- l -LNA, is reported. The synthesis of the uracil nucleobase phosphoramidite was efficiently accomplished in 14 steps and 8 chromatographic purifications starting from a known sugar intermediate. Biophysical evaluation revealed that substitution along the edge of the major groove does not impair the high affinity duplex forming ability of α- l -LNA modified oligonucleotides.