Synthesis method of ribonucleic acid H-phosphonate monomer and oligonucleotide synthesis using this monomer

摘要

The present invention relates to a method for synthesizing ribonucleic acid H-phosphonate monomers and a method for synthesizing oligonucleotides using the monomers. The present invention relates to a method for producing an H-phosphonate-nucleoside derivative that can selectively protect the 2'-position of a ribonucleoside monomer necessary for RNA oligonucleotide synthesis and can be produced at low cost. In the present invention, the 2′-position and 3′-position hydroxyl groups having slightly different reactivity are reacted with an aromatic acyl halide at a low temperature to perform selective esterification at the 2′-position, followed by one-pot It is characterized in that the 3′-position hydroxyl group is captured by a phosphityl group so that the 2′-position and 3′-position transition of the acyl group is not caused.