PREPARATION METHOD OF RIBONUCLEIC ACID HAVING ALKYL PROTECTIVE GROUP AT POSITION 2'

摘要

PROBLEM TO BE SOLVED: To provide a method for selectively and efficiently introducing an alkyl protective group such as a 2-cyanoethoxymethyl (CEM) group to a hydroxyl group at position 2' in a ribonucleic acid within a short step in a state wherein hydroxyl groups at positions 3' and 5' are not protected or only the hydroxyl group at position 5' is protected.

SOLUTION: The ribonucleic acid of formula [II] (wherein BASE is a nucleobase which may have a protective group; R1is a protective group of a hydrogen atom or a hydroxyl group; R2is an alkyl group; X is a leaving group; and Ar is an aryl group) wherein the alkyl protective group is introduced to the hydroxyl group at position 2' is prepared by reacting a boronate of a ribonucleic acid of formula [I], prepared in the presence of an arylboronic acid, with an alkylating agent of formula [III] in the presence of a Lewis base and a silver compound.

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