PRODUCTION METHOD FOR RIBONUCLEOSIDE PHOSPHOROTHIOATE

摘要

PROBLEM TO BE SOLVED: To provide a stereoselective production method of ribonucleoside phosphorothioate which is expected to have high nuclease resistance and cell membrane permeability.SOLUTION: In the synthetic process of phosphorothioate RNA by the oxazaphospholidine method, high condensation efficiency is obtained without impairing diastereoselectivity by using cyanoethoxy methyl group as a protective group of 2'-OH group of RNA, and by using N-(cyanomethyl) pyrrolidinium triflate or N-phenyl imidazolium triflate as a nucleophilic agent.SELECTED DRAWING: None