摘要 |
PROBLEM TO BE SOLVED: To provide an industrially useful method for introducing a fluorine atom to the 3'-αposition of a nucleoside derivative by a few number of processes in a high yield, consequently at a low cost. SOLUTION: A nucleoside derivative containing a hydroxy group or a silylated hydroxy group at the 2'-αposition and a halogen atom except a fluorine atom at the 3'-βposition is reacted with a dialkylaminosulfur trifluoride to transfer the halogen atom to the 2'-βposition to give a wholly new compound fluorinated at the 3'-αposition. Further the halogen atom except the fluorine atom at the 2'-βposition of the compound is reduced, a hydroxy group at the 5'-position is deprotected and, if required, protection, deprotection and modification of nucleic acid base are carried out to synthesize the objective nucleoside derivative fluorinated at the 3'-αposition and deoxidized at the 2'-position.
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