发明名称 NUCLEOTIDE DERIVATIVE AND METHOD FOR PRODUCING THE SAME
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.
申请公布号 JP2001122891(A) 申请公布日期 2001.05.08
申请号 JP19990307545 申请日期 1999.10.28
申请人 AJINOMOTO CO INC 发明人 TAKAMATSU SATOSHI;NAITO MASAKI;YAMASHITA KEIZO;INAYAMA TAKASHI;IZAWA KUNISUKE
分类号 C07H19/06;C07H19/16;(IPC1-7):C07H19/06 主分类号 C07H19/06
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