基本信息:
- 专利标题: 4’−置換ヌクレオシド誘導体の立体選択的合成法
- 申请号:JP2019031293 申请日:2019-08-08
- 公开(公告)号:JPWO2020032152A1 公开(公告)日:2021-08-10
- 发明人: 向後 悟 , 松浦 智子
- 申请人: ヤマサ醤油株式会社
- 申请人地址: 千葉県銚子市新生町2丁目10番地の1
- 专利权人: ヤマサ醤油株式会社
- 当前专利权人: ヤマサ醤油株式会社
- 当前专利权人地址: 千葉県銚子市新生町2丁目10番地の1
- 优先权: JP2018149849 2018-08-09 JP2019087957 2019-05-08
- 主分类号: C07H1/00
- IPC分类号: C07H1/00 ; C07H9/04 ; C07H19/00 ; C07H19/067 ; C07H15/04
Current synthesis methods for 4'-substituted nucleoside derivatives include a step in which stereoisomers are produced and therefore have problems such as decreased yield and complication of a refinement step. Thus, a synthesis method has been sought that is simpler and does not produce stereoisomers. The present invention provides a synthesis method for a 4'-substituted nucleoside intermediate represented by formula (6), the method comprising the following steps 1 through 3: step 1 in which a compound of formula (3) is used as a starting raw material, and a nucleophile is made to act on the compound of formula (3) to obtain the compound of formula (4) in which a substituent group has been stereoselectively introduced; step 2 in which the compound of formula (4) is hydrolized to obtain the compound of formula (5); and step 3 in which the compound of formula (5) is held in acidic conditions to obtain the compound represented by formula (6). In the formulas, R1 indicates a protective group of a hydroxyl group, Me indicates a methyl group, and X indicates a substituent group.
公开/授权文献:
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