发明名称 Labeled nucleosides and method for their preparation
摘要 <p>The invention relates to a method for the chemical preparation of labeled nucleosides via an oxidative-ring-opening step and a reductive-ring-closure step starting from a labeled D-glucose nucleoside resulting in the corresponding D-ribose-nucleoside by removing the carbon atom 3 on the glucose and comprising the steps of: 1. a protection of the sugar ring hydroxyl groups, 2. a sugar-base condensation, whereby the base is a purine or a pyrimidine, 3. a deprotection of the sugar ring hydroxyl groups, 4. an oxidative-ring-opening and removal of the carbon atom 3, and 5. a reductive-ring-closure resulting in labeled D-ribose-nucleoside. The invention further relates to a compound obtainable via the method according to the invention having the formula selected from Ä&lt;13&gt;C,&lt;15&gt;NÜ labeled 6'-O-mono- or 6'-O-bis-C1-C6-alkyloxytrityl-D-glycopyranosyl nucleosides, or Ä&lt;13&gt;C,&lt;15&gt;NÜ labeled tetra-O-acetyl-D-glycopyranosyl nucleosides or Ä&lt;13&gt;C,&lt;15&gt;NÜ labeled glycopyranosyl nucleosides.</p>
申请公布号 EP1186306(A1) 申请公布日期 2002.03.13
申请号 EP20000870188 申请日期 2000.09.05
申请人 K.U. LEUVEN RESEARCH & DEVELOPMENT 发明人 LAGOJA, IRENE;HERDEWIJN, PIET
分类号 A61K51/04;(IPC1-7):A61K51/04 主分类号 A61K51/04
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