
基本信息:
- 专利标题: FLUORINATION METHOD
- 专利标题(中):FLUORIERUNGSVERFAHREN
- 申请号:EP15713569.0 申请日:2015-03-20
- 公开(公告)号:EP3119737A1 公开(公告)日:2017-01-25
- 发明人: GOUVERNEUR, Veronique , TREDWELL, Matthew , PRESHLOCK, Sean
- 申请人: Oxford University Innovation Limited
- 申请人地址: Buxton Court 3 West Way Botley Oxford OX2 0SZ GB
- 专利权人: Oxford University Innovation Limited
- 当前专利权人: OXFORD UNIVERSITY INNOVATION LIMITED
- 当前专利权人地址: OXFORD UNIVERSITY INNOVATION LIMITED
- 代理机构: Silcock, Peter James
- 优先权: GB201405002 20140320
- 国际公布: WO2015140572 20150924
- 主分类号: C07B59/00
- IPC分类号: C07B59/00 ; C07F5/04
摘要:
The present invention relates to a process for producing an organic compound comprising an 18F atom. The compounds comprising an 18F can be useful as PET ligands for use in diagnostics and/or scanning. The process of the invention comprises treating an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp2 hybridised carbon atom, with (i) 18F – and (ii) a copper compound. The invention also provides the use of an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp2 hybridised carbon atom, in a process for producing an organic compound comprising an 18F atom, which process comprises treating the organoboron compound with (i) 18F – and (ii) a copper compound. The invention also provides a compound of formula (XXXVII): wherein: each PGA is independently H or an alcohol protecting group; PGB is H or a carboxylic acid protecting group; each PGC is independently an amine protecting group; Z is a group selected from a boronic ester group, a boronic acid group, a borate group, and a trifluoroborate group; and a is an integer from 0 to 4.
摘要(中):
本发明涉及一种制备包含18F原子的有机化合物的方法。 包含18F的化合物可用作用于诊断和/或扫描的PET配体。 本发明的方法包括处理有机硼化合物,其有机硼化合物包含与sp2杂化碳原子键合的硼原子,与(i)18 F-和(ii)铜化合物。 本发明还提供有机硼化合物的用途,该有机硼化合物包括与sp2杂化碳原子键合的硼原子,所述有机硼化合物在制备包含18 F原子的有机化合物的方法中,所述方法包括用(i) 18F-和(ii)铜化合物。 本发明还提供式(XXXVII)化合物:其中:各PGA独立地为H或醇保护基; PGB是H或羧酸保护基; 每个PGC独立地是胺保护基; Z是选自硼酸酯基,硼酸基,硼酸酯基和三氟硼酸酯基的基团; a为0〜4的整数。
IPC结构图谱:
C | 化学;冶金 |
--C07 | 有机化学 |
----C07B | 有机化学的一般方法;所用的装置 |
------C07B59/00 | 有机化合物中引入同位素 |