公开(公告)号：WO2015140572A1

公开(公告)日：2015-09-24

申请号：PCT/GB2015/050831

申请日：2015-03-20

Applicant: ISIS INNOVATION LIMITED

Inventor： GOUVERNEUR, Veronique ,  TREDWELL, Matthew ,  PRESHLOCK, Sean

IPC: C07B59/00 ,  C07F5/04

CPC classification number: C07B59/002 ,  C07B59/00 ,  C07B59/001 ,  C07B2200/05 ,  C07C17/361 ,  C07C37/62 ,  C07C41/22 ,  C07C45/65 ,  C07C67/317 ,  C07C201/12 ,  C07C209/74 ,  C07C231/12 ,  C07C253/30 ,  C07C303/40 ,  C07D209/08 ,  C07D215/18 ,  C07D277/30 ,  C07D295/073 ,  C07D295/16 ,  C07F5/025 ,  C07F5/04 ,  Y02P20/55

Abstract: The present invention relates to a process for producing an organic compound comprising an 18 F atom. The compounds comprising an 18 F 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 sp 2 hybridised carbon atom, with (i) 18 F – 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 sp 2 hybridised carbon atom, in a process for producing an organic compound comprising an 18 F atom, which process comprises treating the organoboron compound with (i) 18 F – and (ii) a copper compound. The invention also provides a compound of formula (XXXVII): wherein: each PG A is independently H or an alcohol protecting group; PG B is H or a carboxylic acid protecting group; each PG C 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.

Abstract translation: 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，该有机硼化合物包含与sp2杂化的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，该有机硼化合物包含与sp2杂化的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。