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    • 72. 发明公开
    • FLUORINATION METHOD
    • FLUORIERUNGSVERFAHREN
    • EP3119737A1
    • 2017-01-25
    • EP15713569.0
    • 2015-03-20
    • Oxford University Innovation Limited
    • GOUVERNEUR, VeroniqueTREDWELL, MatthewPRESHLOCK, Sean
    • C07B59/00C07F5/04
    • C07B59/002C07B59/00C07B59/001C07B2200/05C07C17/361C07C37/62C07C41/22C07C45/65C07C67/317C07C201/12C07C209/74C07C231/12C07C253/30C07C303/40C07D209/08C07D215/18C07D277/30C07D295/073C07D295/16C07F5/025C07F5/04Y02P20/55
    • 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.
    • 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。
    • 76. 发明公开
    • COMPOUNDS AND THEIR SYNTHESIS
    • VERBINDUNGEN UND DEREN SYNTHESE
    • EP2906548A1
    • 2015-08-19
    • EP13783361.2
    • 2013-10-14
    • UCL Business Plc.
    • ARSTAD, ErikSANDER, KerstinGENDRON, Thibault
    • C07D333/74C07D333/76C07D401/06C07C381/12C07D207/46C07D211/22C07D211/70C07D213/70A61K51/04A61K51/06A61K51/08
    • C07C381/12B01D15/08B01J20/22C07B59/001C07B59/002C07C17/361C07C25/13C07C45/65C07C47/55C07C49/807C07C67/317C07C69/78C07D207/46C07D211/20C07D211/22C07D211/32C07D211/70C07D213/61C07D213/70C07D333/74C07D333/76C07D401/06C07D403/06
    • The present invention relates to sulfonium salts of formula (I): (I), their preparation, and utility as precursors for preparing functionalised organic compounds, wherein R1 and R2 are the same or different and each is independently selected from an optionally substituted aryl group, an optionally substituted alkynyl group, an optionally substituted alkenyl group, an optionally substituted alkyl group, an optionally substituted cycloalkyl group, an optionally substituted cycloalkenyl group, an optionally substituted aralkyl group, an optionally substituted arylalkenyl group, an optionally substituted heteroaryl group, an optionally substituted heterocyclyl group, an optionally substituted amine, an optionally substituted alkoxy group, an optionally substituted thioether group, an optionally substituted phosphine group, an optionally substituted boron species, an optionally substituted carbene, an organometallic moiety, and a halide, or R1 and R2 are joined together to form an optionally substituted sulfur-containing ring; W is a bond, an optionally substituted alkynylene group, an optionally substituted alkenylene group, and optionally substituted alkylene group, an optionally substituted heterocyclyl group, an optionally substituted aryl group or an optionally substituted heteroaryl group; R3 is a moiety comprising at least one basic group, provided that when R3 does not contain any carbon atoms, W is not a bond; X is an anionic species; and n is an integer selected from 1 to 5.
    • 本发明涉及式(I)的锍盐:(I),其制备和用作制备官能化有机化合物的前体,其中R 1和R 2相同或不同,并且各自独立地选自任选取代的芳基 ,任选取代的炔基,任选取代的烯基,任选取代的烷基,任选取代的环烷基,任选取代的环烯基,任选取代的芳烷基,任选取代的芳基烯基,任选取代的杂芳基, 任选取代的杂环基,任选取代的胺,任选取代的烷氧基,任选取代的硫醚基,任选取代的膦基,任选取代的硼种,任选取代的卡宾,有机金属部分和卤化物,或R 1和 R2连接在一起形成一个选项 取代的含硫环; W是键,任选取代的亚炔基,任选取代的亚烯基和任选取代的亚烷基,任选取代的杂环基,任选取代的芳基或任选取代的杂芳基; R3是包含至少一个碱性基团的部分,条件是当R3不含任何碳原子时,W不是键; X是阴离子物种; n为1〜5的整数。