Method for preparing organoboron derivative containing oxygen and aromatic ring as labeled precursor of dopamine positron emission tomography imaging agent
申请人:INSTITUTE OF NUCLEAR ENERGY RESEARCH, ATOMIC ENERGY COUNCIL, EXECUTIVE YUAN, R.O.C.
公开号:US10934314B1
公开(公告)日:2021-03-02
A method for preparing organoboron derivatives containing oxygen atoms and an aromatic ring as labeled precursors of dopamine positron emission tomography imaging agents is revealed. Hydrochloride salt of cocaine is used as an initiator. Organoboron derivatives containing oxygen atoms are directly produced on an aromatic ring as drug substances and the aromatic ring is directly labeled with radioisotope fluorine-18 (F-18). The method takes only five steps including four steps for preparing organoboron derivatives containing oxygen atoms and an aromatic ring as drug substances and a step of labeling the aromatic ring of the organoboron derivatives with F-18 directly. Not only the process time is significantly reduced, the total yield rate is also improved effectively.
揭示了一种制备含氧原子和芳香环的有机硼衍生物作为多巴胺正电子发射断层扫描成像剂的标记前体的方法。可卡因的盐酸盐被用作引发剂。含氧原子的有机硼衍生物直接在芳香环上生成作为药物物质,并且芳香环直接标记了放射性同位素氟-18(F-18)。该方法仅需五个步骤,包括四个步骤用于制备含氧原子和芳香环的有机硼衍生物作为药物物质,以及一步用于直接将有机硼衍生物的芳香环标记为F-18。不仅显著缩短了过程时间,还有效提高了总产率。