Expeditious preparation of PET probes by molecular renovation strategy enabled by inert-bond cleavage

2017 Fiscal Year Final Research Report

• Project/Area Number: 15K05509
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Synthetic chemistry
• Research Institution: Institute of Physical and Chemical Research
• Principal Investigator: Niwa Takashi 国立研究開発法人理化学研究所, ライフサイエンス技術基盤研究センター, 副チームリーダー (30584396)
• Co-Investigator(Renkei-kenkyūsha): ZHANG Zhouen 国立研究開発法人理化学研究所, ライフサイエンス技術基盤研究センター, 研究員 (00416207)
• Project Period (FY): 2015-04-01 – 2018-03-31
• Keywords: ホウ素化反応 / 遷移金属触媒 / 不活性結合切断反応 / PETプローブ / 標識反応 / 分子プローブ / PET

Outline of Final Research Achievements

To realize expeditious preparation of PET probes, we proposed a novel synthetic strategy for them by using a bioactive compound in interest as a starting material. In this project, we named the novel strategy “molecular renovation strategy” and developed borylation reactions and a 11C-labeling reaction that are required to realize this idea. Utilizing boron compounds prepared by the newly developed methods as common intermediates, we achieved synthesis of various molecular probes such as a PET probe within two steps, demonstrating practicality of the synthetic strategy.

Free Research Field

有機反応化学