Expeditious preparation of PET probes by molecular renovation strategy enabled by inert-bond cleavage
Project/Area Number |
15K05509
|
Research Category |
Grant-in-Aid for Scientific Research (C)
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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
|
Project Status |
Completed (Fiscal Year 2017)
|
Budget Amount *help |
¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2017: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2016: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2015: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
|
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 / フルオロアルケン / ミミック化合物 / 陽電子放射断層撮像(PET) / 脱フッ素ホウ素化 / 脱カルボニルホウ素化 / アリールスルフィド / ロジウム触媒 / 銅触媒 / 炭素–フッ素結合切断 / 結合活性化 / ニッケル / 銅 / 共触媒 |
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.
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Report
(4 results)
Research Products
(67 results)