Development of [18F]trifluoromethylation reaction by using of reactivity of boron substituent

• Project/Area Number: 25861138
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Radiation science
• Research Institution: National Institute of Radiological Sciences
• Principal Investigator: Fujinaga Masayuki 国立研究開発法人放射線医学総合研究所, 分子イメージング研究センター, 研究員 (70623726)
• Project Period (FY): 2013-04-01 – 2016-03-31
• Project Status: Completed (Fiscal Year 2015)
• Budget Amount: ¥3,380,000 (Direct Cost: ¥2,600,000、Indirect Cost: ¥780,000); Fiscal Year 2015: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000); Fiscal Year 2014: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000); Fiscal Year 2013: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
• Keywords: 有機ホウ素化合物 / トリフルオロメチル化 / KF

Outline of Final Research Achievements

In this study, we developed a novel trifluoromethylation reaction with aryl boronic acid derivatives from two routes. As a result, transformation of CF2CO2Et or CF2PO(OEt)2 group into CF3 group were not proceeded. On the other hand, in the case of using CuCF3, which was prepared from CuI, ClCF2CO2Na and KF, the desired compound was obtained in low yield. This method was also found to be obtained some byproducts. Thus, further study is needed for the method