Practical protocol of preparation of [18F]CF3 labelled probe for diagnostic agents

2016 Fiscal Year Final Research Report

• Project/Area Number: 26713041
• Research Category: Grant-in-Aid for Young Scientists (A)
• Allocation Type: Partial Multi-year Fund
• Research Field: Radiation science
• Research Institution: Nagasaki University
• Principal Investigator: MIZUTA Satoshi 長崎大学, 医歯薬学総合研究科(医学系), 助教 (50717618)
• Research Collaborator: OTAKI Hiroki 長崎大学, 医歯薬学総合研究科(医学系), 助教 ; WATANABE Ken 長崎大学, 医歯薬学総合研究科(医学系), 助教 ; ISHIKAWA Takeshi 長崎大学, 医歯薬学総合研究科(医学系), 准教授
• Project Period (FY): 2014-04-01 – 2017-03-31
• Keywords: フッ素含有ヘテロ環 / フッ素化反応 / イミダゾリウム塩 / イオン性液体 / 生理活性物質

Outline of Final Research Achievements

Our group addressed to development of new methods for synthesis of trifluoromethyl compounds via a fluorination reaction as a key step. Reactions of dibromofluoromethylthio substrates with KF and silver(I) salt were performed affording the trifluoromethylthio products. The F-CF2S bond forming reaction might be available for the hot fluorination reaction with radio isotope. Alternatively, we have developed methods for synthesis of new trifluoromethyl compounds. As one examples, phase transfer catalysts, trifluoromethylthio substituted imidazolium salts from thiourea and electrophilic trifluoromethylating reagents have been synthesized.In addition, dibromo-2-trifluoromethyl acrylic acid ethyl ester found to be a versatile platform for the stereoselective preparation of functionalized-α-trifluoromethyl α,β-unsaturated lactones and trifluoromethyl pyrazolinones. Ionic liquid-mediated hydrofluorination of 3-bromooxindoles also have been achieved.

Free Research Field

有機化学、放射線科学