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KMID : 1145520150010020080
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Journal of Radiopharmaceuticals and Molecular Probes
2015 Volume.1 No. 2 p.80 ~ p.87
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Recent advances of aromatic C-F bond borylation and its application to positron emission tomography
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Song Dal-Nim
Lee Sang-Hee
Lee Byung-Chul
Kim Sang-Eun
Lee Eun-Sung
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Abstract
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Carbon-fluorine (C-F) bonds have been found ubiquitously in pharmaceuticals, radiopharmaceuticals, agrochemicals, and material science due to their unique properties such as thermal and oxidative stability and lipophilicity to improve bioavailability. For the past five years, there have been significant advances in F-18 fluorination of aromatic complex molecules combined with the development of late-stage fluorination reactions. More recently, direct incorporation of F-18 to fluorinated aromatic molecules via borylation of C-F bonds has been developed by Niwa and Hosoya. In this minireview, we will discuss the progress of C-F bondborylation of fluorinated arenes utilizing transition metal catalysts and the impact on the development of F-18 radiotracers for positron emission tomography (PET).
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KEYWORD
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F-18 fluorination, Carbon-fluorine activation, Borylation, Catalysis
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