| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2016: ¥780,000 (Direct Cost: ¥600,000、Indirect Cost: ¥180,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2014: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
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| Outline of Final Research Achievements |
Hitherto unknown difluoromethylated (CF2H) boron derivatives should be employed as a brand-new BNCT (boron neutron capture therapy)drugs. The CF2H moiety has been recognized as one of the lipophilic bioisostere of hydroxy group. The CF2H-B derivatives are thus expected to be the key in the development of novel biofunctional compounds such as L-amino acids-based difluoromethylboron congener for BNCT.
We have already developed the Umpolung approach of fluoroform (HCF3, HFC-23) for the synthesis of difluoromethyl-substituted compounds. The C-F bond in CF3H can be activated and hence substituted by appropriate organolithium nucleophiles. Therefore, nucleophilic boryllithium is promising to synthesize the desired air-stable difluoromethylated boron compounds via the C-F activation. We herein demonstrate the C-F activation of fluoroform by boryllithium. Structural characterization of the difluoromethylated boron compounds was also carried out.
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