Facile C−F Bond Activation Approach to FAMT-Based Difluoromethyl-BNCT Drug Candidates

Akitaka Yokawa, Miho Hatanaka, Koichi Mikami

Research output: Contribution to journalArticlepeer-review

4 Citations (Scopus)


Lithium 1,3-bis(2,6-diisopropylphenyl)-1,3,2-diazaborolidinyl-2-uide activates the C−F linkage of fluoroform (CF3H) to provide air-stable difluoromethylborane compounds. Computational analysis of SN2-type transition state for the C−F bond activation of fluoroform with boryllithium clarifies the mechanism involving the lithium dimeric species in the pre-reaction complex. FAMT (=3-fluoro-l-α-methyl-tyrosine)-based difluoromethyl-BNCT (boron neutron capture therapy) drug candidates is thus produced by the present C−F bond activation.

Original languageEnglish
Article numbere2000211
JournalHelvetica Chimica Acta
Issue number2
Publication statusPublished - 2021 Feb
Externally publishedYes


  • BNCT drug
  • C−F bond activation
  • boron
  • boryllithium
  • difluoromethylation
  • drug design
  • fluoroform

ASJC Scopus subject areas

  • Catalysis
  • Biochemistry
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry


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