Enriched 10B-diboron reagents synthesis from 10BF3

Stable isotopes have become vital tools in drug development and discovery. Because of the unique high neutron absorption properties of boron-10, boron neutron capture therapy (BNCT) has been considered as an ideal technology for cancer treatment. Along with the promising progress of accelerator neutron sources, the efficient synthesis of 10B-enriched molecular carriers becomes crucial for BNCT drug development. However, there is a lack of enriched 10B-reagent available for installing 10B in various carriers. Herein, we developed a synthesis of 10B-enriched diboron(4) reagents from the primary source of boron-10, 10BF3. The conversion of BF3 to chloro-diaminoboron in the presence of chlorosilane and diamine is crucial for its success. The synthesis of these diboron(4) reagents will not only build up an efficient bridge between inorganic 10B-source and numerous organic 10B-molecules but also benefit boron-related mechanistic studies. The use of 10B2pin2 in several catalytic borylation technologies produces various organo-10B compounds, including the approved BNCT drug 10B-L-BPA.