Synthesis of novel benzoxaborole-containing phenylalanine analogues

The synthesis of novel benzoxaborole-containing phenylalanine analogues 2 and 3 has been developed. The key steps involve the preparation of appropriate precursors from the readily available amino acids and the formation of benzoxaborole ring directly in the corresponding amino acid fragment. The resulting compounds 2-3 show improved water solubility at physiological pH, suggesting their potential use as boron delivery agents for boron neutron capture therapy. (C) 2011 Elsevier Ltd. All rights reserved.