Abstract

Synthesis of (2-methoxy-5-dihydroxyborylphenyl)alanine, (2-butoxy-5-dihydroxyborylphenyl) alanine, and (2-methoxy-4-dihydroxyborylphenyl)alanine for Boron Neutron Capture Therapy is described. In the key step, the amino acid functionality was introduced by the Wittig reaction. The approach provides a general access to alkoxy substituted boronated phenylalanines.

Keywords: boronated amino acids, boron neutron capture therapy, boronates, boronic acids, wittig reaction