Development of the first and practical method for enantioselective synthesis of 10B-enriched p-borono-l-phenylalanine

At present p-(10B)borono-l-phenylalanine (l-10Bpa) is used clinically as an excellent 10B carrier for BNCT; however, its enantioselective synthesis has not been reported yet. The present Letter describes the first and practical method for enantioselective synthesis of 10B-enriched l-Bpa using Z-l-Ser-OMe as the chiral synthon in good total yield and high optical purity.