Development of positron emitter labeled agents for boron neutron capture therapy

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In this study, we tried to establish a new practical method for synthesis of4-borono-2-fluoro-L-phenylalanine (FBPA) via nucleophilic substitution reaction with fluoride to apply it to preparation of 18F-FBPA. The strategy was that bromonitrobenzaldehyde was used as starting material and phenylalanine scaffold was constructed after nucleophilic a fluorination. We evaluated the reactions that compose the synthetic pathway. However, it turned out to be difficult to synthesize FBPA through the synthesis pathway especially due to the difficulty in introducing boronic acid group into the aryl ring.