This invention discloses a high-
boron-loading
manganese-based
boron drug for BNCT diagnosis and treatment, its preparation, and its application, belonging to the fields of
biomedicine and
nuclear medicine. The
boron drug structure is shown in general formula 7, with
manganese porphyrin as the core skeleton. A
benzene ring
side chain at the meso position of the
porphyrin ring is connected to a boron-10-containing
catechol borate ester group via an
amide bond. All boron atoms are boron-10 isotopes. The preparation method includes: first constructing the
manganese porphyrin skeleton through condensation, cyclization, and
metal coordination reactions; then independently preparing boron source units; and finally obtaining the target product through
amide bond
coupling. This boron
drug possesses high boron-10 loading, efficient blood-brain barrier penetration, and excellent
MRI imaging performance, enabling real-time and precise monitoring of boron drug distribution
in vivo. The quantitative correlation between imaging signals and
boron concentration guides the timing of
neutron irradiation, integrating MRI tracing and BNCT treatment, effectively solving the problems of low boron loading, inability to penetrate the blood-brain barrier, and difficulty in real-time monitoring of
in vivo distribution in existing boron drugs.