申请人:OSAKA UNIVERSITY
公开号:US20200369578A1
公开(公告)日:2020-11-26
The invention relates to a method of producing the radiolabeled aryl compound (I) Ar—X, or a salt thereof, wherein X is
211
At,
210
At,
123
I,
124
I,
125
I, or
131
I. The method involves reacting the aryl boronic acid compound (II) Ar—Y, or a salt thereof, wherein Y is a borono group (—B(OH)
2
) or an ester group thereof, with a radionuclide selected from
211
At,
210
At,
123
I,
124
I,
125
I and
131
I, in the presence of an oxidizing agent selected from an alkali metal iodide, an alkali metal bromide, N-bromosuccinimide, N-chlorosuccinimide and hydrogen peroxide, in water.
本发明涉及一种制备放射性标记的芳基化合物(I)Ar-X或其盐的方法,其中X为211At、210At、123I、124I、125I或131I。该方法涉及在水中,在碱金属碘化物、碱金属溴化物、N-溴代琥珀酰亚胺、N-氯代琥珀酰亚胺和过氧化氢选一种氧化剂的存在下,将芳基硼酸化合物(II)Ar-Y或其盐,其中Y为硼酸基(—B(OH)2)或其酯基,与从211At、210At、123I、124I、125I和131I中选择的放射性核素反应。