A SIMPLE METHOD FOR THE PREPARATION OF I-123 AND I-125 LABELED IODOBENZODIAZEPINES

被引：0
|
作者：
MCBRIDE, BJ [1 ]
BALDWIN, RM [1 ]
KERR, JM [1 ]
WU, JL [1 ]
机构：
[1] MEDIPHYS INC,EMERYVILLE,CA 94608
来源：
APPLIED RADIATION AND ISOTOPES | 1991年 / 42卷 / 02期
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D O I：
暂无
中图分类号：
O61 [无机化学];
学科分类号：
070301 ; 081704 ;
摘要：
The tributyltin derivative of the benzodiazepine antagonist ethyl 7-iodo-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate (Ro 16-0154) was synthesized by a one-step Pd catalyzed reaction between bistributyltin and Ro 16-0154. Electrophilic iodination of the tributyltin compound with no-carrier-added I-125 and I-123 gave a 50-70% radiochemical yield of a greater than 98% radiochemically pure Ro 16-0154. The specific activity of [I-123]Ro 16-0154 and [I-125]Ro 16-0154 was 180,000 and 1700 Ci/mmol, respectively, but the effective specific activity was 6900 and 300 Ci/mmol due to the presence of benzodiazepine impurities which have similar receptor binding properties.
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页码：173 / 175
页数：3
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