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氚标记伯氨喹磷酸盐的制备

PREPARATION OF [~3H]-LABELLED PRIMAQUINE SALT

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【作者】 沈德福; 马远鸣; 赵夏令;

【Author】 SHEN DEFU, MA YUANMING, ZHAO XIALING(Shanghai Institute of Nucleonic, Academia Simca and Department of Physical Chemistry, School of Pharmacy, Shanghai Medical University, Shanghai)

【机构】 中国科学院上海原子核研究所; 上海医科大学药学院物理化学教研室; 中国科学院上海原子核研究所;

【摘要】 本文报道用氚气与磷酸伯氨喹在二氧六环溶液中进行催化同位素交换制备氚标记伯氨喹磷酸盐([3H]PQ),所得产品的放射性比度为4.4×1010Bq/mmol,其放化纯度为95%以上,都比国外报道为高。经质谱证实[3H]标记位置可能在喹啉环上,得率为40%以上。

【Abstract】 3H-Primaquine was prepared by isotopio exchange between [3H]-gas and primaquine through PdO/BaSO4 catalysation in dioxane solution. The specific radioactivity equaled 4.4×1010 Bq/mmol and radiochemical purity was over 95%, much higher than other past reports. The [3H] was labeled at the position of the quinoline ring and was proven by mass spectrometry. The yield obtained was over 40%.

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