| ~3H和~(14)C标记常咯啉的合成 |
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| 引用本文： | 章辛,鲍跃文,丁瑞勤. ~3H和~(14)C标记常咯啉的合成[J]. 核技术, 1988, 0(5) |
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| 作者姓名： | 章辛 鲍跃文 丁瑞勤 |
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| 作者单位： | 中国科学院上海药物研究所(章辛，鲍跃文)，中国科学院上海药物研究所(丁瑞勤) |
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| 摘 要： | 本文用合成方法制备了抗心律不齐新药常咯啉的三种不同位置~3H和~(14)C的标记化合物。以5-溴邻氨基苯甲酸按Scheme 1经5步反应得6-溴代常咯啉(Ⅵ),Ⅵ用氚经催化脱卤得[6-~3H]常咯啉(Ⅰ)用[~(14)]甲酸制成[~(14)C]甲酰胺,按Scheme 1经二步反应得[2~(14)C]5-氯代喹唑啉(V,R=H)再按Sc-heme2即得[2-~(14)C]常咯啉(Ⅱ)。以[~(14)C]甲醛为原料按Schemel的最后一步可直接制得(甲撑-~(14)C)常咯啉(Ⅲ)
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| 关 键 词： | ~(14)CH和~3H 标记常咯啉 抗心律不齐药 |
Synthesis of ~3H,and ~(14)C labelled changrolin |
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| Zhang Xin Bao Yuewen Eihg Ruiqin. Synthesis of ~3H,and ~(14)C labelled changrolin[J]. Nuclear Techniques, 1988, 0(5) |
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| Authors: | Zhang Xin Bao Yuewen Eihg Ruiqin |
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| Abstract: | In this paper 3 kinds of [14C] and (3H) changrolin labelled at different positions (I,II , III) were prepared. The synthesis of I was illustrated in Scheme 1. Heating 5-bromoanthranilic acid with formamide yielded IV, which, on heating with POCl3 gave V. Condensation of V with 4-aminophenol and then subjected to Mannich reaction produced 6-bromochangrolin (VI), Catalytic dehalogenation of VI with tritium gas gave I.The synthesis of n was started from (14C) formamide and anthranilic acid. Labelled 4-chloroquine obtained was condensed with Mannich base (VII) directly (Scheme 2).III was prepared by 1 step with (14C) formaldehyde, (Scheme 1). |
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| Keywords: | ~3H and ~(14)C labelled changrolin antiarrhythlnic agent |
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