| ~3H和~(14)C标记常咯啉的合成 |
| |
| 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(5). |
| |
| 作者姓名： | 章辛 鲍跃文 丁瑞勤 |
| |
| 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) |
| |
| 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)
|
| 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 |
| |
| Zhang Xin Bao Yuewen Eihg Ruiqin.Synthesis of ~3H,and ~(14)C labelled changrolin[J].Nuclear Techniques,1988(5). |
| |
| Authors: | Zhang Xin Bao Yuewen Eihg Ruiqin |
| |
| 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). |
| |
| Keywords: | ~3H and ~(14)C labelled changrolin antiarrhythlnic agent |
| 本文献已被 CNKI 等数据库收录！ |
|
