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本文合成了抗心律失常新药常咯啉的~3H和~(14)C标记化合物。5-溴邻氨基苯甲酸按常咯啉类似合成方法经四步反应生成6-溴代常咯啉(Ⅰ),Ⅰ在钯碳催化下通氚制得[6-~3H]-常咯啉(Ⅱ)。[~(14)C]-甲酸铵脱水得[~(14)C]-甲酰胺后经三步反应制得[2-~(14)C]-常咯啉(Ⅲ)。4-(对羟
In this paper, ~ 3H and ~ (14) C labeled compounds of anti-arrhythmic new drugs, 5-Bromo-anthranilic acid was synthesized by the method of analogous synthesis of the pyrroline analog by four steps to form 6-bromocyclic morpholine (Ⅰ). I was tritiated with palladium on carbon to give [6- ~ 3H] (Ⅱ). The [2- (14) C] -normal statin (Ⅲ) was prepared by the reaction of [~ (14) C] - ammonium formate after dehydration to give [~ (14) C] 4- (p-hydroxy