两种四乙酸四氮杂环烷化合物的合成

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在氢氧化钾存在下,1,4,7,10-四氮杂环十二烷与溴乙酸进行N-羧甲基化反应,得到N,N′N″N-四乙酸1,4,7,10-四氛杂环十二烷(DOTA,I),经重结晶纯化,产率88.1%.在碳酸钾存在下,1,4,8,11-四氮杂环十四烷与溴乙酸卡酯进行反应,生成N-乙酸苄酯中间体.该中间体在室温和4.04×105Pa氢气压力下,用Pd/C地催化氢解脱苄基得到N,N′N″N-四乙酸1,4,8,11-四氮杂环十四烷(TETA,Ⅲ),产率56.0%。 N, N-carboxymethylation of 1,4,7,10-tetraazacyclododecane with bromoacetic acid in the presence of potassium hydroxide affords 1, 4, 7 , 10-tetraazacyclododecane (DOTA, I) was purified by recrystallization to yield 88.1%. In the presence of potassium carbonate, 1,4,8,11-tetraazacyclotetradecane was reacted with The reaction of benzyl bromoacetate to form benzyl N-benzyl acetate intermediates was carried out by catalytic hydrogenolysis of benzylidene with Pd / C at room temperature under hydrogen pressure of 4.04 × 10 5 Pa to obtain N, N’N "N- Tetraacetic acid 1,4,8,11-tetraazacyclotetradecane (TETA, III) was obtained in a yield of 56.0%.
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