An improved synthesis of cis,cis-1,3,5-triaminocyclohexane. Synthesis of novel hexadentate ligand derivatives for the preparation of gallium radiopharmaceuticals
An improved synthesis of cis,cis-1,3,5-triaminocyclohexane. Synthesis of novel hexadentate ligand derivatives for the preparation of gallium radiopharmaceuticals
复制标题
DOI：
10.1016/0960-894x(96)00110-2
复制
发表时间：
1996-04-09
影响因子：
2.7
通讯作者：
Brechbiel, MW
中科院分区：
文献类型：
--
作者：
Bowen, T;Planalp, RP;Brechbiel, MW
顺式，顺式-1,3,5-三氨基环己烷的改进合成，产率为 82%，涉及市售的顺式，顺式-1,3,5-环己烷三甲酸与 DPPA 反应，得到三（氨基甲酸苄酯）作为 Curtius 重排产物。脱保护产生三胺，三胺作为可以组装各种螯合结构的平台。制备新型三(2-亚甲基吡啶基)三胺和三(2-亚甲基噻吩基)三胺配体以研究它们用作镓放射性药物的适用性。
An improved synthesis of cis,cis-1,3,5-triaminocyclohexane in 82% yield involves reaction of the commercially available cis,cis-1,3,5-cyclohexanetricarboxylic acid with DPPA to afford the tri(benzylcarbamate) as the Curtius rearrangement product Deprotection yields the triamine which serves as a platform from which a variety of chelating structures may be assembled. Novel tris(2-methylenepyridyl)triamine and tris(2-methylenethienyl)triamine ligands are prepared to investigate their suitability for use as gallium radiopharmaceuticals.