Synthesis of C- and N-functionalised derivatives of 1,4,7-triazacyclononane-1,4,7-triyltriacetic acid (NOTA), 1,4,7,10-tetra-azacyclododecane-1,4,7,10-tetrayltetra-acetic acid (DOTA), and diethylenenetriaminepenta-acetic acid (DTPA): bifunctional complexing agents for the derivatisation of antibodies
作者:Jonathan P. L. Cox、Andrew S. Craig、Ian M. Helps、Karl J. Jankowski、David Parker、Michael A. W. Eaton、Andrew T. Millican、Kenneth Millar、Nigel R. A. Beeley、Byron A. Boyce
DOI:10.1039/p19900002567
日期:——
Using (2S)-lysine as a precursor, the syntheses of aminobutyl derivatives of 1,4,7-triazacyclononane, 1,4,7,10-tetra-azacyclododecane, and 3-azapentane-1,5-diamine are described. Transformation into their reactive maleimide derivatives is described and alternative strategies for synthesising the title complexing agents involving nitrogen functionalisation are defined.
描述了使用(2S)-赖氨酸作为前体,合成了1,4,7-三氮杂环壬烷,1,4,7,10-四氮杂环十二烷和3-氮杂戊烷-1,5-二胺的氨基丁基衍生物。描述了向其反应性马来酰亚胺衍生物的转化,并且定义了用于合成涉及氮官能化的标题络合剂的替代策略。