Synthesis and Evaluation of Diastereoisomers of 1, 4, 7-Triazacyclononane-1, 4, 7-tris-(glutaric acid)(NOTGA) for Multimeric Radiopharmaceuticals of Gallium

…, T Uehara, T Rokugawa, Y Higaki, H Suzuki…

Index: Gomez, Francisco L. Guerra; Uehara, Tomoya; Rokugawa, Takemi; Higaki, Yusuke; Suzuki, Hiroyuki; Hanaoka, Hirofumi; Akizawa, Hiromichi; Arano, Yasushi Bioconjugate Chemistry, 2012 , vol. 23, # 11 p. 2229 - 2238

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Citation Number: 10

Abstract

In the conventional synthesis of 1, 4, 7-tris-(glutaric acid)-1, 4, 7-triazacyclononane (NOTGA), four isomeric species are usually generated by the alkylation of 1, 4, 7- triazacyclononane with α-bromoglutaric acid diester. To estimate their biological efficacies as well as their stability and radiochemistry, the RRR/SSS and RRS/SSR NOTGA-tBu prochelators were isolated and the corresponding cyclic RGDfK (RGD) conjugates with ...