대한핵의학회지 (1967년~2009년)
대한핵의학회지 2005;39(4)215~223
안정한 방사금속 착물을 위한 거대고리 리간드 개발
(Development of Macrocyclic Ligands for Stable Radiometal Complexes)
Author 유정수·이재태1,
Jeong soo Yoo, Ph.D., Jae tae Lee, M.D., Ph.D.1
Affiliation 경북대학교 의과대학 분자의학과, 핵의학과1
Department of Molecular Medicine, Department of Nuclear Medicine1, Kyungpook National University School of Medicine, Korea
Abstract

Current interest in the regioselective N-functionalization of tetraazacycloalkanes (cyclen and cyclam) stems mainly from their complexes with radioactive metals for applications in diagnostic (64Cu, 111In, 67Ga) and therapeutic (90Y) medicine, and with paramagnetic ions for magnetic resonance imaging (Gd+3). Selective methods for the N-substitution of cyclen and cyclam is a crucial step in most syntheses of cyclen and cyclam-based radiometal complexes and bifunctional chelating agents. In addition, mixing different pendent groups to give hetero-substituted cyclen derivatives would be advantageous in many applications for fine-tuning the compound's physical properties. So far, numerous approaches for the regioselective N-substitution of tetraazacycloalkanes and more specifically cyclen and cyclam are reported. Unfortunately, none of them are general and every strategy has its own strong points and drawbacks. Herein, we categorize numerous regioselective N-alkylation methods into three strategies, such as 1) direct substitution of the macrocycle, 2) introduction of the functional groups prior to cyclization, and 3) protection/functionalization/deprotection. Our discussion is also split into the methods of mono- and tri-functionalization and di-functionalizataion based on number of substituents. At the end, we describe new trials for the new macrocycles which form more stable metal complexes with various radiometals, and briefly mention the commercially available tetraazacycloalkanes which are used for the biconjugation of biomolecules.(Korean J Nucl Med 39(4):215-223, 2005)

Keyword Regioselective N-Functionalization, Tetraazacycloalkanes, Cyclen, Cyclam
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