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 |
Full text Article |
39040215.pdf
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