Carbohydrate Conjugates for Molecular Imaging and Radiotherapy: 99mTc(I) and 186Re(I) Tricarbonyl Complexes of N-(2'-Hydroxybenzyl)-2-amino-2-deoxy-D
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- 作者：Simon R. Bayly ; Cara L. Fisher ; Tim Storr ; Michael J. Adam ; and Chris Orvig
- 刊名：Bioconjugate Chemistry
- 出版年：2004
- 出版时间：July 2004
- 年：2004
- 卷：15
- 期：4
- 页码：923 - 926
- 全文大小：58K
- 年卷期：v.15,no.4(July 2004)
- ISSN：1520-4812
文摘
An approach to a new class of potential radiopharmaceuticals is demonstrated by the labeling of aglucosamine derivative with the tricarbonyls of 99mTc and 186Re. The proligand HL2 (N-(2'-hydroxybenzyl)-2-amino-2-deoxy-d-glucose) was produced by hydrogenation of the corresponding Schiff baseand reacted with [NEt4]2[Re(CO)3Br3] to form the neutral complex [(L2)Re(CO)3] in 40% yield. 1H and13C NMR spectra indicate that the {Re(CO)3} core is bound in a tridentate fashion via the amino N,phenolato O, and C-3 hydroxyl O atoms of the ligand. At the tracer-level, labeling of HL2 with[99mTc(CO)3(H2O)3]+ and [186Re(CO)3(H2O)3]+ was achieved in aqueous conditions in 95 ± 2% and 94± 3% average radiochemical yields, respectively.