A convenient synthesis of novel bifunctional prochelators for coupling to bioactive peptides for radiometal labelling

被引：107

作者：

Eisenwiener, KP ^{[1
]}

Powell, P ^{[1
]}

Mäcke, HR ^{[1
]}

机构：

[1] Univ Basel Hosp, Dept Radiol, Inst Nucl Med, Div Radiol Chem, CH-4031 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(00)00413-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New DOTA-based bifunctional prochelators, e.g., 1-(1-carboxy-3-carbotertbutoxypropyl)-4,7,10-(carbotertbutoxymethyl)-1,4,7, 10-tetraazacyclodode-cane (DOTAGA(tBu)(4)), (6d) for a broad application in the modification of biomolecules with metal ions were prepared. The five-step synthesis of 6d has an overall yield of about 20%. The coupling of 6d to a bioactive peptide on solid-phase was exemplified with use of a CCK-B (cholecystokinin) analogue. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2133 / 2135

页数：3

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