Solid-phase approach to the synthesis of cyclen scaffolds from cyclotetrapeptides

被引：12

作者：

Alcaro, MC

Orfei, M

Chelli, M

Ginanneschi, M

Papini, AM

机构：

[1] Dipartimento Chim Organ Ugo Schiff, I-50019 Sesto Fiorentino, FI, Italy

[2] CNR, ICCOM, I-50019 Sesto Fiorentino, FI, Italy

来源：

TETRAHEDRON LETTERS | 2003年 / 44卷 / 28期

关键词：

macrocycles; cyclen; solid-phase synthesis; cyclization; cyclotetrapeptide;

D O I：

10.1016/S0040-4039(03)01213-9

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Cyclen derivatives, as coordinating ligands, have recovered considerable interest for the development of diagnostic and therapeutic drugs, mimicking the binding site of metalloproteins. We demonstrate that the on-resin reduction of head-to-tail cyclotetrapeptides, anchored to a solid support by the side-chain of a trifunctional amino acid, is an efficient synthetic strategy. The proposed approach leads to the cyclen scaffold still bound to the resin, ready for further decorations. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：5217 / 5219

页数：3

共 21 条

[1] A novel approach for the solid-phase synthesis of substituted cyclic guanidines, their respective bis analogues, and N-acylated guanidines from N-acylated amino acid amides [J].