Synthesis of a novel 14-membered highly constrained cyclic peptidic scaffold

被引:4
作者
Arnusch, CJ [1 ]
Pieters, RJ [1 ]
机构
[1] Univ Utrecht, Inst Pharmaceut Sci, Dept Med Chem, NL-3508 TB Utrecht, Netherlands
关键词
S(N)AR reaction; cyclic peptide; Bi-aryl ether;
D O I
10.1016/j.tetlet.2004.03.131
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The synthesis and NMR analysis of a novel highly constrained scaffold is described. The 14-membered macrocyclic ring structure was inspired by many medicinally relevant natural products that also contain the bi-aryl ether moiety. The synthesis required only commercially available starting materials and involved a base mediated SNAr cyclization. A conformational search,,vas performed, which indicated a strong preference for a single conformation, which was consistent with observed ROE signals by NMR. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4153 / 4156
页数:4
相关论文
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