Synthesis of conformationally constrained spirodihydrofuropyridine analogues of epibatidine

被引：14

作者：

Abe, H ^{[1
]}

Arai, Y ^{[1
]}

Aoyagi, S ^{[1
]}

Kibayashi, C ^{[1
]}

机构：

[1] Tokyo Univ Pharm & Life Sci, Sch Pharm, Tokyo 1920392, Japan

来源：

TETRAHEDRON LETTERS | 2003年 / 44卷 / 14期

关键词：

D O I：

10.1016/S0040-4039(03)00395-2

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Conformationally constrained spirofuropyridine analogues of epibatidine, syn-2 and anti-2, in which the 7-azabicyclo[2.2.1]heptane system and the 2-chloropyridine ring are held rigidly with the shorter and longer N-N distances, respectively, were synthesized from N-Boc-7-azabicyclo[2.2.1]heptan-2-one. The preliminary binding studies suggested that syn-2 has stronger binding affinity for nAChRs than anti-2. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：2971 / 2973

页数：3

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