Synthesis of epibatidine isomers:: endo-5-and 6-(6′-chloro-3′-pyridyl-2-azabicyclo[2.2.1]heptanes

被引:31
作者
Cox, CD
Malpass, JR [1 ]
Gordon, J
Rosen, A
机构
[1] Univ Leicester, Dept Chem, Leicester LE1 7RH, Leics, England
[2] AstraZeneca R&D Boston, Worcester, MA 01605 USA
来源
JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1 | 2001年 / Royal Society of Chemistry卷 / 19期
关键词
D O I
10.1039/b106212n
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Synthesis of the title;compounds is described; detailed NMR data are provided in support of the proposed stereostructures. The 5- and 6-endo-compounds show high selectivity for alpha4 beta2 versus alpha7 nAChR subtypes; in contrast, the exo-stereoisomers show comparatively weak affinity at both subtypes.
引用
收藏
页码:2372 / 2379
页数:8
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