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空间固定的色胺和5-甲氧基色胺衍生物对5-羟色胺受体亚型的选择性,I:N-烷基和N,N-二烷基-3-吲哚基双环[2.2.1]庚烷-2-胺的合成

Selectivity of sterically fixed tryptamine and 5-methoxytryptamine derivatives for serotonin receptor subtypes, I: Synthesis of N-alkyl- and N,N-dialkyl-3-indolylbicyclo[2.2.1]heptane-2-amines.

作者信息

Rehse K, Zimmermann H

机构信息

Institut für Pharmazie, Freien Universität Berlin, Germany.

出版信息

Arch Pharm (Weinheim). 1994 Feb;327(2):67-75. doi: 10.1002/ardp.19943270203.

DOI:10.1002/ardp.19943270203
PMID:8135645
Abstract

Twenty-six title compounds with the ethylamine part of tryptamine or 5-methoxytryptamine fixed in an anticlinal ecliptic conformation were synthesized for assaying them at the different known serotonin receptors. Several alkylation methods have been improved and adapted for the space consuming norbornane system. The structures were fully elucidated by high-field NMR spectroscopy. All 1H- and 13C-signals could be assigned by means of 1H-1H- and 13C-1H-correlation spectroscopy (COSY).

摘要

合成了26种标题化合物,其中色胺或5-甲氧基色胺的乙胺部分固定为反式偏位构象,用于在不同已知的5-羟色胺受体上进行测定。几种烷基化方法已得到改进并适用于空间消耗大的降冰片烷体系。通过高场核磁共振光谱对结构进行了全面阐释。所有的1H和13C信号都可以通过1H-1H和13C-1H相关光谱(COSY)进行归属。

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