Intramolecular azide-alkyne cycloaddition for the fast assembly of structurally diverse, tricyclic 1,2,3-triazoles
Intramolecular azide-alkyne cycloaddition for the fast assembly of structurally diverse, tricyclic 1,2,3-triazoles
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DOI：
10.1021/ol800291t
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发表时间：
2008-04-17
期刊：
影响因子：
5.2
通讯作者：
Pericas, Miquel A.
中科院分区：
文献类型：
--
作者：
Oliva, Ana I.;Christmann, Ute;Pericas, Miquel A.
描述了以环状环氧化物为原料，通过连续的叠氮分解、炔丙基化和 1,3-偶极环加成合成新型三环 1,2,3-三唑。还报道了通过 N-芳基化反应进行衍生化和对映体纯化合物的合成。其中一些化合物对 sigma-1 受体表现出显着的亲和力。
The synthesis of novel tricyclic 1,2,3-triazoles starting from cyclic epoxides via the sequential azidolysis, propargylation and 1,3-dipolar cycloaddition is described. Derivatization by N-arylation reaction and the synthesis of enantiomerically pure compounds is also reported. Some of these compounds exhibit significant affinity for the sigma-1 receptor.