Trimethylsilyl-directed 1,3-dipolar cycloaddition reactions in the solid-phase synthesis of 1,2,3-triazoles

被引:76
|
作者
Coats, SJ [1 ]
Link, JS [1 ]
Gauthier, D [1 ]
Hlasta, DJ [1 ]
机构
[1] Johnson & Johnson Pharmaceut Res & Dev LLC, Spring House, PA 19477 USA
关键词
D O I
10.1021/ol047637y
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
[GRAPHICS] A regioselective method for the preparation of 1,5-trisubstituted H-1-1,2,3-triazoles via a 1,3-dipolar cycloaddition of 1-trimethylsilylacetylenes with organciazides is described. Immobilization of the azide on REM resin and subsequent cycloaddition afforded a 2 x 2 x 4 x 3 membered 1,5-disubstituted H-1-1,2,3-triazole library with an average purified yield of 68%.
引用
收藏
页码:1469 / 1472
页数:4
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