Trimethylsilyl-directed 1,3-dipolar cycloaddition reactions in the solid-phase synthesis of 1,2,3-triazoles |
| |
Authors: | Coats Steven J Link Jeffrey S Gauthier Diane Hlasta Dennis J |
| |
Affiliation: | Johnson & Johnson Pharmaceutical Research & Development, L.L.C., Welsh and McKean Roads, Spring House, Pennsylvania 19477-0776, USA. |
| |
Abstract: | [reaction: see text] A regioselective method for the preparation of 1,5-trisubstituted 1H-1,2,3-triazoles via a 1,3-dipolar cycloaddition of 1-trimethylsilylacetylenes with organoazides 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 1H-1,2,3-triazole library with an average purified yield of 68%. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|