Yi He, Xiaolong Li, Jue Li
Jul 16, 2014
Citations
0
Influential Citations
2
Citations
Journal
Tetrahedron Letters
Abstract
Abstract In this study, a novel and convenient route for the construction of 5-((1 H -1,2,4-triazol-1-yl)methyl)-1 H -indoles ( 8 ) is presented starting from (1 H -1,2,4-triazol-1-yl)methanol ( 5 ) and indolines ( 6 ) under 98% H 2 SO 4 at room temperature for 4–24 h, followed by deacetylation and dehydrogenation. Based on this finding, a novel route to synthesize Rizatriptan starting from tryptamine was designed and accomplished with 48.5% overall yield in 6 steps. Compared with operational art, the new route afforded higher yield and more pure products requiring no chromatographic purification, which may further be applied in industrialization.