Title of article :
A novel and convenient route for the construction of 5-((1H-1,2,4-triazol-1-yl)methyl)-1H-indoles and its application in the synthesis of Rizatriptan
Author/Authors :
He، نويسنده , , Yi and Li، نويسنده , , Xiaolong and Li، نويسنده , , Yu-Jue and Li، نويسنده , , Xiaocen and Guo، نويسنده , , Li and Hai، نويسنده , , Li and Wu، نويسنده , , Yong، نويسنده ,
Issue Information :
هفته نامه با شماره پیاپی سال 2014
Pages :
4
From page :
3938
To page :
3941
Abstract :
In this study, a novel and convenient route for the construction of 5-((1H-1,2,4-triazol-1-yl)methyl)-1H-indoles (8) is presented starting from (1H-1,2,4-triazol-1-yl)methanol (5) and indolines (6) under 98% H2SO4 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.
Keywords :
4-Triazol-1-yl)methyl)-1H-indoles , Rizatriptan , (1H-1 , 2 , 4-Triazol-1-yl)methanol , Tryptamine , 5-((1H-1 , 2
Journal title :
Tetrahedron Letters
Serial Year :
2014
Journal title :
Tetrahedron Letters
Record number :
1890039
Link To Document :
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