Journal
TETRAHEDRON LETTERS
Volume 61, Issue 19, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2020.151844
Keywords
Annulation reaction; DMF; 1,2,4-triazolo[3,4-a]pyridine; Triazine
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Funding
- Priority Academic Program Development of Jiangsu Higher Education Institutions (PAPD)
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1,2,4-Triazolo[3,4-a]pyridines and related heterocycles and substituted triazines were commonly discovered scaffolds in a variety of pharmaceutical and agrochemical agents. Herein, we report a highly efficient and practical method using DMF and its derivative for the [4+1] and [5+1] annulation reactions to prepare these heterocycles. This metal free reaction takes advantages of shelf stable DMF as solvent and carbon donor, imidazole chloride as a catalyst, the mild reaction condition tolerates a broad substrate range and substitutes. The prepared 3-unsubstituted 1,2,4-triazolo[3,4-a]pyridine and derivatives allow further introduction of a variety of functional group1 at 3-position. (C) 2020 Elsevier Ltd. All rights reserved.
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