- Metal free [4+1] and [5+1] annulation reactions to prepare heterocycles using DMF and its derivatives as one-carbon source
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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.
- Liu, Lingfeng,Qiao, Chunhua,Shen, Bei,Xu, Yiwen
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supporting information
(2020/04/01)
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- ASK1 inhibitor and application thereof
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The invention relates to compounds represented by a general formula (I) shown in the specification, a pharmaceutically acceptable salt and ester, or a stereoisomer of the compounds. The invention alsorelates to a preparation method of the compounds, a pharmaceutical preparation and a pharmaceutical composition containing the compounds. The compounds provided by the invention can effectively inhibit the amino acid phosphorylation of ASK1 and inhibit the activation of the ASK1; therefore, the compounds can treat and/or prevent ASK1-mediated diseases and related diseases.
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Paragraph 0169; 0174-0176
(2020/02/10)
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