- 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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- Imidazole-triazine type compound and preparation method and application thereof
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The invention provides an imidazole-triazine type compound which is shown as the formula 3 in the description and a preparation method and application thereof. The method comprises the steps that a triazine compound and an alpha,beta-unsaturated ketone type compound are mixed and added into a solvent, under the existence of a metal copper catalyst and an oxidizing material, the mixed solution is stirred and reacts 5-20 hours under the temperature of 60-150 DEG C, after the reaction is finished, the reacted solution is subjected to post processing, and the imidazole-triazine type compound which is shown as the formula 3 is obtained; the metal copper catalyst is halogenide of the copper or a copper salt; the oxidizing material is a halogen elementary substance. The imidazole-triazine type compound can be applied to prepare antibacterial drugs or antibacterial agents, and the preferred antibacterial drugs are the drugs which inhibit activity of escherichia coli.
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Paragraph 0028; 0029; 0030
(2017/10/06)
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- 2,4-diamine-1,3,5-triazine compound, preparation method and application thereof
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The invention provides a 2,4-diamine-1,3,5-triazine compound represented as the formula (III). A preparation method includes the following steps: adding compounds represented as the formulas (I) and (II), a metal copper catalyst, a ligand, an alkaline sub
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Paragraph 0030; 0031; 0032; 0033; 0034
(2016/12/07)
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- Diuretics on the basis of N substituted 2,4 diamino s triazines by cyclisation of biguanides
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The structural class of 2,4 diamino s triazines (5) functioning as diuretics has become accessible by a novel preparatory procedure. The new synthesis is based on the aminomethinylating principle of s triazine (1), under the action of which biguanides (2) are cyclized to 5 passing through the intermediary states 3 and 4.
- Kreutzberger
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p. 1860 - 1862
(2007/10/04)
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