- 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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- N-(2-guanidino-ethylimino)-morpholine antigen based on thiotriazinone structure restrictiveness, antibody and application
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The present invention discloses a N-(2-guanidino-ethylimino)-morpholine hapten based on thiotriazinone structure restrictiveness, an artificial antigen, an antibody and an application. The structure of the N-(2-guanidino-ethylimino)-morpholine hapten is represented by a formula I shown in the description, wherein R is -H and -CH3. The N-(2-guanidino-ethylimino)-morpholine artificial antigen and antibody are prepared base on the hapten, and the artificial antigen and antibody have high detection efficiency and simple operation to N-(2-guanidino-ethylimino)-morpholine, and can be used in enzyme-linked immunosorbent assay rapid detection of the N-(2-guanidino-ethylimino)-morpholine; and the antigen and the antibody have a simple synthetic process, lower costs, and good application prospects.
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Paragraph 0049; 0054; 0055
(2018/06/04)
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- Regioselective synthesis of imidazo[1,2-a][1,3,5]triazines and 3,4-dihydroimidazo[1,2-a][1,3,5]triazines from [1,3,5]triazin-2,4-diamines
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An efficient and practical procedure was developed to prepare novel imidazo[1,2-a][1,3,5]triazines and 3,4-dihydroimidazo[1,2-a][1,3,5]triazines with a good regioselectivity and high yields, starting from dicyandiamide and the corresponding arylamines. Mechanistic studies for the subsequent cyclocondensation with chloroacetaldehyde support a pathway, which begins with the displacement of the chloro atom activated by an adjacent CO group, followed by cyclization and dehydration.
- Dao, Pascal,Garbay, Christiane,Chen, Huixiong
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p. 3867 - 3871
(2013/07/05)
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