- Synthetic method of alpha-position dibromination of alpha-heterocyclic carbonyl compound
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The invention discloses a synthetic method of alpha-position dibromination of an alpha-heterocyclic carbonyl compound, and belongs to the technical field of organic synthesis, and the method comprisesthe following steps: by taking the alpha-heterocyclic carbonyl compound as a raw material, adding a bromination reagent, a solvent and a small molecular catalyst, and reacting under light irradiationto obtain a corresponding product. The method has the advantages of high yield, simplicity and convenience in operation, mild reaction conditions, wide substrate adaptability and the like.
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Paragraph 0027-0028; 0033-0035; 0096-0098
(2020/05/30)
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- Synthesis and cyclization reaction of pyrazolin-5-one derivatives
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A versatile synthetic method for preparing 3-pyrazolin-5-ones and 5,8-dihydro-1H-pyrazolo[1,2-a]pyridazines from simple β-keto esters is demonstrated. The synthetic strategies involve the acylation of β-keto esters, cyclocondensation with hydrazine followed by trapping with a diene under oxidative conditions.
- Jung, Jae-Chul,Blake Watkins,Avery, Mitchell A.
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- Synthesis and antiamoebic activity of 3,7-dimethyl-pyrazolo[3,4-e][1,2,4] triazin-4-yl thiosemicarbazide derivatives
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A series of 3,7-dimethyl-pyrazolo[3,4-e][1,2,4]triazin-4-yl thiosemicarbazide derivatives 3-22 were prepared and evaluated in vitro against HM1:1MSS strain of Entamoeba histolytica, to identify the compounds for antiamoebic activity. They exhibited antiamoebic activity in the range (IC 50 = 0.81-7.31 μM). The results were compared to the activity of known drug metronidazole. It is inferred from the in vitro studies that the compounds 10, 11, 17 and 18 were found to be significantly better inhibitors of E. histolytica since IC50 values in the μM range elicited by these compounds are much lower than metronidazole. Besides, compounds 11 and 17 have shown the most promising antiamoebic activity (IC50 = 0.81 μM of 11, IC50 = 0.84 μM of 17 versus IC50 = 1.81 μM of metronidazole). The study suggests the possibility of developing triazine analogues as potential drug candidates for antiamoebic activity.
- Singh, Shailendra,Husain, Kakul,Athar, Fareeda,Azam, Amir
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p. 255 - 262
(2007/10/03)
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- Synthesis and antifungal activity of 4-substituted-3,7-dimethylpyrazolo[3,4-e][1,2,4]triazine
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A convenient synthesis and antifungal activity of four compounds namely 2-(3,7-dimethyl-4H-pyrazolo[3,4-e][1,2,4]triazin-4-yl)acetic acid 2, 3,7-dimethyl-4-(4-methylphenyl-pyrazolo[3,4-e][1,2,4]triazine 3, 4-(3,7-dimethyl-4H-pyrazolo[3,4-e][1,2,4]tri-azin-4-yl)aniline 4 4-(3,7-dimethyl-4H-pyrazolo[3,4-e][1,2,4]triazin-4-yl)benzoic acid 5 have been reported.
- Tewari, Ashish Kumar,Mishra, Lily,Verma,Mishra, Anil
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p. 664 - 667
(2007/10/03)
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