| 84% |
|
Dissolving 1-chloro-4-iodo-2-trifluoromethylbenzene (10 mmol) obtained in Reaction 1.220 ml of toluene,Isoxazole-4-amine is added sequentially to the system(12mmol),Palladium acetate (0.5 mmol),2,2'-bis(diphenylphosphino)-1,1'-binaphthyl(12 mmol), 3 ml of triethylamine, after stirring for 10 minutes, add 10 ml of cesium carbonate (10 mmol)The aqueous solution is heated to 50 ° C for 4 hours. After the reaction is completed, 20 ml of water is added to the system.Stir for 20 minutes, dispense,The organic phase is dried over anhydrous sodium sulfate. Concentrated, flash column chromatography,2.2 g of yellow N-(4-chloro-3-trifluoromethylphenyl)-<strong>[108511-97-3]isoxazole-4-amine</strong> powder was obtained with a yield of 84percent. |
| 84% |
|
The 1-chloro-4-iodo-2-trifluoromethylbenzene (10 mmol) obtained in the reaction 1.2 was dissolved in 20 ml of toluene, and the system was sequentially added with <strong>[108511-97-3]<strong>[108511-97-3]isoxazol-4-amin</strong>e</strong> (12 mmol), palladium acetate ( 0.5 mmol), 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl (12 mmol), 3 ml of triethylamine. After stirring for 10 minutes, add 10 ml of cesium carbonate (10 mmol). The aqueous solution is heated to 50 ° C for 4 hours. After the reaction is completed, 20 ml of water is added to the system, stirred for 20 minutes, and the organic phase is dried over anhydrous sodium sulfate, concentrated, and then purified by flash column chromatography.2.2 g of yellow N-(4-chloro-3-trifluoromethylphenyl)-<strong>[108511-97-3]isoxazole-4-amine</strong> powder was obtained in a yield of 84percent. |
| 84% |
With palladium diacetate; caesium carbonate; 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl; triethylamine; In toluene; at 50℃; for 4h; |
1-Chloro-4-iodo-2-trifluoromethylbenzene (10 mmol) obtained in Reaction 1.2 was dissolved in 20 ml of toluene.Isoxazole-4-amine (12 mmol) was added sequentially to the system.Palladium acetate (0.5 mmol),2,2'-bis(diphenylphosphino)-1,1'-binaphthyl (12 mmol),3 ml of triethylamine,After stirring for 10 minutes,Add 10 ml of aqueous solution of cesium carbonate (10 mmol),Heat to 50 ° C for 4 hours.After the reaction was completed, 20 ml of water was added to the system, and the mixture was stirred for 20 minutes, and the organic phase was dried over anhydrous sodium sulfate, concentrated, and purified by flash column chromatography.2.2 g of yellow N-(4-chloro-3-trifluoromethylphenyl)-<strong>[108511-97-3]isoxazole-4-amine</strong> powder was obtained in a yield of 84percent. |
| 84% |
|
The 1-chloro-4-iodo-2-trifluoromethylbenzene (10 mmol) obtained in the reaction 1.2 was dissolved in 20 ml of toluene, and the system was sequentially added with <strong>[108511-97-3]<strong>[108511-97-3]isoxazol-4-amin</strong>e</strong> (12 mmol), palladium acetate ( 0.5 mmol), 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl (12 mmol), 3 ml of triethylamine. After stirring for 10 minutes, add 10 ml of cesium carbonate (10 mmol). The aqueous solution was heated to 50 ° C for 4 hours. After the reaction was completed, 20 ml of water was added to the system, stirred for 20 minutes, and the organic phase was dried over anhydrous sodium sulfate.Concentration and flash column chromatography gave 2.2 g of yellow N-(4-chloro-3-trifluoromethylphenyl)-<strong>[108511-97-3]isoxazole-4-amine</strong> powder, yield 84percent. |
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