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With copper(I) oxide; oxygen; In 1-methyl-pyrrolidin-2-one; at 80℃; for 4h;Sealed tube; Green chemistry;
0.3 mmol of <strong>[456-14-4]4-fluorobenzamidine hydrochloride</strong> (No. 3 corresponding compound, 0.0579 g) was weighed out, 0.4 mmol of 2-phenyl-1-hydrogenindole (corresponding to (30) the corresponding compound, 0.0770 g) And 0.06 mmol cuprous oxide (0.0086 g) in 20 mL of the test tube reaction tube, Plus 3mL N-methyl pyrrolidone as solvent, tube mouth closed with oxygen balloon, Stirring at 80 ° C for 4 hours; after completion of the reaction, The reaction solution was extracted with ethyl acetate, dried over anhydrous sodium sulfate and separated by column chromatography (column chromatography separation conditions: the stationary phase was 300-400 mesh silica powder, the mobile phase was ethyl acetate (A) and petroleum ether (3) The mobile phase change procedure (A: B) was 1: 6) to give 0.0787 g of the reaction product. According to the characterization data, the reaction product was 2-phenyl-4- (4-fluorophenyl) -benzo [1,3,5] triazolidin-5-hydrogen-6-one (purity> 95percent); the product yield was calculated and the result was 78percent.
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