Trifluoromethylthiolation reagent and application thereof
A technology of trifluoromethylthio and sodium trifluoromethylsulfinate, applied in the direction of organic chemistry, etc., can solve the problems of high toxicity, difficulty in preparation and expensive raw materials of trifluoromethylthio flower reagent, and achieve high yield , Substrate adaptability, cheap effect
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Embodiment 1
[0021] In a reactor containing solvent toluene, add sodium trifluoromethylsulfinate (62.4g), indole (23.4g), dimethyl phosphite (55mL), iodine element (about 10g) and copper acetate (50g ), stirred at 110° C. for more than 12 hours under nitrogen protection conditions. After the reaction, the product 3-trifluoromethylthioindole was obtained after filtration, distillation and column chromatography separation. , the yield was 89%.
Embodiment 2
[0023] In a reactor containing solvent toluene, add sodium trifluoromethanesulfinate (62.4g), indole (23.4g), diethyl phosphite (60mL), iodine element (about 10g) and copper acetate (50g ), stirred at 110° C. for more than 12 hours under nitrogen protection conditions. After the reaction, the product 3-trifluoromethylthioindole was obtained after filtration, distillation and column chromatography separation. , and the yield was 87%.
Embodiment 3
[0025] In the reactor containing solvent toluene, add sodium trifluoromethyl sulfinate (62.4g), N-methylindole (26.2g), diethyl phosphite (60mL), iodine simple substance (about 10g) and Copper acetate (50 g), stirred at 110° C. under nitrogen protection for more than 12 hours. After the reaction, the product N-methyl-3-trifluoromethylthioindole was obtained after filtration, distillation and column chromatography separation. , and the yield was 84%.
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