Gem-difluoromethylene-containing azo compound and preparation method thereof
A technology of difluoromethylene azo and sodium difluoromethane sulfinate, applied in directions such as organic chemistry, can solve the problems such as the synthetic method of geminal difluoromethylene has not yet been reported, and achieves good tolerance, The effect of mild reaction conditions and easy operation
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Embodiment 1
[0277] Example 1: Under nitrogen protection, copper sulfate (0.05mmol), TsOH (0.35mmol), tetrafluoroborate-4-methoxyphenyldiazonium salt (0.6mmol) were added successively in a 10ml reaction tube equipped with magnetons ), 1,3-benzoxazole-2-difluoromethanesulfinate sodium (2.0mmol), DCM 2.5ml, TBHP (4.0mmol) was added dropwise at 50°C with stirring. The reaction was stopped after 10 h, and the solid in the reaction solution was filtered through a short column of silica gel and concentrated. The crude product was separated and purified by column chromatography to obtain the target product 3p with a yield of 88%.
Embodiment 2
[0278] Example 2: Under nitrogen protection, add cuprous iodide (0.07mmol), trifluoroacetic acid (0.25mmol), and tetrafluoroborate-4-ethanonephenyldiazonium salt in sequence in a 10ml reaction tube equipped with magnetons (0.5mmol), sodium 1,3-benzoxazole-2-difluoromethanesulfinate (2.0mmol), Dioxane 4ml, TBHP (3.5mmol) was added dropwise at 20°C with stirring. The reaction was stopped after 8 h, and the solid in the reaction solution was filtered through a short column of silica gel and concentrated. The crude product was separated and purified by column chromatography to obtain the target product 3b with a yield of 86%.
Embodiment 3
[0279] Embodiment three: under nitrogen protection, silver acetate (0.5mmol), hydrochloric acid (2.5mmol), tetrafluoroboric acid-4-benzophenone phenyl diazonium salt (1.0mmol) were added successively in a 20ml reaction tube equipped with magnetons ), 1,3-benzoxazole-2-sodium difluoromethanesulfinate (3.5mmol), dimethylformamide 6.0ml, reaction stirring at room temperature and adding TBHP (6mmol) dropwise. The reaction was stopped after 10 h, and the solid in the reaction solution was filtered through a short column of silica gel and concentrated. The crude product was separated and purified by column chromatography to obtain the target product 3c with a yield of 23%.
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