Method for synthesizing biaryl ketone compounds through carbonylation by taking chloroform as carbonyl source without transition metal participation
A technology of diaryl ketones and compounds, which is applied in the field of catalytic synthesis, can solve the problems of carbonyl sources such as toxicity, safety hazards, and difficult handling, and achieve the effects of easy handling, avoiding flammability, and stable treatment
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Embodiment 1
[0031] Compound 1: Add 4-fluorophenylboronic acid (0.75mmol), sodium carbonate (1.0mmol), cesium hydroxide monohydrate (2.5mmol), sodium iodide (0.25mmol), pivalic acid (0.75mmol) ), 4-iodophenylacetylene (0.5mmol), chloroform (1.5mmol) and ethylene glycol (2.0g), and reacted at 120°C for 24h. Cool to room temperature, extract, evaporate the solvent under reduced pressure, and separate by column chromatography to obtain a yield of 86%.
Embodiment 2
[0033] Compound 1: Add 4-fluorophenylboronic acid (0.75mmol), sodium carbonate (1.0mmol), cesium hydroxide monohydrate (2.5mmol), sodium iodide (0.25mmol), pivalic acid (0.75mmol) ), 4-iodophenylacetylene (0.5mmol), chloroform (1.5mmol) and ethylene glycol (2.0g), and reacted at 50°C for 72h. Cool to room temperature, extract, evaporate the solvent under reduced pressure, and separate by column chromatography to obtain a yield of 25%.
Embodiment 3
[0035] Compound 1: Add 4-fluorophenylboronic acid (0.75mmol), sodium carbonate (1.0mmol), cesium hydroxide monohydrate (2.5mmol), sodium iodide (0.25mmol), pivalic acid (0.75mmol) ), 4-iodophenylacetylene (0.5mmol), chloroform (1.5mmol) and ethylene glycol (2.0g), and reacted at 200°C for 0.5h. Cool to room temperature, extract, evaporate the solvent under reduced pressure, and separate by column chromatography to obtain a yield of 90%.
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