Tedizolid impurity and preparing method thereof
A technology of tedizolid and impurities, which is applied in the field of drug synthesis, can solve the problems of uncontrolled impurities, no public reports of impurities, etc., and achieve the effect of quality assurance, fewer steps, and simple operation methods
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[0029] Example 1
[0030] Under nitrogen protection, add 5-bromo-2-(2-methyl-2H-tetrazol-5-yl)pyridine (10g, 41.6mmol), (6-(2-methyl-2H-tetrazole) to the reaction flask -5-yl)pyridin-3-yl)boronic acid (8.5g, 41.6mmol), [1,1'-bis(diphenylphosphine)ferrocene]palladium dichloride (304mg, 0.416mmol), potassium carbonate (11.5g, 83.2mmol) and 20mL of a mixture of tetrahydrofuran and water (1:1, V / V), heated to 30°C, stirred and reacted for 4 hours, TLC detected the completion of the reaction, added 20ml of water, filtered to obtain tertizolamide impurity I 12.6g.
Example Embodiment
[0031] Example 2
[0032] Under nitrogen protection, add 5-bromo-2-(2-methyl-2H-tetrazol-5-yl)pyridine (21g, 62.4mmol), (6-(2-methyl-2H-tetrazole) into the reaction flask -5-yl)pyridin-3-yl)pinacol borate (11.9g, 41.6mmol), bis(triphenylphosphine) palladium dichloride (292mg, 0.416mmol), sodium tert-butoxide (6.2g, 83.2 mmol) and 30 mL of toluene, the temperature was raised to 110° C., the reaction was stirred for 5 hours, TLC detected that the reaction was completed, and 11.9 g of Tedizolamide impurity I was obtained by filtration.
Example Embodiment
[0033] Example 3
[0034] Under nitrogen protection, add 5-iodo-2-(2-methyl-2H-tetrazol-5-yl)pyridine (11.9g, 41.6mmol), (6-(2-methyl-2H-tetra Azol-5-yl)pyridin-3-yl)boronic acid (4.25g, 20.8mmol), [1,1'-bis(diphenylphosphine)ferrocene]palladium dichloride (304mg, 0.416mmol), tert Sodium butoxide (8.0 g, 83.2 mmol) and 20 mL of dioxane were heated to 80° C., the reaction was stirred for 2 hours, TLC detected that the reaction was completed, and 12 g of tertizolamide impurity I was obtained by filtration.
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