Sodium hydride → 5-[5-Bromo-4-(2-hydroxy-1-methyl-propoxy)-pyrimidin-2-ylamino]-pyridine-2-sulfonic acid amide

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Reaction Steps

270 mg (1.5 mmol) of (2R, 3R)-(−)-2,3-butanediol is dissolved in 3 ml of pyridine and mixed with 30 mg (0.69 mmol) of sodium hydride. It is allowed to stir for 15 minutes at room temperature and then 110 mg (0.3 mmol) of 5-(5-bromo-4-chloro-pyrimidin-2-ylamino)-pyridine-2-sulfonic acid amide is added. After 1 hour at room temperature, it is stirred for 4 more hours at 50° C. Concentration by evaporation and flashing with dichloromethane/MeOH 4:1 yields 42 mg of 5-[5-bromo-4-(2-hydroxy-1-methyl-propoxy)-pyrimidin-2-ylamino]-pyridine-2-sulfonic acid amide: (34% of theory)°

Provenance & Evidence