反应详情

530 mg (1.9 mmol) of (R)-2-(5-bromo-2-chloro-pyrimidin-4-ylamino)-butan-1-ol is added to a suspension of 303 mg of a mixture that consists of 4-amino-thiophene-2-sulfonic acid amide and 5-amino-thiophene-2-sulfonic acid amide (ratio: 2:1) in 7 ml of ethanol and 170 μl of concentrated HCl. The reaction mixture is stirred for 21 hours under reflux. After cooling, the batch is purified by chromatography (Flashmaster II, hexane/EE 2:8). The crude product that is obtained is then recrystallized (ethyl acetate/diisopropyl ether). 47 mg (0.11 mmol, 7% of theory) of the product 4-[5-bromo-4-(1-hydroxymethyl-propylamino)-pyrimidin-2-ylamino]-thiophene-2-sulfonic acid amide is obtained.

1. temperatureunder reflux
2. temperatureAfter cooling
3. customthe batch is purified by chromatography (Flashmaster II, hexane/EE 2:8)
4. customThe crude product that is obtained
5. customis then recrystallized (ethyl acetate/diisopropyl ether)