تفاعل #67039

معادلة التفاعل

ethyl 4-isopropyl-2-(methylsulfonyl)pyrimidine-5-carboxylate

1,4-dioxane

exo-2-aminonorbornane

→

ethyl rac-2-[(1R,2R,4S)-bicyclo[2.2.1]hept-2-ylamino]-4-isopropylpyrimidine-5-carboxylate

المردود 84.4%

المذيبات

water

ظروف التفاعل

المعالجة

1. 1
   استخلاصthe aqueous layer was extracted with ethyl acetate
2. 2
   غسيلThe organic layer was washed with water and saturated brine
3. 3
   تجفيفdried over anhydrous magnesium sulfate
4. 4
   أخرىthe solvent was evaporated under reduced pressure
5. 5
   أخرىThe residue was purified by silica gel column chromatography (eluent: hexane-ethyl acetate)

الإجراء التجريبي

To a mixture of ethyl 4-isopropyl-2-(methylsulfonyl)pyrimidine-5-carboxylate (500 mg) and 1,4-dioxane (10 mL) was added exo-2-aminonorbornane (612 mg) at room temperature, and the mixture was stirred at the same temperature for 2 hours. To the reaction mixture was added water, and the aqueous layer was extracted with ethyl acetate. The organic layer was washed with water and saturated brine, and dried over anhydrous magnesium sulfate, and then the solvent was evaporated under reduced pressure. The residue was purified by silica gel column chromatography (eluent: hexane-ethyl acetate) to obtain ethyl rac-2-[(1R,2R,4S)-bicyclo[2.2.1]hept-2-ylamino]-4-isopropylpyrimidine-5-carboxylate (470 mg) as a white solid.

المصدر