反应详情

tert-butyl 3-(aminomethyl)-3-fluoropiperidine-1-carboxylate (3.86 g, 16.6 mmol) and DIPEA (3.22 g, 24.9 mmol) were added to a solution of 5,7-dichloropyrido[3,4-b]pyrazine (3.32 g, 16.6 mmol) in THF (60 mL) and the mixture was refluxed overnight. The volatile components were evaporated and the residue was extracted with ethyl acetate. Ethyl acetate was washed with brine and dried. The solvent was removed in vacuo The crude residue was purified by silica-gel chromatography eluting with Hexane-50% EtOAc/Hexane (gradient) then C18 column to afford the subtitled compound as pale yellow solid 1.76 g. MS (m/z): 396 (M+H)+

1. temperaturethe mixture was refluxed overnight
2. customThe volatile components were evaporated
3. extractionthe residue was extracted with ethyl acetate
4. washEthyl acetate was washed with brine
5. customdried
6. customThe solvent was removed in vacuo The crude residue
7. customwas purified by silica-gel chromatography
8. washeluting with Hexane-50% EtOAc/Hexane (gradient)