反应详情

2.03 g (10 mmol) 5-bromonicotinic acid, 1 g (1 eq.) 2-fluoroethylamine, 2.31 g (1.2 eq.) EDC.HCl, 123 mg (0.1 eq.) DMAP and 5.6 mL (4 eq.) triethylamine are stirred in 60 mL dichloromethane for 20 hours at room temperature. The reaction mixture is extracted with dichloromethane and water, the combined organic phases are washed with brine, dried with sodium sulfate and evaporated. The residue is triturated in diethylether and hexane to yield after filtration the desired product as a white powder. MS(ES+): 347 and 349 (M+1).

1. extractionThe reaction mixture is extracted with dichloromethane and water
2. washthe combined organic phases are washed with brine
3. dry with materialdried with sodium sulfate
4. customevaporated
5. customThe residue is triturated in diethylether
6. customhexane to yield
7. filtrationafter filtration the desired product as a white powder