反应详情

In a similar manner as described for Intermediate 48, using 6-(1-aminoethyl)-N-[4-(methyloxy)phenyl]-1,2,4-triazin-3-amine (Intermediate 47) (100 mg, 0.41 mmol), and cyclohexylacetic acid (64 mg, 0.45 mmol), except that the reaction was stirred for 4 h and the crude reaction mixture reduced under vacuum, partitioned between dichloromethane and saturated sodium bicarbonate solution and the layers separated. The aqueous was re-extracted with dichloromethane and the combined organic layers washed with brine, dried with magnesium sulfate, filtered and reduced to give 2-cyclohexyl-N-[1-(3-{[4-(methyloxy)phenyl]amino}-1,2,4-triazin-6-yl)ethyl]acetamide (100 mg) as a yellow solid. MS m/z 370 (M+1).

1. customthe crude reaction mixture
2. custompartitioned between dichloromethane and saturated sodium bicarbonate solution
3. customthe layers separated
4. extractionThe aqueous was re-extracted with dichloromethane
5. washthe combined organic layers washed with brine
6. dry with materialdried with magnesium sulfate
7. filtrationfiltered