反应详情

[6-(Methyloxy)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]acetaldehyde (0.250 g, 1.14 mmol) was combined with 1,1-dimethylethyl 4-piperidinylcarbamate (0.229 g, 1.14 mmol) in a 1:1 MeOH/DCM solution. Excess Na2SO4 was added as a drying agent and the solution was stirred at ambient temperature overnight. NaBH(OAc)3 (0.724 g, 3.42 mmol) was added and the reaction was stirred an additional 2 h. The solution was concentrated onto silica gel under vacuum and the crude residue purified by column chromatography (silica gel) using a DCM/DCM-MeOH—NH4OH (90:10:1) gradient to yield the desired compound (0.271 g, 59%).

1. stirringthe reaction was stirred an additional 2 h
2. concentrationThe solution was concentrated onto silica gel under vacuum
3. customthe crude residue purified by column chromatography (silica gel)