反应详情

Ethyl 2-[6-(aminomethyl)-3-azabicyclo[3.1.0]hex-3-yl]pyrimidine-5-carboxylate (200 mg, 0.76 mmol) was stirred with 2-naphthaldehyde (119 mg, 0.76 mmol) in MeOH (10 ml) at r.t. under N2 for 16 h. NaBH4 (46 mg, 1.22 mmol) was then added and the mixture stirred for 10 min. Sat. aq. NH4Cl (20 ml) was added and the mixture stirred for 20 min. The reaction was then diluted with H2O (50 ml) and extracted with Et2O (2×100 ml). The combined organic layers were dried (MgSO4) and the solvent removed in vacuo to give the title compound as a yellow oil which was used in the next step without further purification. LCMS purity 92%, m/z 403 [M+H]+.

1. stirringthe mixture stirred for 20 min
2. extractionextracted with Et2O (2×100 ml)
3. dry with materialThe combined organic layers were dried (MgSO4)
4. customthe solvent removed in vacuo