反应详情

To a solution of 4-chloro-N-(3-chlorophenyl)pyrimidin-2-amine (300 mg, 1.25 mmol) and tert-butyl 2-(aminomethyl)-piperidine-1-carboxylate (540 mg, 2.50 mmol) in THF (10 mL) is added diisopropylethyl-amine (0.43 mL, 2.50 mmol). The reaction is heated at reflux for 18 hours and then cooled to room temperature. The crude reaction is partitioned between EtOAc and sat. NaHCO3. The organic layer is dried (MgSO4), concentrated in vacuo, and purified over silica (MeOH/CH2Cl2) to afford 268 mg (51% yield) of the desired compound: MS (ESI, pos. ion) m/z: 418 (M+1).

1. temperatureThe reaction is heated
2. temperatureat reflux for 18 hours
3. customThe crude reaction
4. customis partitioned between EtOAc and sat. NaHCO3
5. dry with materialThe organic layer is dried (MgSO4)
6. concentrationconcentrated in vacuo
7. custompurified over silica (MeOH/CH2Cl2)