反应详情

To a stirred solution of rac-cis-1-(5-(4-fluorophenyl)-2-methylthiazole-4-carbonyl)-3-methylpiperidine-2-carbaldehyde and 5-fluoropyridin-2-amine in methanol/acetic acid (50:1) was added sodium cyanoborohydride at 0° C. The reaction was then stirred at rt overnight. After ˜16 h, the reaction mixture was transferred to a seperatory funnel, diluted with EtOAc, saturated NaHCO3 and the layers separated. The organic layer was washed with water, brine, dried (MgSO4), and concentrated in vacuo. The crude reaction mixture was purified by reverse-phase preparative HPLC to afford the title compound. MS (ESI) 443.2 (M+H).

1. waitAfter ˜16 h
2. customthe reaction mixture was transferred to a seperatory funnel
3. customthe layers separated
4. washThe organic layer was washed with water, brine
5. dry with materialdried (MgSO4)
6. concentrationconcentrated in vacuo
7. customThe crude reaction mixture
8. customwas purified by reverse-phase preparative HPLC