反应详情

温度

100 °C

In a 20 mL microwave vial is placed 5-(6-benzyloxymethyl-pyrimidin-4-yloxy)-4-fluoro-2-methyl-1H-indole (2.59 g, 7.13 mmol) in methane sulfonic acid (15 ml) and the solution is heated in a microwave reactor at 100° C. for 5 min. The reaction is then diluted with 250 mL EtOAc and saturated aqueous NaHCO3. The aqueous layer is washed with EtOAc (4×100 mL). The organic phases are combined, washed with (2×150 mL) water, followed by (1×60 mL brine), dried over Na2SO4, and concentrated in vacuo. The residue is purified via FCC (0-20% MeOH/DCM) to give the title compound. MS (ESI) m/z 274.1 (M+1).

1. washThe aqueous layer is washed with EtOAc (4×100 mL)
2. washwashed with (2×150 mL) water
3. dry with materialdried over Na2SO4
4. concentrationconcentrated in vacuo
5. customThe residue is purified via FCC (0-20% MeOH/DCM)