反应详情

温度

80 °C

Potassium carbonate (410 mg, 2.97 mmol) was added to a solution of 1-benzenesulfonyl-2-[2-cyclopentyl-1-(4-methanesulfonyl-phenyl)-vinyl]-1H-pyrrolo[2,3-b]pyridin-5-ol (prepared as in Example 13, 310 mg, 0.59 mmol) in N,N-dimethylformamide (2 mL) at room temperature for 30 min. 2-Dimethylaminoethyl chloride hydrochloride (85.6 mg, 0.59 mmol) was then added. The mixture was heated at 80° C. for 1 h. The resulting reaction mixture was diluted with ethyl acetate (150 mL), washed with brine, dried over anhydrous sodium sulfate and then concentrated in vacuo to afford (2-{1-benzenesulfonyl-2-[2-cyclopentyl-1-(4-methanesulfonyl-phenyl)-vinyl]-1H-pyrrolo[2,3-b]pyridin-5-yloxy}-ethyl)-dimethyl-amine (350 mg, quant.) as a light yellow solid which was used in the next step without further purification: LC/MS m/e calcd for C31H35N3O5S2 [M+H]+ 594.77, observed 594.2.

1. customThe resulting reaction mixture
2. washwashed with brine
3. dry with materialdried over anhydrous sodium sulfate
4. concentrationconcentrated in vacuo