ethyl 2-(5-fluoro-2-Methyl-1H-indol-1-yl)acetate synthesis

Yield:851460-85-0 95%

Reaction Conditions:

with caesium carbonate in N,N-dimethyl-formamide at 60; for 3 h;

Steps:

1.8 Step 8

To the compound 5-fluoro-2-methyl-1H-indole (10.00 g, 67.04 mmol) and cesium carbonate (32.77 g, 100.56 mmol) in 100 mL of N,N-dimethylformamide at room temperature Ethyl bromoacetate (13.44 g, 80.45 mmol) was added dropwise to the solution. The reaction solution was reacted at 60°C for 3 hours. After the reaction was completed, 200 mL of saturated sodium bicarbonate solution was added to the reaction solution, and the mixture was extracted with ethyl acetate (100 mL×3). The organic phase was washed with saturated aqueous sodium chloride solution, dried over anhydrous sodium sulfate, filtered, and concentrated using a silica gel column. Purification (petroleum ether/ethyl acetate 100-50%) gave the title compound 1k (15.00 g, pale yellow oil, yield: 95%).

References:

CN107987072,2018,A Location in patent:Paragraph 0080; 0095; 0096