4-ETHOXY-2-FLUOROBENZALDEHYDE synthesis

Yield:532965-74-5 83%

Reaction Conditions:

with potassium carbonate in N,N-dimethyl-formamide at 25 - 60; for 10 h;Inert atmosphere;

Steps:

136B

To a mixture of 2-fluoro-4-hydroxy-benzaldehyde (1.0 g, 7.1 mmol) and potassium carbonate (2.0 g, 14 mmol) in N, N-dimethylformamide ( 10 mL) at 25 °C under nitrogen was added iodoethane (1.1 g, 7.1 mmol). The mixture was stirred at 60 °C for 10 hours, concentrated in vacuo, diluted with ethyl acetate (200 mL), washed with saturated sodium bicarbonate solution (3 x 50 mL) and brine (3 x 50 mL), dried with anhydrous sodium sulfate and concentrated in vacuo to give compound B-238 (1.0 g, 83% yield) as a red solid. -NMR (CD₃OD, 400 MHz): 10.09 (s, 7.76-7.67 (m, IH), 6.83-6.74 (m, 2H), 4.11 (t, J=6.8 Hz, 2H), 1.40 (t, J=7.0 Hz, 3H).

References:

WO2016/100184,2016,A1 Location in patent:Paragraph 00537-00538