反应详情

温度

120 °C

To a solution of ethyl 3-(4-{[2-ethyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]methyl}-1-piperidinyl)propanoate (D140) (1.3 g, 3.03 mmol) in N,N-Dimethylformamide (DMF) (6 mL) and Water (1.500 mL) was added 3-bromo-5-{3-chloro-4-[(1-methylethyl)oxy]phenyl}-1,2,4-thiadiazole (D43) (1.010 g, 3.03 mmol), tripotassium phosphate (1.928 g, 9.08 mmol) and Pd(Ph3P)4 (0.350 g, 0.303 mmol). The reaction mixture was heated by Biotage Initiator to 120° C. for 20 min. The reaction mixture was diluted with ethyl acetate, washed with water, dried and concentrated and purified by ISCO column chromatography to afford ethyl 3-(4-{[3-(5-{3-chloro-4-[(1-methylethyl)oxy]phenyl}-1,2,4-thiadiazol-3-yl)-2-ethylphenyl]methyl}-1-piperidinyl)propanoate (D141) (0.63 g). MS (ES): C30H38ClN3O3S requires 555.2. found 556.2 (M+H+).

1. washwashed with water
2. customdried
3. concentrationconcentrated
4. custompurified by ISCO column chromatography