反应详情

A solution of ethyl (4-{[2-ethyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]methyl}-1-piperidinyl)acetate (D144) (200 mg, 0.481 mmol), 3-bromo-5-{3-chloro-4-[(1-methylethyl)oxy]phenyl}-1,2,4-thiadiazole (D43) (161 mg, 0.481 mmol), tripotassium phosphate (307 mg, 1.444 mmol) and Pd(Ph3P)4 (55.6 mg, 0.048 mmol) in N,N-Dimethylformamide (DMF) (6 mL) and Water (1.500 mL) was heated by Biotage Initiator to 120° C. for 15 min. The reaction solution was diluted with ethyl acetate, washed with water, dried over sodium sulphate, concentrated and purified by ISCO column chromatography to afford ethyl (4-{[3-(5-{3-chloro-4-[(1-methylethyl)oxy]phenyl}-1,2,4-thiadiazol-3-yl)-2-ethylphenyl]methyl}-1-piperidinyl)acetate (D145) (80 mg). MS (ES): C29H36ClN3O3S requires 541.2. found 542.2 (M+H+).

1. washwashed with water
2. dry with materialdried over sodium sulphate
3. concentrationconcentrated
4. custompurified by ISCO column chromatography