反应详情

温度

60 °C

A solution of (R)-benzyl 3-(5-bromothiophene-2-sulfonamido)-4-(dimethylamino)butanoate (25 mg, 0.05 mmol) and 3-ethynyltoluene (6 mg, 0.055 mmol) in ethyl acetate (0.5 mL) and H2O (50 μL) was purged with argon. Triethylamine (15 μL, 0.1 mmol), copper iodide (0.5 mg, 0.05 eq) and Bis(triphenylphosphine)palladium(II) dichloride (0.9 mg, 0.025 eq) were added and the solution was heated to 60° C. for 2 h. The mixture was cooled and purified by silica gel chromatography (CH2Cl2 to 2% MeOH in CH2Cl2) to give the title compound as a green oil (25 mg, 92%). MS ESI 497.3 [M+H]+, calcd for [C26H28N2O4S+H]+ 497.15.

1. temperatureThe mixture was cooled
2. custompurified by silica gel chromatography (CH2Cl2 to 2% MeOH in CH2Cl2)