反应详情

Under an N2 atmosphere 5 mL 2 M Na2CO3 solution and 47 mg (0.41 mmol) tetrakis-triphenylphosphane-palladium are added to a solution of 310 mg (0.82 mmol) 1-{2-[4-(4-bromo-thiophen-2-ylethynyl)-phenoxy]-ethyl}-pyrrolidine and 129 mg (0.82 mmol) 4-chlorophenyl-boric acid in 10 mL 1,4-dioxane and the reaction mixture is refluxed for 1 h. The hot solution is filtered through a fibreglass filter, the filtrate is extracted with EtOAc, the organic phase is washed with water and dried over MgSO4. After the desiccant and solvent have been eliminated the residue is purified by chromatography (silica gel, EtOAc/MeOH/NH3 8:2:0.2).

1. temperaturethe reaction mixture is refluxed for 1 h
2. filtrationThe hot solution is filtered through a fibreglass
3. filtrationfilter
4. extractionthe filtrate is extracted with EtOAc
5. washthe organic phase is washed with water
6. dry with materialdried over MgSO4
7. customis purified by chromatography (silica gel, EtOAc/MeOH/NH3 8:2:0.2)