反应详情

3-{4-[1-(4-Bromo-phenoxyl)-heptyl]-benzoylamino}-propionic acid methyl ester (isomer 1, 100 mg, 0.21 mmol), potassium carbonate (85 mg, 0.63 mmol), 4-trifluoromethoxylphenyl boronic acid (86 mg, 0.42 mmol) and tetrakis-(triphenylphosphine)palladium (24 mg, 0.021 mmol) are place in a flask. After the reaction is purged with N2 for several times, THF/H2O (20 ml/5 ml) is added. The resulting solution is refluxed overnight, concentrated and acidified by 1 N HCl (0.6 mL), extracted with ethyl acetate. Combined organic layers are washed with water and brine, dried over sodium sulfate, purified by reverse phase HPLC to give the title compound (40 mg). MS (ES): 526.2 [M−H]−.

1. customAfter the reaction is purged with N2 for several times, THF/H2O (20 ml/5 ml)
2. additionis added
3. temperatureThe resulting solution is refluxed overnight
4. concentrationconcentrated
5. extractionextracted with ethyl acetate
6. washCombined organic layers are washed with water and brine
7. dry with materialdried over sodium sulfate
8. custompurified by reverse phase HPLC