反应详情

A mixture of 5-bromo-1-(4-isopropoxyphenyl)indole-2-carboxylic acid ethyl ester (154 mg, 0.38 mmol), K3PO4 (282 mg, 1.83 mmol), Pd(OAc)2 (4.5 mg, 0.02 mmol), tri(o-tolyl)phosphine (12 mg, 0.04 mmol), and toluene (3.5 mL) was stirred under argon for 25 min at room temperature. 4-Cyclohexylphenylboronic acid (117 mg, 0.57 mmol) in EtOH (0.5 mL) was added and the mixture was heated at reflux for 1 h. The mixture was allowed to cool, poured into NaHCO3 (aq. sat.), and extracted wait EtOAc. The combined extracts were washed with brine, dried over Na2SO4, concentrated and purified by chromatography to give the sub-title compound (170 mg, 93%).

1. temperaturethe mixture was heated
2. temperatureat reflux for 1 h
3. temperatureto cool
4. extractionextracted
5. waitwait EtOAc
6. washThe combined extracts were washed with brine
7. dry with materialdried over Na2SO4
8. concentrationconcentrated
9. custompurified by chromatography