反应详情

tert.-butyl 4-bromo-2-methyl-benzoate (12 g; 43.4 mmol), caesium carbonate (21.2 g, 65 mmol), palladium(II)-acetate (1 g, 4.45 mmol) and BINAP (2.37 g, 4.40 mmol) are suspended in 150 ml of toluene under a nitrogen atmosphere and stirred for 10 minutes at ambient temperature. Then benzylamine (5.7 ml, 52.1 mmol) is added dropwise and the mixture is heated to 100° C. for two days. The mixture is then cooled, filtered to remove undissolved matter and evaporated to dryness. The oily residue is purified by chromatography (silica gel, petroleum ether/ethyl acetate 98:2). White crystals are obtained.

1. temperaturethe mixture is heated to 100° C. for two days
2. temperatureThe mixture is then cooled
3. filtrationfiltered
4. customto remove undissolved matter
5. customevaporated to dryness
6. customThe oily residue is purified by chromatography (silica gel, petroleum ether/ethyl acetate 98:2)
7. customWhite crystals are obtained