反应详情

温度

80 °C

A mixture of 5 g (20 mmol) 1-Bromo-2-fluoro-4-trifluoromethyl-benzene, 4.6 g (24.7 mmol) n-Boc-piperazine, 106 mg (0.1 mmol) Tris(dibenzylideneacetone)dipalladium chloroform complex 2.77 g (28.8 mmol) sodium-t-butoxide and 144 mg (0.4 mmol) 2-(Dicyclohexylphosphino)biphenyl in 50 ml toluene was heated for 16 h at 80° C. After cooling to room temperature the mixture was treated with 15 g Isolute HM-N and all volatiles were removed under vacuum. The residue was purified on silica eluting with a gradient of heptane/EtOAc to yield after evaporation 4.54 g (63%) of the title compound as white amorphous solid.

1. temperatureAfter cooling to room temperature the mixture
2. additionwas treated with 15 g Isolute HM-N
3. customall volatiles were removed under vacuum
4. customThe residue was purified on silica eluting with a gradient of heptane/EtOAc
5. customto yield
6. customafter evaporation 4.54 g (63%) of the title compound as white amorphous solid