反应详情

温度

50 °C

The product from Example 42B (3.14 g, 5.64 mmol) and 4-cyclopropylaniline (6.01 g, 45.2 mmol) were combined in DMF (20 mL). The mixture was stirred at 50° C. under nitrogen for 3 hours. The reaction mixture was partitioned between 1M HCl and ethyl acetate. The organic layer was washed with brine three times, dried with sodium sulfate, filtered and evaporated. The residue was purified by chromatography on silica gel eluting with ethyl acetate/hexane (0.5% to 1%) to give the title compound (2.12 g, 76%) as a mixture of stereoisomers as a sticky solid.

1. customThe reaction mixture was partitioned between 1M HCl and ethyl acetate
2. washThe organic layer was washed with brine three times
3. dry with materialdried with sodium sulfate
4. filtrationfiltered
5. customevaporated
6. customThe residue was purified by chromatography on silica gel eluting with ethyl acetate/hexane (0.5% to 1%)