反应详情

温度

100 °C

(±)-tert-Butyl 4-((1-(5-bromo-2-((2-(trimethylsilyl)ethoxy)methyl)-2H-indazol-7-yl)ethoxy)methyl)-4-(4-fluorophenyl)piperidine-1-carboxylate (75 mg, 0. 113 mmol), cyclopropyl boronic acid (20 mg, 0.34 mmol), and tetrakis(triphenylphosphine) palladium(0) (13. 1 mg, 0.011 mmol) were combined in dry tetrahydrofuran (2 mL) followed by addition of 0.58 mL of a 1 N aqueous potassium hydroxide solution in a microwave tube and sealed. After flushing the mixture with nitrogen, the mixture was heated at 100° C. for 1 h via microwave. After cooling to room temperature, the reaction mixture was concentrated, dissolved in ethyl acetate and washed with water and brine, concentrated and purified by flash chromatography on silica gel (20% EtOAc/Hex) to afford 70.5 mg (100%) as an oil. LC/MS (HPLC method 2): tR=3.738 min, 624.24(MH)+.

1. customsealed
2. customAfter flushing the mixture with nitrogen
3. temperatureAfter cooling to room temperature
4. concentrationthe reaction mixture was concentrated
5. dissolutiondissolved in ethyl acetate
6. washwashed with water and brine
7. concentrationconcentrated
8. custompurified by flash chromatography on silica gel (20% EtOAc/Hex)
9. customto afford 70.5 mg (100%) as an oil