反应详情

A mixture of 4-(5-bromo-2-methoxyphenyl)-1,1,1-trifluoro-4-methyl-2-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)pentan-2-ol (188 mg, 0.4 mmol), pyridine 3-boronic acid 1,3-propanediol cyclic ester (89 mg, 0.6 mmol), potassium carbonate (K2CO3; 166 mg, 1.2 mmol), and Pd(PPh3)4 (46.2 mg, 0.04 mmol) in 3.0 mL of DME-MeOH-DMF (1:1.5:0.5) was microwaved for 20 minutes at 120° C., cooled to room temperature, diluted with 20 mL of ethyl acetate and filtered through diatomaceous earth. The filtrate was washed with 5 mL of 1.0 M aqueous sodium hydroxide solution, water, and brine, dried over magnesium sulfate, and concentrated in vacuo. The residue was purified by silica gel chromatography to yield 90 mg (48% yield) of the title compound as a white foam.

1. customwas microwaved for 20 minutes at 120° C.
2. filtrationfiltered through diatomaceous earth
3. washThe filtrate was washed with 5 mL of 1.0 M aqueous sodium hydroxide solution, water, and brine
4. dry with materialdried over magnesium sulfate
5. concentrationconcentrated in vacuo
6. customThe residue was purified by silica gel chromatography