反应详情

温度

120 °C

A mixture of 3-bromo-2-(4-fluoro-phenyl)-4-hydroxy-1-phenyl-1H-pyrrolo[2,3-c]pyridine-5-carboxylic acid ethyl ester (200 mg), Zn(CN)2 (31 mg), Zn dust (3.5 mg), Pd2(dba)3 (20 mg), dppf (24.4 mg) in DMA (1 mL) was heated to 120° C. for 145 min; then the mixture was partitioned between EtOAc and water, the organic phase was then washed with sat. NaCl solution, dried over anhydrous sodium sulfate, filtered and concentrated sequentially to give a residue, which was purified with column to give desired title compound (83 mg). The title compound, ESI MS (m/z): 402 (M+H)+.

1. customthen the mixture was partitioned between EtOAc and water
2. washthe organic phase was then washed with sat. NaCl solution
3. dry with materialdried over anhydrous sodium sulfate
4. filtrationfiltered
5. concentrationconcentrated sequentially
6. customto give a residue, which
7. customwas purified with column