反应详情

温度

100 °C

20 mg (0.11 mmol) of copper iodide, 28 mg (0.27 mmol) of triethylamine and 14 mg (0.02 mmol) of dichlorobis(triphenylphosphine)-palladium (II) are added to a suspension of 80 mg (0.21 mmol) of 8-iodo-4-oxo-4,5-dihydro-3H-pyrrolo[2,3-c]quinoline-1-ethyl carboxylate in 2.4 ml of anhydrous dioxan, then this mixture is degassed under argon. After 15 minutes, 32 mg (0.31 mmol) of 2-ethynyl-pyridine are added, then the mixture is heated at 100° C. for 3 hours. The raw reaction product is then filtered on celite, the filtrate is evaporated to dryness and the residue is purified by chromatography on silica (eluent ethyl acetate) to give 34 mg (46%) of 4-oxo-8-pyridin-2-ylethynyl-4,5-dihydro-3H-pyrrolo[2,3-c]quinoline-1-ethyl carboxylate in the form of a brown solid.

1. customthis mixture is degassed under argon
2. customThe raw reaction product
3. filtrationis then filtered on celite
4. customthe filtrate is evaporated to dryness
5. customthe residue is purified by chromatography on silica (eluent ethyl acetate)