5-[(4-Chloro-2-fluorophenyl){5-fluoro-7-[(methylsulfanyl)methyl]-1H-indol-3-yl}methyl]-2,2-dimethyl-1,3-dioxane-4,6-dione → Ethyl 3-(4-chloro-2-fluorophenyl)-3-{5-fluoro-7-[(methylsulfanyl)methyl]-1H-indol-3-yl}propanoate

Participants

Reaction Steps

1.9 mg (0.03 mmol) of copper powder were added to 2.20 g of the compound from Example 16A with a purity of 71% (3.26 mmol) in 25 ml of pyridine and 6.7 ml of ethanol. The reaction mixture was heated under reflux for 1 h. It was concentrated, and the residue was purified by flash chromatography on silica gel (mobile phase: cyclohexane/ethyl acetate gradient) to result in 1.22 g (88% of theory) of the target compound.

Provenance & Evidence