Trifluoroacetic acid → 2-({5-Fluoro-7-[(methylsulfonyl)methyl]-1H-indol-3-yl}[2-fluoro-4-(trifluoro-methyl)phenyl]methyl)cyclopropanecarbonitrile

Participants

Reaction Steps

1.63 g (7.35 mmol) of indium(III) chloride and 0.85 ml (11.0 mmol) of trifluoroacetic acid were added to 1.59 g (6.13 mmol) of the compound from Example 164A and 1.90 g (7.35 mmol) of the compound from Example 87A in 100 ml of 1,2-dichloroethane, and the mixture was heated under reflux overnight. It was concentrated and the residue was purified by preparative HPLC (RP18 column; mobile phase: acetonitrile/water gradient with addition of 0.1% formic acid) to result in 763 mg (27% of theory) of the title compound as mixture of diastereomers.

Provenance & Evidence