Trifluoroacetic acid → 2-[1-(2,4-Difluorophenyl)-1-{5-fluoro-7-[(methylsulfanyl)methyl]-1H-indol-3-yl}ethyl]cyclopropanecarbonitrile

Participants

Reaction Steps

273 mg (1.23 mmol) of indium(III) chloride and 0.1 ml (1.34 mmol) of trifluoroacetic acid were added to 250 mg (1.12 mmol) of the compound from Example 11A and 437 mg (2.24 mmol) of the compound from Example 133A were introduced into 44 ml of dichloromethane, and the mixture was stirred at RT overnight. The reaction mixture was concentrated in a rotary evaporator. The residue was purified by preparative HPLC (RP18 column; mobile phase: acetonitrile/water gradient with addition of 0.1% formic acid) to result in 313 mg (69% of theory) of the title compound as mixture of diastereomers.

Provenance & Evidence