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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 561681Generated: October 27, 2026

Trifluoroacetic acid → HCID 58392454, compound

https://huagongshe.com/reaction/561681

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
Reactantindium(III)chlorideHCID 159675—
Reactant5-Fluoro-7-[(methylsulfonyl)methyl]-1H-indoleHCID 58392318—
Reactant(4-Chlorophenyl)(2,2-difluorocyclopropyl)methanolHCID 58392413—
Solvent1,2-DichloroethaneHCID 11—
ProductHCID 58392454HCID 58392454—

Reaction Steps

97.1 mg (0.44 mmol) of indium(III) chloride and 0.05 ml (0.07 mmol) of trifluoroacetic acid were added to 80.0 mg (0.37 mmol) of the compound from Example 159A and 100 mg (0.44 mmol) of the compound from Example 87A in 4 ml of 1,2-dichloroethane, and the mixture was heated under reflux overnight. It was concentrated and the residue was taken up in ethyl acetate and washed with saturated aqueous sodium bicarbonate solution and saturated aqueous sodium chloride solution, dried over sodium sulfate, filtered and concentrated. The residue was purified by preparative HPLC (RP18 column; mobile phase: acetonitrile/water gradient with addition of 0.1% formic acid) to result in 6.0 mg (4% of theory) of the title compound as mixture of diastereomers.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08063234B2
Source datasetuspto-grants-2011_11
ORD IDord-ff602075e8c14e479ad01e3a9d396931
Source noteuspto-grants-2011_11