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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 561665Generated: October 26, 2026

Dichloromethane → 3-[(2-Chloro-4-fluorophenyl)(cyclopropyl)methyl]-6-fluoro-7-[(methylsulfanyl)methyl]-1H-indole

https://huagongshe.com/reaction/561665

Reaction equation

Participants

RoleNameHCIDCharge
ReactantDichloromethaneHCID 6344—
ReactantTrifluoroacetic acidHCID 6422—
Reactant(4-Chloro-2,6-difluorophenyl)(cyclopropyl)methanolHCID 58392245—
Reactant6-Fluoro-7-[(methylsulfanyl)methyl]-1H-indoleHCID 58392259—
Product3-[(2-Chloro-4-fluorophenyl)(cyclopropyl)methyl]-6-fluoro-7-[(methylsulfanyl)methyl]-1H-indoleHCID 58392412—

Reaction Steps

514 mg (2.56 mmol) of the compound from Example 156A and 0.24 ml (3.07 mmol) of trifluoroacetic acid were added to 500 mg (2.56 mmol) of the compound from Example 9A in 4 ml of dichloromethane. The reaction mixture was stirred at RT for 30 min, and the crude product was then purified three times by preparative HPLC (mobile phase: acetonitrile/water gradient) and once by flash chromatography on silica gel (mobile phase: cyclohexane/ethyl acetate 10/1). 404 mg (41% of theory) of the title compound were obtained.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08063234B2
Source datasetuspto-grants-2011_11
ORD IDord-4657a26252854f42966973f351de36ac
Source noteuspto-grants-2011_11