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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 561676Generated: October 30, 2026

Trifluoroacetic acid → 3-[(4-Chloro-2,6-difluorophenyl)(cyclopropyl)methyl]-5-fluoro-7-[(methylsulfonyl)methyl]-1H-indole

https://huagongshe.com/reaction/561676

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
Reactant(4-Chloro-2,6-difluorophenyl)(cyclopropyl)methanolHCID 58392245—
Reactant5-Fluoro-7-[(methylsulfonyl)methyl]-1H-indoleHCID 58392318—
SolventDichloromethaneHCID 6344—
Product3-[(4-Chloro-2,6-difluorophenyl)(cyclopropyl)methyl]-5-fluoro-7-[(methylsulfonyl)methyl]-1H-indoleHCID 58392165—

Reaction Steps

96 mg (0.44 mmol) of the compound from Example 156A and 0.04 ml (0.53 mmol) of trifluoroacetic acid were added to 100 mg (0.44 mmol) of the compound from Example 87A in 3 ml of dichloromethane. The reaction mixture was stirred at RT for 45 min, the solvent was removed in vacuo, and the crude product was then purified by preparative HPLC (mobile phase: acetonitrile/water gradient). 162 mg (86% 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-24da6ea17b374dd4bdcfe0906fe97368
Source noteuspto-grants-2011_11