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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 561677Generated: October 26, 2026

Trifluoroacetic acid → 3-[Cyclopropyl(2,2-difluoro-1,3-benzodioxol-5-yl)methyl]-5-fluoro-7-[(methylsulfonyl)methyl]-1H-indole

https://huagongshe.com/reaction/561677

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
ReactantCyclopropyl(2,2-difluoro-1,3-benzodioxol-5-yl)methanolHCID 58392116—
Reactant5-Fluoro-7-[(methylsulfonyl)methyl]-1H-indoleHCID 58392318—
SolventDichloromethaneHCID 6344—
Product3-[Cyclopropyl(2,2-difluoro-1,3-benzodioxol-5-yl)methyl]-5-fluoro-7-[(methylsulfonyl)methyl]-1H-indoleHCID 44595238—

Reaction Steps

100 mg (0.44 mmol) of the compound from Example 157A 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 5 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). 151 mg (78% 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-0bbde19fc05242369e05029fe0bb3454
Source noteuspto-grants-2011_11