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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 558246Generated: October 29, 2026

Trifluoroacetic acid → Methyl 5-acetyl-2-(2-fluoro-4-iodophenylamino)-3,4-difluorobenzoate

https://huagongshe.com/reaction/558246

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
ReactantN-IodosuccinimideHCID 120273—
ReactantMethyl 5-acetyl-2-(2-fluorophenylamino)-3,4-difluorobenzoateHCID 59519431—
SolventDimethylformamideHCID 6228—
SolventEthyl AcetateHCID 8857—
ProductMethyl 5-acetyl-2-(2-fluoro-4-iodophenylamino)-3,4-difluorobenzoateHCID 59519381—

Reaction Steps

To a solution of methyl 5-acetyl-2-(2-fluorophenylamino)-3,4-difluorobenzoate (0.47 mmol, 0.16 g) in DMF (10 ml) was added NIS (0.56 mmol, 0.13 g) and TFA (0.10 ml), and the reaction was stifled at room temp overnight. The crude was diluted with EtOAc and washed with H2O. The organic fraction was dried over MgSO4 and concentrated under reduced pressure to yield the desired product in 90% (0.23 g).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08063049B2
Source datasetuspto-grants-2011_11
ORD IDord-e807b901fb0a4356a8cf7ddd48731e63
Source noteuspto-grants-2011_11