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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1410246Generated: November 2, 2026

Trifluoroacetic acid → N-(4-bromo-phenyl)-2-(2-chloro-5-{[amino]-methyl}-phenylamino)-6-(2,2-difluoro-ethoxy)-1-methyl-1H-benzimidazole-5-carboxylic acid amide

https://huagongshe.com/reaction/1410246

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
ReactantN-(4-Bromo-phenyl)-2-(2-chloro-5-{[(tert-butoxycarbonyl)-amino]-methyl}-phenylamino)-6-(2,2-difluoro-ethoxy)-1-methyl-1H-benzimidazole-5-carboxylic acid amideHCID 86646339—
SolventDichloromethaneHCID 6344—
ProductN-(4-bromo-phenyl)-2-(2-chloro-5-{[amino]-methyl}-phenylamino)-6-(2,2-difluoro-ethoxy)-1-methyl-1H-benzimidazole-5-carboxylic acid amideHCID 59529876—

Reaction Steps

A mixture of N-(4-bromo-phenyl)-2-(2-chloro-5-{[(tert-butoxycarbonyl)-amino]-methyl}-phenylamino)-6-(2,2-difluoro-ethoxy)-1-methyl-1H-benzimidazole-5-carboxylic acid amide (1.35 g; 2.03 mmol) and TFA (3.47 g; 30.5 mmol) in DCM (75 mL) was stirred over night at rt. The mixture was cooled to 0° C. and basicified to pH ˜10 and extracted with DCM. The organic extracts were dried over Na2SO4, filtered and concentrated. The residue was washed with a mixture of Et2O and petroleum ether to give the sub-title compound.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08921405B2
Source datasetuspto-grants-2014_12
ORD IDord-6384e2fdd33a48c0aea157071707954f
Source noteuspto-grants-2014_12