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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 2241906Generated: November 1, 2026

Water → 1-Benzyl-4-(2-fluoro-4-nitrophenyl)-[1,4]diazepane

https://huagongshe.com/reaction/2241906

Reaction equation

Participants

RoleNameHCIDCharge
ReactantWaterHCID 962—
ReactantBenzyl BromideHCID 7498—
ReactantPotassium CarbonateHCID 11430—
ReactantHCID 68547759HCID 68547759—
SolventDimethylformamideHCID 6228—
Product1-Benzyl-4-(2-fluoro-4-nitrophenyl)-[1,4]diazepaneHCID 59204898579.2%

Reaction Conditions

Temperature80 °C

Reaction Steps

Potassium carbonate (0.526 g, 3.80 mmol) and benzyl bromide (0.155 ml, 0.130 mmol) were added to a solution of 1-(2-fluoro-4-nitrophenyl)-[1,4]diazepane hydrochloride (compound of Reference Example 55; 0.300 g, 1.08 mmol) in anhydrous N,N-dimethylformamide (6 ml), and the mixture was stirred at 80° C. for 6 hours. Water was added to the reaction mixture and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine and dried over anhydrous sodium sulfate. The residue obtained by evaporation of the solvent under reduced pressure was purified by column chromatography on silica gel (methanol ethyl acetate=1:1) to give the title compound (0.248 g, 69%) as a brown liquid.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07671058B2
Source datasetuspto-grants-2010_03
ORD IDord-f647db050e31459d910fae45e2faaa5b
Source noteuspto-grants-2010_03