Back
HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 2090739Generated: October 29, 2026

Methanol → tert-butyl ({5-[2-fluoro-3-(hydroxymethyl)phenyl]-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl}methyl)methylcarbamate

https://huagongshe.com/reaction/2090739

Reaction equation

Participants

RoleNameHCIDCharge
ReactantMethanolHCID 887—
ReactantWaterHCID 962—
ReactantSodium borohydrideHCID 4311764—
Reactanttert-butyl {[5-(2-fluoro-3-formylphenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]methyl}methylcarbamateHCID 86631002—
SolventTetrahydrofuranHCID 8028—
Producttert-butyl ({5-[2-fluoro-3-(hydroxymethyl)phenyl]-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl}methyl)methylcarbamateHCID 6697471461.1%

Reaction Steps

To a solution of tert-butyl {[5-(2-fluoro-3-formylphenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]methyl}methylcarbamate (388 mg) in tetrahydrofuran (8 mL) were added under ice-cooling, sodium borohydride (41.3 mg) and methanol (3 mL). After stirring at the same temperature for 30 min, water was added to the reaction mixture and the mixture was extracted with ethyl acetate. The extract was washed with saturated brine, dried over anhydrous sodium sulfate, and concentrated under reduced pressure. The residue was purified by basic silica gel column chromatography (eluent: hexane-ethyl acetate=2:1→1:2) to give the title compound as a colorless oil (yield 238 mg, 61%).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08436187B2
Source datasetuspto-grants-2013_05
ORD IDord-3f82e0d9c9614b9694afeaac62b53b90
Source noteuspto-grants-2013_05