Reaktion #1446525

Reaktionsgleichung

N-iodosuccinic acid imide

N,N-dimethylformamide

2-benzyl-6-[(3R,4R)-3,4-difluoropyrrolidine-1-yl]pyridine

→

target compound

Ausbeute 100.2%

2-Benzyl-6-[(3R,4R)-3,4-difluoropyrrolidine-1-yl]-3-iodopyridine

Ausbeute 100.2%

Lösungsmittel

Water

Reaktionsbedingungen

Aufarbeitung

1. 1
   Temperaturcooling
2. 2
   Extraktionthe mixture was extracted with ethyl acetate
3. 3
   WaschenThe organic phase was washed with an aqueous sodium thiosulfate solution, water and brine
4. 4
   Sonstigethe solvent was removed
5. 5
   Wascheneluted with hexane/ethyl acetate (10:1)

Vorschrift

94 mg of N-iodosuccinic acid imide was added little by little to 5.0 ml of an N,N-dimethylformamide solution containing 104 mg of 2-benzyl-6-[(3R,4R)-3,4-difluoropyrrolidine-1-yl]pyridine under ice-cooling, followed by stirring overnight as it was. Water was added to the reaction solution and the mixture was extracted with ethyl acetate. The organic phase was washed with an aqueous sodium thiosulfate solution, water and brine, and the solvent was removed. The residue was subjected to NH-silica gel (Fuji Silicia) column chromatography and eluted with hexane/ethyl acetate (10:1), to give 152 mg of the target compound.

Quelle