Potassium Carbonate → 5-Chloro-pyridine-2-sulfonic acid (4-difluoromethoxy-benzyl)-((R)-5.5-difluoro-2-oxo-azepan-3-yl)-amide

温度

65 °C

5-Chloro-pyridine-2-sulfonic acid ((R)-5,5-difluoro-2-oxo-azepan-3-yl)-amide (0.21 g, 0.61 mmol), 4-(difluoromethoxy)benzyl bromide (0.23 g, 0.91 mmol), K2CO3 (0.85 g, 6.08 mmol), KI (0.02 g, 0.12 mmol) were added to dry DMF (10 ml) and the resultant reaction mixture was stirred for 1.5 h at 65° C. and for additional 3 h at room temperature under an argon atmosphere. The solvent was removed under reduced pressure and the residue was purified over silica gel (first: ethyl acetate/n-heptane 1:2 v/v; second: dichloromethane/MeOH, 100:0-95:5): brownish oil, 0.23 g;

1. customthe resultant reaction mixture
2. customThe solvent was removed under reduced pressure
3. customthe residue was purified over silica gel (first: ethyl acetate/n-heptane 1:2 v/v; second: dichloromethane/MeOH, 100:0-95:5)

ORDレコード

ord-6873cfde16ff470a95b2f71e5fbab44a

出典データセット

uspto-grants-2009_03

DOI

10.6084/m9.figshare.5104873.v1

特許番号

US07501406B2