反应详情

Combine 1-(3,4,5-trimethoxybenzoyl)-3-(4-fluorophenyl)-3-(2-methanesulfonyloxyethyl)pyrrolidine (0.62 g, 1.4 mmol) and 4-(1-(2-ethoxyethyl)-1H-benzimidazol-2-yl)[1,4]diazepane (0.5 g, 1.7 mmol), and N,N-diisopropylethylamine (0.39 g, 3.0 mmol) in acetonitrile (10 mL). Heat to reflux. After 2 days, cool evaporate in vacuo to obtain a residue. Chromatograph the residue on silica gel eluting with 2% triethylamine/20% methanol/ethyl acetate to give a residue. Dissolve the residue in dichloromethane, extract with brine, dry the organic layer over Na2SO4, filter, and evaporate in vacuo to give the title compound: Rf=0.36 (silica gel, 2% triethylamine/30% methanol/ethyl acetate).

1. temperatureHeat to reflux
2. temperaturecool
3. customevaporate in vacuo
4. customto obtain a residue
5. extractionextract with brine
6. dry with materialdry the organic layer over Na2SO4
7. filtrationfilter
8. customevaporate in vacuo