反应详情

Combine 1-(3,4,5-trimethoxybenzyl)-3-(4-fluorophenylmethyl)-3-(3-methanesulfonyloxypropyl)-2-oxopyrrolidine (0.43 g, 1.50 mmol), (1-(2-ethoxyethyl)-1H-benzimidazol-2-yl)(piperidin-4-yl)amine (0.74 g, 1.46 mmol), and N,N-diisopropylethylamine (0.39 g, 3.0 mmol) in acetonitrile (10 mL). Heat to reflux. After 12 hours, dilute the reaction mixture with ethyl acetate and extract twice with water. Dry the organic layer over Na2SO4, filter, and evaporate in vacuo to give a residue. Chromatograph the residue on silica gel eluting with 10% methanol/ethyl acetate/2% triethylamine. Combine the product containing fractions and evaporate in vacuo to give a residue. Combine the residue and dichloromethane and extract with brine. Dry the organic layer over Na2SO4, filter, and evaporate in vacuo to give the title compound.

1. temperatureHeat to reflux
2. extractionextract twice with water
3. dry with materialDry the organic layer over Na2SO4
4. filtrationfilter
5. customevaporate in vacuo
6. customto give a residue
7. additioncontaining fractions
8. customevaporate in vacuo
9. customto give a residue
10. extractionextract with brine
11. dry with materialDry the organic layer over Na2SO4
12. filtrationfilter
13. customevaporate in vacuo