反应详情

Heat 500 mg (2.19 mmol) 4-chloro-5-phenylfuro[2,3-d]pyrimidine, 1.51 ml (8.67 mmol) DIEA and 1 ml DMF to 160° C. and add 787.6 mg (4.34 mmol) 6-aminohexanoic acid methyl ester hydrochloride. After 4 h at 160° C., cool the reaction mixture, add to ice water and extract three times with ethyl acetate. Combine the organic phases and wash with saturated ammonium chloride solution, dry over magnesium sulphate and concentrate under vacuum. Purify the residue by chromatography on silica gel (solvent: cyclohexane/ethyl acetate 10:1→3:1). 470 mg (63.9% of theor.) of the target compound is obtained.

1. temperaturecool the reaction mixture
2. extractionextract three times with ethyl acetate
3. washwash with saturated ammonium chloride solution
4. dry with materialdry over magnesium sulphate
5. concentrationconcentrate under vacuum
6. customPurify the residue by chromatography on silica gel (solvent: cyclohexane/ethyl acetate 10:1→3:1)
7. custom470 mg (63.9% of theor.) of the target compound is obtained