反应详情

4-Chloro-6-iodo-3-methanesulfonyl-2-methyl-quinoline (compound of example D.2) (300 mg, 0.786 mmol), 4-hydroxypiperidine (87 mg, 0.865 mmol) and N,N-diisopropyl ethyl amine (0.148 mL, 0.865 mmol) were heated in dry N,N-dimethylformamide (3 mL) for 0.5 h at 100° C. N,N-Dimethylformamide was evaporated at 40° C./0.1 mbar, and the residue directly purified by chromatography on silica gel in dichloromethane/methanol 20:1. One obtained a yellow oil which was triturated with ethyl acetate and the resulting white crystals were filtered off. One obtained 218 mg (62%) of white crystals. MS: m/z=447 (M+H).

1. customN,N-Dimethylformamide was evaporated at 40° C./0.1 mbar
2. customthe residue directly purified by chromatography on silica gel in dichloromethane/methanol 20:1
3. customOne obtained a yellow oil which
4. customwas triturated with ethyl acetate
5. filtrationthe resulting white crystals were filtered off