反应详情

100 mg (0.26 mmol) Methanesulfonic acid 5-[1-(4-fluoro-phenyl)-1H-indol-5-yl]-pent-4-ynyl ester and 0.5 ml (5.2 mmol) N-allylmethylamine were stirred in 1 ml DMF at 60° C. for 1.5 h. The solution was concentrated, and the residue was dissolved in water and CH2Cl2. 2M NaOH was added and the inorganic phase was extracted with CH2Cl2. The combined organic phases were washed with water and dried over Na2SO4. Column chromatography with CH2Cl2/MeOH 19:1 yielded 50 mg (55%) Allyl-{5-[1-(4-fluoro-phenyl)-1H-indol-5-yl]-pent-4-ynyl}-methyl-amine as light yellow oil, MS: 347 (MH+).

1. concentrationThe solution was concentrated
2. dissolutionthe residue was dissolved in water
3. addition2M NaOH was added
4. extractionthe inorganic phase was extracted with CH2Cl2
5. washThe combined organic phases were washed with water
6. dry with materialdried over Na2SO4