反应详情

6-Amino-3-(4-pyridyl)-2-(4-fluorophenyl)-7-aza-indole (17) (100 mg, 0.329 mmol), benzaldehyde (100 ml, 0.987 mmol), and 1,2-dichloroethane (20 mL) were allowed to stir for 15 min followed by the addition of sodium triacetoxyborohydride (139 mg, 0.658 mmol) as a solid. After 16 h at 23° C., the reaction was partitioned between ethyl acetate (200 mL) and satd bicarbonate (80 mL). The organic layer was washed with brine (80 mL), and dried (Na2SO4). After concentration in vacuo, a portion of the residue was purified by preparative chromatography to afford 6-(phenylmethylamino)-3-(4-pyridyl)-2-(4-fluoro phenyl)-7-aza-indole (144):Mass Spectrum (CI) 395 (MH+).

1. waitAfter 16 h at 23° C.
2. customthe reaction was partitioned between ethyl acetate (200 mL) and satd bicarbonate (80 mL)
3. washThe organic layer was washed with brine (80 mL)
4. dry with materialdried (Na2SO4)
5. concentrationAfter concentration in vacuo
6. customa portion of the residue was purified by preparative chromatography