反应详情

5-bromo-3-(1-tosyl-2-(S)-pyrrolidinylmethoxy)pyridine from step 51b (300 mg, 10.73 mmol), boric acid (107 mg, 10.88 mmol) and Pd(0) (26 mg) were mixed together in benzene (2 mL), and the mixture was heated at reflux for 16 hours. NaHCO3 solution (2%, 1 mL) was added, and the mixture was extracted with chloroform. The CHCl3 was removed under reduced pressure, and the residue was chromatographed on a silica gel column, eluting with ethyl acetate/hexane 1:1 to afford the title compound (300 mg).

1. temperaturethe mixture was heated
2. temperatureat reflux for 16 hours
3. extractionthe mixture was extracted with chloroform
4. customThe CHCl3 was removed under reduced pressure
5. customthe residue was chromatographed on a silica gel column
6. washeluting with ethyl acetate/hexane 1:1