反应详情

温度

25 °C

To a solution of 3-ethyl-1-(2-hydroxy-ethyl)-3-(3-methoxyphenyl)-azepan-2-one (as described above in Step A) (0.6 g, 2.05 mmol) in CH2Cl2 (15 mL) at 0° C. was added NEt3 (0.85 mL, 6.15 mmol) and methanesulfonyl chloride (0.19 mL, 2.45 mmol). The mixture was stirred for 30 min at 25° C. then NaN3 (0.27 g, 4.1 mmol) in DMF (3 mL) was added. The reaction was stirred for 18 hr then partitioned between EtOAc and saturated NaHCO3 solution. The organic layer was washed with brine and dried (MgSO4) Filtration and concentration to dryness gave the title compound.

1. stirringThe reaction was stirred for 18 hr
2. customthen partitioned between EtOAc and saturated NaHCO3 solution
3. washThe organic layer was washed with brine
4. customdried
5. filtration(MgSO4) Filtration and concentration to dryness