反应详情

温度

0 °C

To a stirred, cooled (0° C.) solution (RS)-(3-amino-2-oxo-2H-pyridin-1-yl)-ethoxy-acetic acid ethyl ester (428 mg) and 2,4,6-collidine (0.47 ml) in THF (3 ml) under an argon atmosphere was added dropwise a solution of alpha-toluenesulphonylchloride (340 mg) in THF (2 ml) over 10 min. When addition was complete, stirring at 0° C. was continued for 2 h. The mixture was diluted with EtOAc, washed with 1.0 N HCl and brine, dried (MgSO4), filtered and concentrated to give (RS)-ethoxy-(2-oxo-3-phenylmethanesulfonylamino-2H-pyridin-1-yl)-acetic acid ethyl ester (592 mg) as light brown solid. MS 393.0 ([M−H]−)

1. additionWhen addition
2. washwashed with 1.0 N HCl and brine
3. dry with materialdried (MgSO4)
4. filtrationfiltered
5. concentrationconcentrated