反应详情

3-Fluoro-4-((3R)-3-hydroxy-1-pyrrolidinyl)nitrobenzene (35.8 g, 0.158 M) was dissolved in DMF (200 ml), and treated with imidazole (21.6 g, 0.318 M) and t-butyldimethylsilyl chloride (35.7 g, 0.239 M) and stirred for 18 hours at ambient temperature under nitrogen. Solvent was evaporated, and the residue treated with EtOAc (300 ml) and water (200 ml). The organic layer was washed with water (150 ml) and dried (magnesium sulfate). Evaporation gave the desired product (54 g), of sufficient quality for use without purification.

1. customSolvent was evaporated
2. additionthe residue treated with EtOAc (300 ml) and water (200 ml)
3. washThe organic layer was washed with water (150 ml)
4. dry with materialdried (magnesium sulfate)
5. customEvaporation