反应详情

To a solution of (S)-3-hydroxypyrrolidine (1.84 g, 21 mmol) in DCM (10 mL) at 0° C. was added a solution of 1-(bromomethyl)-3-nitro-5-(trifluoromethyl)benzene (2.00 g, 7 mmol) in DCM (10 mL) dropwise. After the addition, the reaction mixture was allowed to stir at rt for 2 h and then diluted with DCM and washed with brine. Removal of solvent gave (3S)-1-[3-nitro-5-(trifluoromethyl)benzyl]pyrrolidin-3-ol (2.25 g, 100% yield) as yellow oil. LCMS: (FA) ES+ 291.3.Step 2: 3-[((3S)-3-{[tert-butyl(dimethyl)silyl]oxy}pyrrolidin-1-yl)methyl]-5-(trifluoromethyl)aniline

1. additionAfter the addition
2. washwashed with brine
3. customRemoval of solvent