反应详情

To an anhydrous DMF (5 mL) solution of 3-aminobicyclo[1.1.1]pentan-1-yl acetate (1 mmol; prepared as described in Example 1, Step 2) is added potassium carbonate (3 mmol) followed by the addition of methyl iodide (1 mmol) by syringe at r.t. The reaction is monitored by LCMS and TLC. After consumption of starting material, the reaction mixture is quenched by adding water (3 mL) and extracted with ethyl acetate (3×). The organic layers are combined, dried (magnesium sulfate), filtered, and concentrated. The crude residue is subjected to flash chromatography (silica gel, EtOAc/hexanes) to afford 3-(methylamino)bicyclo[1.1.1]pentan-1-yl acetate.

1. customAfter consumption of starting material
2. customthe reaction mixture is quenched
3. additionby adding water (3 mL)
4. extractionextracted with ethyl acetate (3×)
5. dry with materialdried (magnesium sulfate)
6. filtrationfiltered
7. concentrationconcentrated