Acetic Acid → N-benzyl-3-pyrrolidinol

Participants

Reaction Steps

When 960 mg of acetic acid (16 mmol) was added to a solution in ethyl acetate (30 mL) of 3.6146 g of crude (R)-1-benzyl-3-aminopyrrolidine produced in the step 1-1 (14.6 mmol, optical purity: 92.4% e.e., including 29.5% by weight 1-benzyl-3-pyrrolidinol, and 0.8% by weight 1-benzyl-2,5-dihydro-1H-pyrrole as impurities), a crystal was precipitated. After stirring at 5° C. for 30 min, the crystal was filtrated under reduced pressure, which was washed with 20 mL of ethyl acetate, and thereafter vacuum drying was carried out to give a white crystal of 2.5804 g (yield: 75%, optical purity: 94.3% e.e., with no 1-benzyl-3-pyrrolidinol and 1-benzyl-2,5-dihydro-1H-pyrrole detected).

Provenance & Evidence