Tetrahydrofuran → (2R)-4-(1-(Diphenylmethyl)azetidin-3-yl)-1,2-dimethylpiperazine

Participants

Reaction Conditions

Reaction Steps

To a mixed solution of tert-butyl(2R)-4-(1-(diphenylmethyl)azetidin-3-yl)-2-methylpiperazine-1-carboxylate (476 mg, 1.13 mmol) described in Production Example 5-1 and THF (10.0 mL) was added lithium aluminum hydride (171 mg, 4.52 mmol) at 0° C., and the resultant mixture was stirred under reflux for 1 hour and 55 minutes. The reaction mixture was cooled to 0° C., water (171 μL) and a 5 N aqueous sodium hydroxide solution (171 μL) were added thereto, and water (513 μL) was additionally added thereto. The reaction mixture was filtrated using Celite and then washed with ethyl acetate. A filtrate was concentrated under a reduced pressure and the resultant residue was purified by NH silica gel column chromatography (heptane:ethyl acetate=2:1) to give the title compound (342 mg, yield: 90%).

Provenance & Evidence