Benzyl 3-((3S)-3,4-dimethylpiperazin-1-yl)azetidine-1-carboxylate → (S)-4-(Azetidin-3-YL)-1,2-dimethylpiperazine

Participants

Reaction Steps

To a mixed solution of benzyl 3-((3S)-3,4-dimethylpiperazin-1-yl)azetidine-1-carboxylate (28.6 g, 94.3 mmol) described in Production Example 4-2 and methanol (150 mL) was added 10% palladium-carbon (50% aqueous, 10.0 g) at room temperature. The resultant mixture was stirred under a hydrogen atmosphere at room temperature and at 0.35 MPa to 0.40 MPa for 1 hour and 45 minutes. The reaction mixture was purged with a nitrogen atmosphere, and then filtrated using Celite. A filtrate was concentrated under a reduced pressure to give the title compound (21.2 g, yield: quantitative). The product was used in the subsequent reaction without further purification.

Provenance & Evidence