Ammonia → (3R)-1-benzylpyrrolidin-3-amine

関与物質

反応手順

An autoclave was cooled with an acetone/dry ice bath, and an ammonia gas was blown to pool 477 cc of liquid ammonia (corresponding to 25 equivalent of (S)-1-benzyl-3-(methanesulfonyloxy)pyrrolidine). Thereto was added 180 g of (S)-1-benzyl-3-(methanesulfonyloxy)pyrrolidine (672.1 mmol, optical purity: 100% e.e.), which was heated to 100° C. whereby an internal pressure of 55 barr was observed. After allowing the reaction for 5 hrs, the reaction mixture was cooled to room temperature, and ammonia was removed by distillation under reduced pressure. As the residue, 306.7 g of a brown oily material was obtained (reaction yield: 88%, optical purity: 91.2% e.e.).

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