反应详情

A solution of (1-Benzhydryl-azetidin-3-yl)-(4-chloro-phenyl)-methanone (19.8 g, 54.8 mmol) in dichloromethane (250 ml), cooled to −4° C., is treated with 1-chloroethylchloroformate (8.0 ml, 73.8 mmol) and allowed to warm to ambient temperature. The reaction mixture is stirred for 18 hours and then evaporated. The residue is dissolved in methanol (220 ml) and stirred at ambient temperature for 3.5 hours. The methanol solution is concentrated and the product precipitated by addition of diethylether. The precipitate is collected by filtration and dries under high vacuum to afford Azetidin-3-yl-(4-chloro-phenyl)-methanone hydrochloride. [MH]+ 195.95.

1. customevaporated
2. dissolutionThe residue is dissolved in methanol (220 ml)
3. stirringstirred at ambient temperature for 3.5 hours
4. concentrationThe methanol solution is concentrated
5. customthe product precipitated by addition of diethylether
6. filtrationThe precipitate is collected by filtration and dries under high vacuum