ORGN 553 |
| A streamlined process for the synthesis of 3-amino-1-benzhydrylazetidine is described. Commercially available 1-benzhydrylazetidin-3-ol was reacted with methanesulfonyl chloride in the presence of triethylamine in acetonitrile, upon quench with water, the mesylate intermediate (3) was isolated by filtration. The wet filter cake was subsequently treated with ammonium hydroxide/isopropanol in a Parr reactor at ~70°C. The procedure afforded the titled compound as mono acetate salt in 72 – 84% yield. |
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New Reactions and Methodology, Heterocycles and Aromatics, Bioorganic Chemistry
8:00 PM-10:00 PM, Tuesday, 12 September 2006 Moscone Center -- Hall D, Poster
Division of Organic Chemistry |