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Citation
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HERO ID
1628738
Reference Type
Journal Article
Title
An efficient two-step synthesis of 3-amino-1-benzhydrylazetidine
Author(s)
Li, B; Witt, MF; Brandt, TA; Whritenour, D
Year
2006
Issue
7
Page Numbers
478-480
Web of Science Id
WOS:000239612800020
Abstract
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 similar to 70 degrees C. The procedure afforded the titled compound as mono acetate salt in 72-84% yield.
Keywords
azetidine; aminolysis; mesylation; 3-amino-1-azetidine; 1-benzhydrylazetidine
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