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One-Pot Synthesis of 2-Substituted 4-Aryl-4,5-dihydro-3,1-benzoxazepines from 2-(2-Aminophenyl)-1-arylethanols via Dehydration of the Corresponding Amides

โœ Scribed by Shuhei Fukamachi; Hisatoshi Konishi; Kazuhiro Kobayashi

Publisher
John Wiley and Sons
Year
2011
Tongue
German
Weight
149 KB
Volume
94
Category
Article
ISSN
0018-019X

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โœฆ Synopsis

An efficient method for the preparation of 2-substituted 4-aryl-4,5-dihydro-3,1-benzoxazepine derivatives under mild conditions has been developed. The reaction of 2-(2-aminophenyl)ethanols 1 with acid chlorides in the presence of excess Et 3 N in THF at room temperature gave the corresponding Nacylated intermediates 2, which were dehydrated by treatment with POCl 3 to give 2-substituted 4-aryl-4,5-dihydro-3,1-benzoxazepines 3 in a one-pot reaction.

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