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Synthesis of Benzomorphan Analogues by Intramolecular Buchwald—Hartwig Cyclization.

✍ Scribed by Anton S. Khartulyari; Martin E. Maier


Publisher
John Wiley and Sons
Year
2007
Weight
19 KB
Volume
38
Category
Article
ISSN
0931-7597

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Synthesis of Benzomorphan Analogues by I
✍ Anton S. Khartulyari; Martin E. Maier 📂 Article 📅 2007 🏛 John Wiley and Sons 🌐 English ⚖ 181 KB

## Abstract A new strategy toward the important class of benzomorphans is described. The key bond formation is based on an intramolecular Buchwald–Hartwig enolate arylation reaction. Thus, alkylation of piperidones with __ortho__‐bromobenzyl bromides provides the necessary substrates. In the presen

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## Abstract The three‐step strategy involves reductive amination of aromatic aldehydes, addition of the resulting secondary amines to ethyl acrylate and final Buchwald—Hartwig cyclization.