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Synlett 2014; 25(10): 1443-1447
DOI: 10.1055/s-0033-1341258
DOI: 10.1055/s-0033-1341258
letter
Synthesis and Early ADME Evaluation of a Novel Scaffold, Tetrahydro-6H-pyrido[3,2-b]azepin-6-one
Authors
Weitere Informationen
Publikationsverlauf
Received: 14. März 2014
Accepted after revision: 27. März 2014
Publikationsdatum:
12. Mai 2014 (online)
Abstract
The synthesis and preliminary ADME evaluation of novel 4-(trifluoromethyl)-5,7,8,9-tetrahydro-6H-pyrido[3,2-b]azepin-6-ones is presented. The key step is a ring expansion of 4-(trifluoromethyl)-7,8-dihydroquinolin-5(6H)-ones via a Beckmann rearrangement. The rearrangement opens up possibilities to access novel unexplored scaffolds for medicinal chemistry. The biopharmaceutical profiling revealed a strong structural dependency of the druglike properties.
Supporting Information
- for this article is available online at http://www.thieme-connect.com/products/ejournals/journal/
10.1055/s-00000083.
- Supporting Information (PDF)
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References and Notes
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