Seven-membered ring scaffolds for drug discovery: access to functionalised azepanes and oxepanes through diazocarbonyl chemistry

Functionalised azepane and oxepane scaffolds were prepared using diazocarbonyl chemistry and elaborated to show their potential use in library synthesis. Key dicarbonyl containing seven-membered rings were functionalised via diastereoselective Luche reduction of the ketone followed by manipulation o...

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Main Authors: Nortcliffe, Andrew, Moody, Christopher J.
Format: Article
Published: Elsevier 2015
Subjects:
Online Access:https://eprints.nottingham.ac.uk/30957/
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author Nortcliffe, Andrew
Moody, Christopher J.
author_facet Nortcliffe, Andrew
Moody, Christopher J.
author_sort Nortcliffe, Andrew
building Nottingham Research Data Repository
collection Online Access
description Functionalised azepane and oxepane scaffolds were prepared using diazocarbonyl chemistry and elaborated to show their potential use in library synthesis. Key dicarbonyl containing seven-membered rings were functionalised via diastereoselective Luche reduction of the ketone followed by manipulation of the ester and amine groups. Further scaffolds could be accessed by C-alkylation of the dicarbonyl compounds. In addition, an oxepane containing amino acid could be prepared via a diastereoselective enamine reduction.
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spelling nottingham-309572020-05-04T17:01:06Z https://eprints.nottingham.ac.uk/30957/ Seven-membered ring scaffolds for drug discovery: access to functionalised azepanes and oxepanes through diazocarbonyl chemistry Nortcliffe, Andrew Moody, Christopher J. Functionalised azepane and oxepane scaffolds were prepared using diazocarbonyl chemistry and elaborated to show their potential use in library synthesis. Key dicarbonyl containing seven-membered rings were functionalised via diastereoselective Luche reduction of the ketone followed by manipulation of the ester and amine groups. Further scaffolds could be accessed by C-alkylation of the dicarbonyl compounds. In addition, an oxepane containing amino acid could be prepared via a diastereoselective enamine reduction. Elsevier 2015-01-13 Article PeerReviewed Nortcliffe, Andrew and Moody, Christopher J. (2015) Seven-membered ring scaffolds for drug discovery: access to functionalised azepanes and oxepanes through diazocarbonyl chemistry. Bioorganic and Medicinal Chemistry, 23 (11). pp. 2730-2735. ISSN 1464-3391 Seven-Membered Rings Azepane Oxepane Diazocarbonyl Medicinal Chemistry http://dx.doi.org/10.1016/j.bmc.2015.01.010 doi:10.1016/j.bmc.2015.01.010 doi:10.1016/j.bmc.2015.01.010
spellingShingle Seven-Membered Rings
Azepane
Oxepane
Diazocarbonyl
Medicinal Chemistry
Nortcliffe, Andrew
Moody, Christopher J.
Seven-membered ring scaffolds for drug discovery: access to functionalised azepanes and oxepanes through diazocarbonyl chemistry
title Seven-membered ring scaffolds for drug discovery: access to functionalised azepanes and oxepanes through diazocarbonyl chemistry
title_full Seven-membered ring scaffolds for drug discovery: access to functionalised azepanes and oxepanes through diazocarbonyl chemistry
title_fullStr Seven-membered ring scaffolds for drug discovery: access to functionalised azepanes and oxepanes through diazocarbonyl chemistry
title_full_unstemmed Seven-membered ring scaffolds for drug discovery: access to functionalised azepanes and oxepanes through diazocarbonyl chemistry
title_short Seven-membered ring scaffolds for drug discovery: access to functionalised azepanes and oxepanes through diazocarbonyl chemistry
title_sort seven-membered ring scaffolds for drug discovery: access to functionalised azepanes and oxepanes through diazocarbonyl chemistry
topic Seven-Membered Rings
Azepane
Oxepane
Diazocarbonyl
Medicinal Chemistry
url https://eprints.nottingham.ac.uk/30957/
https://eprints.nottingham.ac.uk/30957/
https://eprints.nottingham.ac.uk/30957/