Exploring Novel Silyl-Phosphonite Chemistry and New Bioisosteres

Phosphinic acids are valuable synthetic targets which have many industrial applications. Most notably they have displayed biological activity as herbicides, and as pharmaceutical drugs for the treatment of a range of diseases. Herein, we report a novel P-C bond formation reaction for the synthesis o...

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Main Author: Wheeler, D F
Format: Thesis (University of Nottingham only)
Language:English
English
Published: 2020
Subjects:
Online Access:https://eprints.nottingham.ac.uk/59944/
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author Wheeler, D F
author_facet Wheeler, D F
author_sort Wheeler, D F
building Nottingham Research Data Repository
collection Online Access
description Phosphinic acids are valuable synthetic targets which have many industrial applications. Most notably they have displayed biological activity as herbicides, and as pharmaceutical drugs for the treatment of a range of diseases. Herein, we report a novel P-C bond formation reaction for the synthesis of secondary phosphinic acids. This method is underpinned by the generation of a nucleophilic silylphosphonite intermediate via an unprecedented B(C6F5)3-catalysed silylation of primary phosphinic acids. A proposed mechanism for this transformation has been reported, and the scope of the reaction has been explored, with 20 secondary phosphinic acids being synthesised in 44 - 96% yield. Furthermore, the functionalisation of these phosphinic acids has allowed the synthesis of 8 Pstereogenic tertiary phosphine oxides. The outlined strategy constitutes a controlled route to tertiary phosphine oxides, which avoids PCl3 and other halophosphines.
first_indexed 2025-11-14T21:03:29Z
format Thesis (University of Nottingham only)
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institution University of Nottingham Malaysia Campus
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language English
English
last_indexed 2025-11-14T21:03:29Z
publishDate 2020
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spelling nottingham-599442025-08-11T09:45:41Z https://eprints.nottingham.ac.uk/59944/ Exploring Novel Silyl-Phosphonite Chemistry and New Bioisosteres Wheeler, D F Phosphinic acids are valuable synthetic targets which have many industrial applications. Most notably they have displayed biological activity as herbicides, and as pharmaceutical drugs for the treatment of a range of diseases. Herein, we report a novel P-C bond formation reaction for the synthesis of secondary phosphinic acids. This method is underpinned by the generation of a nucleophilic silylphosphonite intermediate via an unprecedented B(C6F5)3-catalysed silylation of primary phosphinic acids. A proposed mechanism for this transformation has been reported, and the scope of the reaction has been explored, with 20 secondary phosphinic acids being synthesised in 44 - 96% yield. Furthermore, the functionalisation of these phosphinic acids has allowed the synthesis of 8 Pstereogenic tertiary phosphine oxides. The outlined strategy constitutes a controlled route to tertiary phosphine oxides, which avoids PCl3 and other halophosphines. 2020-07-24 Thesis (University of Nottingham only) NonPeerReviewed application/pdf en arr https://eprints.nottingham.ac.uk/59944/1/Exploring%20Novel%20Silyl-Phosphonite%20Chemistry%20and%20New%20Bioisosteres%20-%20Part%201.pdf application/pdf en arr https://eprints.nottingham.ac.uk/59944/2/Exploring%20Novel%20Silyl-Phosphonite%20Chemistry%20and%20New%20Bioisosteres%20-%20Part%202.pdf Wheeler, D F (2020) Exploring Novel Silyl-Phosphonite Chemistry and New Bioisosteres. PhD thesis, University of Nottingham. Phosphinic acids organometallics
spellingShingle Phosphinic acids
organometallics
Wheeler, D F
Exploring Novel Silyl-Phosphonite Chemistry and New Bioisosteres
title Exploring Novel Silyl-Phosphonite Chemistry and New Bioisosteres
title_full Exploring Novel Silyl-Phosphonite Chemistry and New Bioisosteres
title_fullStr Exploring Novel Silyl-Phosphonite Chemistry and New Bioisosteres
title_full_unstemmed Exploring Novel Silyl-Phosphonite Chemistry and New Bioisosteres
title_short Exploring Novel Silyl-Phosphonite Chemistry and New Bioisosteres
title_sort exploring novel silyl-phosphonite chemistry and new bioisosteres
topic Phosphinic acids
organometallics
url https://eprints.nottingham.ac.uk/59944/