Multi-Component Reactions in the Preparation of α- and β- Substituted Phosphonates

Author(s): Mohamed S. Bekheit, Azza A. Kamel

Journal Name: Current Organic Chemistry

Volume 21 , Issue 10 , 2017

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Graphical Abstract:


Multi-component reactions (MCRs) constitute one of the most efficient tools in modern synthetic organic chemistry used for the preparation of highly functionalized organic compounds. They are excellent for the generation of libraries of small-molecule compounds and are indispensable for structure-activity relationship (SAR) studies. Some MCRs generate uncommon, if not unique, structures that have the ability to further modifications. Some MCRs are considered scaffolds in the biological realm and expected to be involved as scientists search for tomorrow’s remedies. They play an important role in organophosphorus chemistry where phosphorus reagents are used as substrates for synthesis of a wide range of heterocyclic phosphonates. Based on the diversity of structures that can be accessed by MCRs, this article presents an overview about multi-component reactions with particular emphasis on their role in preparation of α- and β-substituted phosphonates. The presented examples underline the greatest advantage of multi-component reactions to create diverse bioactive compounds from simple building blocks in only one step. These methodologies will have a bright future in drug design and synthesis.

Keywords: Multi-component reactions, one-pot reaction, Kabachnik-fields reaction, α-aminophosphonates, aminomethylene bisphosphonates, α-acetoxyphosphonates, α-oxycarbanilinophosphonates, β-phosphonomalononitriles.

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Article Details

Year: 2017
Published on: 29 March, 2017
Page: [923 - 938]
Pages: 16
DOI: 10.2174/1385272821666170113114456
Price: $58

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