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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