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Synopsis of recent synthetic methods and biological applications of phosphinic acid derivatives
The chemistry of phosphinic acid derivatives has attracted increasing attention in both synthetic organic and biological fields, and great progress in the application of such compounds has been achieved in recent years. This review aims to document a systematic account of the prevailing methods for the synthesis of acyclic/cyclic phosphinic acids either in enantiopure or in racemic form. The most important among them are Hirao cross-coupling reaction, Michael addition to olefins, Atherton?Todd reaction and Michaelis-Arbuzov reaction. Other noteworthy methods applied for this purpose are benzylation and allylation of hypophosphorous acid, hydrophosphinylation of aldehydes or alkenes and phosphorylation of strained P-heterocycles. Parallel synthetic methods leading to heterocyclic phosphinic acids such as phospholes, azaphospholidines, phosphorines, 1,2-oxaphosphorines, 1,3-azaphosphorines, 1,4,2-oxazaphosphinanes, phosphindoles, and benzazaphosphorines are also disclosed. Finally, selected significant applications in medicinal chemistry of the title compounds like Zn-metalloprotease Inhibitors, prodrug and drug applications are described briefly here. The bibliography includes 304 references.
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Reference£º
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method