One-pot synthesis of dihydropyrimidines via eco-friendly phosphorus derivatives catalysis |
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Affiliation: | 1. Department of Chemical and Biochemical Sciences - Green Process Engineering (CBS-GPE), Mohammed VI Polytechnic University (UM6P), Ben Guerir, Morocco;2. Institut de Chimie de Nice UMR7272, Université Côte d’Azur, CNRS, Nice, France |
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Abstract: | A straightforward, cost effective and eco-friendly protocol for the Biginelli reaction relying on the use of readily available hypophosphorous acid is presented. The methodology developed displays improvements compared to existing methods, is high-yielding, robust and was applied to a panel of dihydropyrimidines and thio-derivatives with various substituents. Related urea derivatives such as guanidines, benzimidazoles and benzothiazoles also reacted efficiently to afford more complex scaffolds. Thus, this rapid and convenient catalysis allows access to a wide diversity of structures including original biologically relevant heterocycles. |
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Keywords: | Phosphate derivatives catalysis Biginelli reaction Dihydropyrimidines One-pot protocol Fused heterocycles |
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