One-pot synthesis of dihydropyrimidines via eco-friendly phosphorus derivatives catalysis

Journal of Saudi Chemical Society

Cyril Ronco¹  Zakaria Moutaoukil²  Rachid Benhida³ 

[1] Institut de Chimie de Nice UMR7272, Université Côte d’Azur, CNRS, Nice, France;Department of Chemical and Biochemical Sciences - Green Process Engineering (CBS-GPE), Mohammed VI Polytechnic University (UM6P), Ben Guerir, Morocco;Institut de Chimie de Nice UMR7272, Université Côte d’Azur, CNRS, Nice, France;

关键词: Phosphate derivatives catalysis;    Biginelli reaction;    Dihydropyrimidines;    One-pot protocol;    Fused heterocycles;   

DOI  :  

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown