Efficient microwave enhanced solvent-free synthesis of potent antifungal agents: Fluorinated benzothiazepine fused β-lactam derivatives

A microwave enhanced, facile cycloaddition has been developed for the synthesis of fluorine containing azeto[2,1-d][1,5]benzothiazepine derivatives (Va–m) on the surface of potassium carbonate (K2CO3). Microwave enhanced solvent-free improved synthesis of required 1,5-benzothiazepines is also developed using montmorillonite clay. The synthesized compounds have been screened ‘in vitro’ for antifungal activity against Rhizoctonia solani, Fusarium oxysporum and Collectotrichum capsici. Most of the compounds have shown good activity against these pathogens.

Graphical abstractA rapid and efficient method is described for the synthesis of 2-chloro-2a-(substituted phenyl)-1-oxo-2,2a,3,4-tetrahydro-1H-azeto[2,1-d][1,5]benzothiazepine-carboxylic acids (Va–m) on the surface of potassium carbonate (K2CO3).Figure optionsDownload full-size imageDownload as PowerPoint slide