Synthesis of 1-phenyl-3, 4-dihydropyrimidine-2(1H)-ones derivatives under solvent free condition and their antimicrobial activity

Abstract

We report herein the use of nickel nitrate hexahydrate [Ni(NO3)2.6H2O] as a new catalyst for the one-pot Biginelli like reaction coupling of 1-phenyl thiourea, ethyl acetoacetate and aromatic aldehydes to afford the corresponding 1-phenyl-3,4-dihydropyrimidin-2(1H)-thiones under solvent free condition to avoid the usage of hazardous organic solvents. The synthesized compounds were evaluated for their antimicrobial activity by KIRBY-BAUER disk diffusion method. Most of the compounds showed good to moderate antimicrobial activity.
 Bangladesh J. Sci. Ind. Res.54(1), 47-54, 2019

Catalytic role in Biginelli reaction: Synthesis and biological property studies of 2‐oxo/thioxo‐1,2,3,4‐tetrahydropyrimidines

“…Most of the produced compounds showed good to moderate antibacterial activity against Bacillus cereus using the Kirby‐Bauer disc‐diffusion method. [ 77 ] Rathod et al described a newer finding route of 2‐thioxo‐1,2,3,4‐tetrahydropyrimidines derivatives with antibacterial properties against S. aureus , Bacillus subtilis , Salmonella typhi , and E. coli and antifungal activities against Aspergillus niger , Aspergillus flavus , Penicillium chrysogenum , and Candida albicans . The different substituted 3,4‐dihydropyridine derivatives were synthesized using triphenylphosphine as a catalyst by Michel Lewis base‐catalyzed one‐pot Biginelli type reaction under solvent‐free conditions.…”

“…Most of the produced compounds showed good to moderate antibacterial activity against Bacillus cereus using the Kirby-Bauer disc-diffusion method. [77] Rathod against both E. coli and S. aureus. [79] Babar independently reported a unique process for the synthesis of substituted dihydropyrimidinones/thiones derivatives under solvent-free conditions using red organic clay as a catalyst.…”

A convenient approach to synthesize substituted 5-Arylidene-3-m-tolyl thiazolidine-2, 4-diones by using morpholine as a catalyst and its theoretical study

“…Hence, a facile efficient process is still desirable. As a continuation our research goal to develop a convenient method to synthesize valuable synthon [33][34][35][36] from easily available starting materials, we developed a two-step method to synthesize thiazolidine-2,4-dione derivatives by using morpholine as a catalyst. We have performed Density functional theory (DFT) calculations in all our synthesized molecules to find out most active compound.…”