79923-70-9

Upstream product

• 141-97-9 ethyl acetoacetate 
• 95-54-5 1,2-diamino-benzene 
• 7647-01-0 hydrogenchloride 

Downstream Products

• 615-15-6 2-Methyl-1H-benzimidazole 
• 141-97-9 ethyl acetoacetate 
• 1542552-89-5 ethyl 2-(3-bromothiophen-2-yl)-4-methyl-2,5-dihydro-1,5-benzodiazepine-3-carboxylate 
• 141-78-6 ethyl acetate 

Relevant academic research and scientific papers

One-pot synthesis of 1,5-benzodiazepine-2,3-dicarboxylates via three-component domino reactions in the presence of γ-Fe2O3@SiO2/Ce(OTf)3

[Figure not available: see fulltext.] Novel, efficient and environmentally friendly approaches have been developed for the synthesis of 1,5-benzodiazepine-2,3-dicarboxylates by one-pot three-component domino reactions in the presence of a catalytic amount

Expedient green-chemistry approaches for a one-pot synthesis of two series of novel 1,5-benzodiazepines: Via domino reactions

Unique green-chemistry approaches have been developed for the one-pot synthesis of two series of novel 1,5-benzodiazepines 4 and 5. The CeCl3-KI promoted two-component domino reaction of 1,2-phenylenediamines with 1,3-acetonedicarboxylate in ethanol affor

Efficient Synthesis and Biological Evaluation of a Novel Series of 1,5-Benzodiazepine Derivatives as Potential Antimicrobial Agents

A series of novel 1,5-benzodiazepine derivatives were rationally designed and synthesized following the principle of the superposition of bioactive substructures by the combination of 1,5-benzodiazepine, pyridine (phenyl), and an ester group. The structur

1,5-Benzodiazepine derivatives as potential antimicrobial agents: Design, synthesis, biological evaluation, and structure-activity relationships

36 Novel 1,5-benzodiazepine derivatives were rationally designed and synthesized according to the principle of superposition of bioactive substructures by the combination of 1,5-benzodiazepines, thiophene or thiazole and ester group. The structures of the target compounds have been characterized by IR, 1H NMR, 13C NMR, MS and elemental analysis. The structure of 1v was further determined using X-ray single crystal diffraction. All synthesized 1,5-benzodiazepine derivatives were evaluated for their in vitro antimicrobial activity against C. neoformans, C. neoformans clinical isolates, C. albicans, E. coli and S. aureus. The bioactive assay results revealed that most of the 1,5-benzodiazepine derivatives exhibited considerable potency against all of the tested strains. In particular, compounds 1v and 1w (MIC: 2-6 μg mL-1, MFC: 10-14 μg mL-1) exhibited excellent antifungal activity and were found to be 32-64 and 9-12.8 times more potent than the reference drugs against C. neoformans, respectively. Moreover, compound 1v (MIC: 40 μg mL-1) displayed equipotent antibacterial activity against E. coli and S. aureus compared to the reference drugs. The most potent of the synthesized compounds 1v and 1w were further studied by evaluating their cytotoxicities, and the results showed that they had relatively low level cytotoxicity for BV2 cell. A preliminary study of the structure-activity relationship revealed that substituents in the phenyl ring and the thiophene ring had a great effect on the antimicrobial activity of these compounds. In addition, the thiazole ring at C2 may be a pharmacophore of these compounds and COOC2H5 group at C3 is the best substituent for the maintenance of antimicrobial activities at low concentrations (1.5625 μg per disc).

B2O3/Al2O3 as a new, highly efficient and reusable heterogeneous catalyst for the selective synthesis of β-enamino ketones and esters under solvent-free conditions

Boron oxide adsorbed on alumina (B2O3/Al 2O3) has been found to be a new and highly efficient heterogeneous catalyst for the synthesis of β-enamino ketones and esters by the enamination of various primary and secondary amines with β-dicarbonyl compounds under solvent-free conditions. The important features of this methodology are broad substrate scope, high yield, no requirement of metal catalysts, high regio-and chemoselectivity and environmental friendliness. In addition, the catalyst could be recovered easily after the reactions and reused without evident loss of reactivity.