51209-70-2

Upstream product

• 120-57-0 piperonal 
• 106-40-1 4-bromo-aniline 
• 495-76-1 piperonol 

Downstream Products

• 1017609-30-1 C₁₆H₁₂BrNO₃ 
• 64468-57-1 N-[2t-benzo[1,3]dioxol-5-yl-1-(4-bromo-phenyl)-4-oxo-azetidin-3r-yl]-phthalimide 

Relevant academic research and scientific papers

Arene diruthenium(II)-mediated synthesis of imines from alcohols and amines under aerobic condition

The utility and selectivity of the newly synthesized dinuclear arene Ru(II) complex were demonstrated towards the synthesis of imines from coupling of alcohols and amines in the aerobic condition. Analytical and various spectral methods have been used to establish the unprecedented formation of the new thiolato-bridged dinuclear ruthenium complex. The molecular structure of the titled complex was evidenced with aid of X-ray crystallographic technique. A wide range of imines were obtained in good-to-excellent yields up to 98% and water as the by-product through an acceptorless dehydrogenative coupling of alcohols with amines. The catalytic reaction operated a concise atom economical without any oxidant with 1 mol% of the catalyst load. Further, the role of base, solvent and catalyst loading of the coupling reaction has been investigated. A plausible mechanism has been described and was found to proceed via the formation of an aldehyde intermediate. Short synthesis of antibacterial drug N-(salicylidene)-2-hydroxyaniline illustrated the utility of the present protocol.

Design, synthesis and biological evaluation of imidazole and oxazole fragments as HIV-1 integrase-LEDGF/p75 disruptors and inhibitors of microbial pathogens

We describe here the synthesis of libraries of novel 1-subtituted-5-aryl-1H-imidazole, 5-aryl-4-tosyl-4,5-dihydro-1,3-oxazole and 5-aryl-1,3-oxazole fragments via microwave (MW)-assisted cycloaddition of para-toluenesulfonylmethyl isocyanide (TosMIC) to imines and aldehydes. The compounds obtained were biologically evaluated in an AlphaScreen HIV-1 IN-LEDGF/p75 inhibition assay with six imidazole-based compounds (16c, 16f, 17c, 17f, 20a and 20d) displaying more than 50% inhibition at 10 μM, with IC50 values ranging from 7.0 to 30.4 μM. Additionally the hypothesis model developed predicts all active scaffolds except 20d to occupy similar areas as the N-heterocyclic (A) moiety and two aromatic rings (B and C) of previously identified inhibitor 5. These results indicate that the identified compounds represent a viable starting point for their use as templates in the design of next generation inhibitors targeting the HIV-1 IN and LEDGF/p75 protein-protein interaction. In addition, the in vitro antimicrobial properties of these fragments were tested by minimum inhibitory concentration (MIC) assays showing that compound 16f exhibited a MIC value of 15.6 μg/ml against S. aureus, while 17f displayed a similar MIC value against B. cereus, suggesting that these compounds could be further developed to specifically target those microbial pathogens.

GREEN SYNTHESIS OF ARYL ALDIMINES USING ETHYL LACTATE

The present invention relates to a method for preparing aryl aldimines. In particular, the present invention relates to methods of preparing aryl aldimines that uses environmentally friendly solvent systems.

One - Pot Reformatsky-Imine addition reaction-leading to the synthesis of structurally diverse β-lactams

The Reformatsky-imine addition reaction of a-bromoethylacetate with aldimines derived from 3,4-methylenedioxy benzaldehyde and α- methylcinnamaldehyde has provided an efficient and practical access to structurally diverse β-lactams. All the new β-lactams