763133-86-4

Upstream product

• 19350-70-0 2-methoxybenzaldehyde p-toluenesulfonylhydrazone 
• 536-74-3 phenylacetylene 
• 135-02-4 ortho-anisaldehyde 
• 1456785-12-8 3-amino-3-(2-methoxylphenyl)-1-phenylprop-2-en-1-one 
• 5416-70-6 2-methoxychalcone 
• 767-91-9 1-ethynyl-2-methoxybenzene 
• 98-88-4 benzoyl chloride 
• 129972-89-0 3-(2-methoxyphenyl)-1-phenylprop-2-yn-1-one 
• 579-74-8 2-Methoxyacetophenone 
• 100-52-7 benzaldehyde 
• 40524-62-7 1-(2-methoxyphenyl)-3-phenyl-2-propene-1-one 

Relevant academic research and scientific papers

A Convenient One-Pot Synthesis of Chalcones and Their Derivatives and Their Antimicrobial Activity

Abstract: A series of chalcones were synthesized by base-catalyzed Clasien-Schmidtcondensation of substituted benzaldehydes and substituted acetophenones at roomtemperature. The addition of hydrazine hydrate and hydroxylamine hydrochlorideacross the double bond of the obtained chalcones gave pyrazole and isoxazolederivatives, respectively. All the synthesized compounds were characterized by1H and 13C NMR andFT-IR spectroscopy and screened for their in vitro antimicrobial activityagainst two bacterial strains, Pseudomonasaeruginosa and Pseudomonasoryzihabitans using Ciprofloxacin as standard drug.1-(2-Methoxyphenyl)-3-phenylprop-2-en-1-one and1-(4-chlorophenyl)-3-phenylprop-2-en-1-one showed significant activity againstboth bacterial strains and hence proved to be potent antimicrobialagents.

Decoupling Activation of Heme Biosynthesis from Anaerobic Toxicity in a Molecule Active in Staphylococcus aureus

Small molecules active in the pathogenic bacterium Staphylococcus aureus are valuable tools for the study of its basic biology and pathogenesis, and many molecules may provide leads for novel therapeutics. We have previously reported a small molecule, 1, which activates endogenous heme biosynthesis in S. aureus, leading to an accumulation of intracellular heme. In addition to this novel activity, 1 also exhibits toxicity towards S. aureus growing under fermentative conditions. To determine if these activities are linked and establish what features of the molecule are required for activity, we synthesized a library of analogs around the structure of 1 and screened them for activation of heme biosynthesis and anaerobic toxicity to investigate structure-activity relationships. The results of this analysis suggest that these activities are not linked. Furthermore, we have identified the structural features that promote each activity and have established two classes of molecules: activators of heme biosynthesis and inhibitors of anaerobic growth. These molecules will serve as useful probes for their respective activities without concern for the off target effects of the parent compound.

A facile and expeditious approach to substituted 1H-pyrazoles catalyzed by iodine

A facile and expeditious method for the synthesis of 1H-pyrazoles by the reaction of α,β-unsaturated aldehydes/ketones and sulfonyl hydrazide catalyzed by as low as 2 mol % I2 has been demonstrated. This synthetic system features simple operation and mild reaction conditions, and displays a broad functional group tolerance furnishing good to excellent yields.

Copper on iron promoted one-pot synthesis of β-aminoenones and 3,5-disubstituted pyrazoles

The reaction of hydroximoyl chlorides with acetylenes in the presence of a copper on iron bimetallic system leads to β-aminoenones via reductive ring opening of isoxazole intermediates. The valuable β-aminoenone building blocks can be isolated or transformed into pyrazoles with the addition of hydrazine in a straightforward one-pot procedure.

An efficient one-pot synthesis of 3,5-disubstituted 1H-pyrazoles

An efficient, general, one-pot, three-component procedure for the preparation of 3,5-disubstituted 1H-pyrazoles via condensation of substituted aromatic aldehydes, tosylhydrazine and terminal alkynes in toluene is reported. The reaction tolerates a variety of functional groups and sterically hindered substrates to afford the desired pyrazoles in yields of 67-91%.