74939-78-9

Upstream product

• 2142-63-4 1-(3-Bromophenyl)ethanone 
• 298-12-4 Glyoxilic acid 
• 97961-06-3 2-hydroxy-4-(3'-bromophenyl)-4-oxo-butanoic acid 

Downstream Products

• 118540-39-9 2-acetylthio-3-(3-bromobenzoyl)propionic acid 
• 62902-65-2 6-(3-bromo-phenyl)-2H-pyridazin-3-one 
• 118540-53-7 4-acetylthio-3-(3-bromobenzoyl)butyric acid 
• 117808-92-1 3-(3-bromobenzoyl)-3-butenoic acid 
• 62903-13-3 4-(3-bromophenyl)-4-oxo-butyric acid 

Relevant academic research and scientific papers

Silver-Catalyzed Diastereoselective Synthesis of Spirocyclic Pyrrolidine-Lactones by 1,3-Dipolar Cycloaddition

The preparation of two enantiomerically enriched amino lactones as chiral starting substrates for asymmetric 1,3-dipolar cycloadditions is described. They act as precursors of the chiral imino lactones, which form in situ the corresponding azomethine ylides. They react with electrophilic alkenes under silver catalysis to afford spirolactone-pyrrolidines products. The sequential method consisting in one-pot imine formation → cycloaddition is optimized and compared with the multicomponent process. The scope of the reaction is studied as well as the stereochemical outcomes and the mechanistic details using DFT calculations and X-ray diffraction analysis.

Microwave-assisted synthesis of 4-oxo-2-butenoic acids by aldol-condensation of glyoxylic acid

4-Oxobutenoic acids are useful as biologically active species and as versatile intermediates for further derivatisation. Currently, routes to their synthesis can be problematic and lack generality. Reaction conditions for the synthesis of 4-oxo-2-butenoic

Irreversible inhibitors of the proline racemase unveil innovative mechanism of action as antibacterial agents against Clostridioides difficile

Proline racemases (PRAC), catalyzing the l-proline and d-proline interconversion, are essential factors in eukaryotic pathogens such as Trypanosoma cruzi, Trypanosoma vivax, and Clostridioides difficile. If the discovery of irreversible inhibitors of T.?cruzi PRAC (TcPRAC) led to innovative therapy of the Chagas disease, no inhibitors of CdPRAC have been discovered to date. However, C.?difficile, due to an increased incidence in recent years, is considered as a major cause of health threat. In this work, we have taken into account the similarity between TcPRAC and CdPRAC enzymes to design new inhibitors of CdPRAC. Starting from (E) 4-oxopent-2-enoic acid TcPRAC irreversible inhibitors, we synthesized 4-aryl substituted analogs and evaluated their CdPRAC enzymatic inhibition against eleven strains of C.?difficile. This study resulted in promising candidates and allowed for identification of (E)-4-(3-bromothiophen-2-yl)-4-oxobut-2-enoic acid 20 that was chosen for complementary in vivo studies and did not reveal in vivo toxicity.

Design, synthesis, and bioevaluation of a novel class of (E)-4-oxo-crotonamide derivatives as potent antituberculosis agents

A series of novel (E)-4-oxo-2-crotonamide derivatives were designed and synthesized to find potent antituberculosis agents. All the target compounds were evaluated for their in vitro activity against Mycobacterium tuberculosis H37Rv(MTB). Results reveal that 4-phenyl moiety at part A and short methyl group at part C were found to be favorable. Most of the derivatives displayed promising activity against MTB with MIC ranging from 0.125 to 4 μg/mL. Especially, compound IIIa16 was found to have the best activity with MIC of 0.125 μg/mL against MTB and with MIC in the range of 0.05–0.48 μg/mL against drug-resistant clinical MTB isolates.

Beta-carbonyl acrylamide compounds, preparation method and applications thereof

The invention provides beta-carbonyl acrylamide compounds, whose structure is shown by the formula (I). The compounds have an activity on preventing mycobacterium tuberculosis (including multi-drug resistant mycobacterium tuberculosis), and thus the compounds can be made into potential novel anti-tuberculosis drugs.

Arylalkane, arylalkene and aryl azaalkane, medicaments containing said compounds and method for the production thereof

The present invention relates to compounds of general formula [in-line-formulae]R—Z1—Z2—Z3—R1, ??(I)[/in-line-formulae] wherein R, R1 and Z1 to Z3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

4-phenyl-4-oxo-2-butenoic acid derivatives with kynurenine-3-hydroxylase inhibiting activity

PCT No. PCT/EP96/04517 Sec. 371 Date May 4, 1998 Sec. 102(e) Date May 4, 1998 PCT Filed Oct. 16, 1996 PCT Pub. No. WO97/17316 PCT Pub. Date May 15, 19974-Phenyl-4-oxo-butenoic acid derivatives for use in the treatment of the human or animal body by therapy; particularly as kynurenine-3-hydroxylase inhibitors, in the prevention and/or treatment of a neurodegenerative disease wherein the inhibition of such an enzyme is needed. The present invention further comprises a selected class of the above mentioned 4-phenyl-4-oxo-butenoic acid derivatives, their pharmaceutically acceptable salts, a process for their preparation and pharmaceutical compositions containing them.