57045-35-9

Upstream product

• 541-73-1 1,3-Dichlorobenzene 
• 2234-16-4 1-(2,4-dichlorophenyl)ethan-1-one 
• 298-12-4 Glyoxilic acid 
• 6000-59-5 glyoxalic acid monohydrate 

Downstream Products

• 1253518-24-9 3-cyano-6-(2,4-dichlorophenyl)-2-methylisonicotinic acid 
• 78874-16-5 1-(2,4-dichloro-phenyl)-propane-1,2-dione 
• 78874-18-7 2-(2,4-Dichloro-phenyl)-2-hydroxy-propionic acid 
• 78874-27-8 3-(2,4-dichlorophenyl)-1H-pyrazole-5-carboxylic acid 
• 78874-31-4 3-(2,4-dichlorophenyl)-5-isoxazolylcarboxylic acid 
• 78874-21-2 5-(2,4-Dichloro-phenyl)-4-hydroxy-3,4-dihydro-2H-pyrazole-3-carboxylic acid 
• 78868-19-6 2-Bromo-4-(2,4-dichloro-phenyl)-3-hydroxy-4-oxo-butyric acid 
• 78874-29-0 5-(2,4-Dichloro-phenyl)-2-phenyl-2H-pyrazole-3-carboxylic acid 
• 78874-38-1 4-(2,4-Dichloro-phenyl)-2-diethylamino-3-hydroxy-4-oxo-butyric acid 
• 78874-44-9 2-Acetoxy-4-(2,4-dichloro-phenyl)-3-hydroxy-4-oxo-butyric acid 
• 78874-42-7 4-(2,4-Dichloro-phenyl)-3-hydroxy-4-oxo-2-piperidin-1-yl-butyric acid 
• 78874-23-4 5-(2,4-Dichloro-phenyl)-4-hydroxy-2-phenyl-3,4-dihydro-2H-pyrazole-3-carboxylic acid 
• 78874-33-6 4-(2,4-Dichloro-phenyl)-3-hydroxy-4-oxo-2-phenylamino-butyric acid 
• 78874-35-8 4-(2,4-Dichloro-phenyl)-3-hydroxy-4-oxo-2-p-tolylamino-butyric acid 

Relevant academic research and scientific papers

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.

Application of 4-oxo-2-crotonamide derivative to preparation of bacteriostatic agents

The invention discloses application of a 4-oxo-2-crotonamide derivative to preparation of bacteriostatic agents. The structure of the 4-oxo-2-crotonamide derivative is shown as a formula (I). The 4-oxo-2-crotonamide derivative has a bacteriostatic effect; good antibacterial activity can be realized on methicillin-resistant staphylococcus aureus, methicillin-resistant staphylococcus epidermidis, vancomycin drug-resistant enterococcus faecalis, vancomycin drug-resistant enterococcus faecium, methicillin-sensitive staphylococcus aureus, methicillin-sensitive staphylococcus epidermidis, vancomycin-sensitive enterococcus faecalis and vancomycin-sensitive enterococcus faecium. The formula I is shown in the description.

Substituted 4-oxo-crotonic acid derivatives as a new class of protein kinase B (PknB) inhibitors: synthesis and SAR study

Protein kinase B (PknB) is an essential serine/threonine protein kinase required for Mycobacterium tuberculosis (M. tb) cell division and cell-wall biosynthesis. A high throughput screen using PknB identified a (E)-4-oxo-crotonic acid inhibitor, named YH-8, which was used as a scaffold for SAR investigations. A significant improvement in enzyme affinity was achieved. The results indicated that the α,β-unsaturated ketone scaffold and “trans-” configuration are essential for the activity against PknB. And compounds with an aryl group, especially with electron-withdrawing substituents on benzene ring, exhibited four fold potency than that of YH-8.

Efficient synthesis of uracil-derived hexa- and tetrahydropyrido[2,3-d] pyrimidines

A reaction of 6-amino-1,3-dimethyluracil with 3-(hetero)aroylacrylic acids and their methyl esters leads to hexahydropyrido[2,3-d]pyrimidine-5-carboxylic acids or the corresponding methyl esters in high to excellent yields. One-pot oxidation of the acid d

A simple, diversity oriented synthesis of highly substituted pyridines

Figure represented. A particularly straightforward and efficient protocol for the synthesis of highly substituted pyridines, based on a condensation reaction of β-aminocrotonitrile and easily accessible (E)-2-oxo-4-aryl-but- 3-enoic acids and (E)-4-oxo-4-

CoA adducts of 4-oxo-4-phenylbut-2-enoates: Inhibitors of MenB from the M. tuberculosis menaquinone biosynthesis pathway

A high-throughput screen led to the discovery of 2-amino-4-oxo-4- phenylbutanoate inhibitors of the 1,4-dihydroxy-2-naphthoyl-CoA synthase (MenB) from the menaquinone biosynthesis pathway in Mycobacterium tuberculosis. However, these compounds are unstabl