139944-56-2

Upstream product

• 90-04-0 2-methoxy-phenylamine 
• 107-08-4 1-iodo-propane 
• 91-23-6 2-Nitroanisole 
• 107-12-0 propiononitrile 
• 107-10-8 propylamine 
• 100-66-3 methoxybenzene 
• 303755-57-9 N-(2-methoxyphenyl)-2,4-dinitrobenzenesulfonamide 
• 921-01-7 rac-cysteine 

Downstream Products

• 83605-26-9 N-(2-Methoxy-phenyl)-N-propyl-propionamide 
• 83604-80-2 2-<4-(propionyloxy)-1-(2-chlorophenethyl)-4-piperidinyl>-N-(2-methoxyphenyl)-N-propylpropionamide 
• 83605-06-5 2-{1-[2-(2-Chloro-phenyl)-ethyl]-4-hydroxy-piperidin-4-yl}-N-(2-methoxy-phenyl)-N-propyl-propionamide 

Relevant academic research and scientific papers

Direct Aryl C?H Amination with Primary Amines Using Organic Photoredox Catalysis

The direct catalytic C?H amination of arenes is a powerful synthetic strategy with useful applications in pharmaceuticals, agrochemicals, and materials chemistry. Despite the advances in catalytic C?H functionalization, the use of aliphatic amine coupling partners is limited. Described herein is the construction of C?N bonds, using primary amines, by direct C?H functionalization with an acridinium photoredox catalyst under an aerobic atmosphere. A wide variety of primary amines, including amino acids and more complex amines are competent coupling partners. Various electron-rich aromatics and heteroaromatics are useful scaffolds in this reaction, as are complex, biologically active arenes. We also describe the ability to functionalize arenes that are not oxidized by an acridinium catalyst, such as benzene and toluene, thus supporting a reactive amine cation radical intermediate.

Thiol activated prodrugs of sulfur dioxide (SO2) as MRSA inhibitors

Drug resistant infections are becoming common worldwide and new strategies for drug development are necessary. Here, we report the synthesis and evaluation of 2,4-dinitrophenylsulfonamides, which are donors of sulfur dioxide (SO2), a reactive sulfur species, as methicillin-resistant Staphylococcus aureus (MRSA) inhibitors. N-(3-Methoxyphenyl)-2,4-dinitro-N-(prop-2-yn-1-yl)benzenesulfonamide (5e) was found to have excellent in vitro MRSA inhibitory potency. This compound is cell permeable and treatment of MRSA cells with 5e depleted intracellular thiols and enhanced oxidative species both results consistent with a mechanism involving thiol activation to produce SO2.

Reductive monoalkylation of aromatic and aliphatic nitro compounds and the corresponding amines with nitriles

(Chemical Equation Presented) A simple, selective, rapid, and efficient procedure for the synthesis of secondary amines from the reductive alkylation of either aliphatic or aromatic nitro compounds and the corresponding amines is reported. Ammonium formate is used as the hydrogen source and Pd/C as the hydrogen transfer catalyst. The reaction is carried out at room temperature. The rate differences for the preferential formation of secondary over tertiary products are due to both steric and electronic factors.

Aminothiazole derivatives, method of preparation and pharmaceutical compositions containing same

The subject of the invention is the compounds of formula: in which R1, R2, R3, R4, R5and R6are as defined in Claim1. The compounds have a high affinity for CRF receptors.