51451-83-3

Upstream product

• 103-69-5 N-ethyl-N-phenylamine 
• 98-95-3 nitrobenzene 
• 836-30-6 4-ntrophenyl(phenyl)amine 
• 75-03-6 ethyl iodide 
• 3665-80-3 N-Ethyl-4-nitroanilin 
• 637-88-7 1,4-Cyclohexanedione 

Downstream Products

• 5543-89-5 (4-aminophenyl)ethylphenylamine 

Relevant academic research and scientific papers

One-way valveN-Preparation method of aryl substituted heterocyclic compound (by machine translation)

The invention relates to the technical field of organic chemical synthesis, in particular to an organic chemical synthesis technology. NThe preparation method comprises ?timetime?: 3 molar ratio, reaction 30 - 60 minutes at normal temperature and normal pressure, water adding quenching after reaction, organic solvent extraction 1:1-1 and column chromatography separation (V). Petroleum ether : VEthyl acetate =40:1 - 20:1). NAryl substituted heterocyclic derivatives. Nitrobenzene is used as Ar-H source. N-methylaniline. N-ethylaniline. N-methyl-heterocycles, tetrahydroquinoline, and the like can be used as the amine source. t- BuBuBuBuBuBuBuONa/DMSO/O2 In the system, a direct arylamine reaction of the aromatic ring is achieved. This process has the advantage that the process is simple and high in atomic economy, avoiding the use of expensive transition metals, mild reaction conditions, and environmental-friendly by-products. (by machine translation)

Synthesis and structure-activity relationships of trisubstituted phenyl urea derivatives as neuropeptide Y5 receptor antagonists

1-((1R,2R)-2-Hydroxy-1-methyl-2-phenylethyl)-1-methyl-3-(4-phenoxyphenyl)urea (1) was identified as a hit from the screening of the neuropeptide Y5 (NPY5) receptor. This lead was optimized for in vitro potency by changing the stereochemistry, the phenylethyl segment, the urea portion, and the 4-phenoxyphenyl group on the molecule. Over 40 analogues of 1 were prepared to study the structure-activity relationship for this series. The most potent compounds in this class have IC50S less than 0.1 nM at the NPY5 receptor (e.g., 40f, 44a, and 47). To determine the functional activity for this series of compounds, selected analogues were tested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptor. All urea analogues tested in the functional assay acted as antagonists (e.g., 1, 32, 40a, and 44e).

Condensations of 1,4-Cyclohexanediones and Secondary Aromatic Amines. The Formation of Alkyldiarylamines and Triarylamines

Condensation of 1,4-cyclohexanedione with N-alkylarylamines gives N-alkyl-N-arylanilines, and that with diarylamines gives triarylamines.A mechanism involving dehydration of monoenamines of the 1,4-dione is proposed for the reaction.Relative rates of substituted N-ethylanilines on competitive reactions plotted vs.Hammet's ? values gave -2.0 as the ρ value.In separate reactions, however, a different tendency is noted for the yield, that is, the ease of reactions with p-chloro and p-nitro derivatives.This discrepancy is explained in terms of acidities of the conjugate acids of the amines used as the actual catalysts.