175357-73-0

Upstream product

• 106-37-6 1.4-dibromobenzene 
• 2393-23-9 4-methoxy-benzylamine 
• 15485-23-1 N-(4-methoxybenzylidene)-4-bromoaniline 
• 123-11-5 4-methoxy-benzaldehyde 
• 106-40-1 4-bromo-aniline 
• 105-13-5 4-Methoxybenzyl alcohol 
• 824-94-2 p-methoxybenzyl chloride 

Downstream Products

• 1134192-48-5 N-(4-bromophenyl)-2-cyano-N-(4-methoxybenzyl)acetamide 
• 15485-23-1 N-(4-methoxybenzylidene)-4-bromoaniline 

Relevant academic research and scientific papers

Design, synthesis and evaluation of novel bis-substituted aromatic amide dithiocarbamate derivatives as colchicine site tubulin polymerization inhibitors with potent anticancer activities

As the continuation of our work on the development of tubulin inhibitors with potential anticancer activities, novel bis-substituted aromatic amide dithiocarbamate derivatives were designed by contacting bis-substituted aryl scaffolds (potential anti-tubulin fragments) with N-containing heterocycles (potential anti-tubulin fragments) in one hybrid using the anticancer dithioformate unit as the linker. The antiproliferative activity against three digestive tract tumor cells was evaluated and preliminary structure activity relationships were summarized. Among these compounds, compound 20q exhibited most potent antiproliferative activity against MGC-803, HCT-116, Kyse30 and Kyse450 cells with IC50 values of 0.084, 0.227, 0.069 and 0.078 μM, respectively. In further studies, compound 20q was identified as a novel tubulin inhibitor targeting the colchicine binding site. Compound 20q could inhibit the microtubule assembly and disrupt cytoskeleton in Kyse30 and Kyse450 cells. The results of molecular docking suggested that compound 20q could tightly bind into the colchicine binding site of tubulin by hydrogen bonds and hydrophobic interactions. Compound 20q dose-dependently inhibited the cell growth and colony formation, effectively arrested cells at the G2/M phase and induce mitochondrial apoptosis in Kyse30 and Kyse450 cells. In addition, Compound 20q could regulate the expression of G2/M phase and mitochondrial apoptosis related proteins. Collectively, compound 20q was here reported as a novel tubulin inhibitor with potential anticancer activities.

Formation of 3-Aminophenols from Cyclohexane-1,3-diones

meta-Aminophenols are formed by the action of DBU on 3-amino-2-chlorocyclohex-2-en-1-ones at room temperature in MeCN. The chloro compounds are generated by treating 3-aminocyclohex-2-en-1-ones with the easily prepared halogenating agent BnNMe3·ICl2 in Me

Chromium-Catalyzed Alkylation of Amines by Alcohols

The alkylation of amines by alcohols is a broadly applicable, sustainable, and selective method for the synthesis of alkyl amines, which are important bulk and fine chemicals, pharmaceuticals, and agrochemicals. We show that Cr complexes can catalyze this C?N bond formation reaction. We synthesized and isolated 35 examples of alkylated amines, including 13 previously undisclosed products, and the use of amino alcohols as alkylating agents was demonstrated. The catalyst tolerates numerous functional groups, including hydrogenation-sensitive examples. Compared to many other alcohol-based amine alkylation methods, where a stoichiometric amount of base is required, our Cr-based catalyst system gives yields higher than 90 % for various alkyl amines with a catalytic amount of base. Our study indicates that Cr complexes can catalyze borrowing hydrogen or hydrogen autotransfer reactions and could thus be an alternative to Fe, Co, and Mn, or noble metals in (de)hydrogenation catalysis.

One-pot stepwise reductive amination reaction by N-coordinate sulfonamido-functionalized Ru(II) complexes in water

New complexes of formula [RuCl(p-cymene)(L)] (7–12) were prepared with [RuCl2(p-cymene)]2 and pre-synthesized N-arenesulfonly-o-phenylenediamines (1–6) and characterized using 1H NMR, 13C NMR, Fourier transform

PURINE INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA

The instant invention provides compounds of formula (I) which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflamation, asthma, COPD and cancer.

NaBH4/PhCO2H: An efficient system for reductive amination of aldehydes

NaBH4/PhCO2H system has been used for thereductive aminationofa varietyof aldehydes withanilines. The reductive amination reactions have been performed within 60-120 min in THFunder reflux conditionsin high to excellent yields of products (85-95%).

Reductive amination of aldehydes by NaBH4 in the presence of NaH2PO4.H2O

Thereductive aminationofa variety of aldehydes withanilines has been carried out by NaBH4/NaH2PO4.H2O as new reducing systemswithin 55-100 min in THFunder reflux conditionsin high to excellent yields of products (85-92%).

NaBH4/C: A convenient system for reductive amination of aldehydes

In this context, NaBH4 in the presence of activated charcoal has been used for thereductive aminationofa variety of aldehydes withanilines. Tne reductive amination reactions have been performed within 60-100 min in THFunder reflux conditionsin high to excellent yields of products (85-90%).

Efficient and chemoselective direct reductive amination of aromatic aldehydes catalyzed by oxo-rhenium complexes containing heterocyclic ligands

This work describes the catalytic activity of 17 oxo-rhenium complexes containing heterocyclic ligands in the direct reductive amination of 4-nitrobenzaldehyde with 4-chloroaniline, using phenylsilane as reducing agent. In general, all of the catalysts tested gave excellent yields of the secondary amine, although, the best result was obtained with the catalytic system PhSiH3/ReOBr2(Hhmpbta)(PPh3) (2.5 mol %). This system was also applied to the synthesis of a large variety of secondary amines in good to excellent yields and tertiary amines in moderate yields, with tolerance of different functional groups.

In(OTf)3 catalyzed N-benzylation of amines utilizing benzyl alcohols in water

An In(OTf)3-catalyzed N-benzylation of amines utilizing benzyl alcohols through direct C-O bond activation has been reported. The reaction was performed in water without any base, additive, ligand or inert gas protection to afford the chem-selective mono- or bis-alkylated aromatic amines in good to excellent yields.