21262-08-8

Upstream product

• 19103-79-8 2-chloro-propionyl isothiocyanate 
• 106-40-1 4-bromo-aniline 
• 7623-09-8 2-chloropropionyl chloride 
• 103-88-8 4-bromoacetanilide 
• 21262-52-2 2-chloro-N-phenylpropanamide 

Downstream Products

• 868771-26-0 N-(4-bromo-2-nitro-phenyl)-2-chloro-propionamide 
• 868771-37-3 N-(2-amino-4-bromo-phenyl)-2-chloro-propionamide 
• 24463-25-0 6-bromo-3-methyl-3,4-dihydro-1H-quinoxalin-2-one 

Relevant academic research and scientific papers

Optimization of bifunctional piperidinamide derivatives as σ1R Antagonists/MOR agonists for treating neuropathic pain

Here, we describe the optimization, synthesis, and associated pharmacological analgesic activities of a new series of bifunctional piperidinamide derivatives as sigma-1 receptor (σ1R) antagonists and mu opioid receptor (MOR) agonists. The new compounds were evaluated in vitro in σ1R and MOR binding assays. The most promising compound 114 (also called HKC-126), showed superior affinities for σ1R and MOR and good selectivity to additional receptors related to pain. Compound 114 showed powerful dose-dependent analgesic effects in the acetic acid writhing test, formalin test, hot plate test, and chronic constriction injury (CCI) neuropathic pain model. In contrast to an equianalgesic dose of fentanyl, compound 114 produced fewer opioid-like side effects, such as reward liability, respiratory depression, physical dependence, and sedation. Lastly, the pharmacokinetic properties of this drug were also acceptable, and these results suggest that compound 114, as a mixed σ1R/MOR ligand, has potential for treating neuropathic pain.

Inhibitory Effects of New Mercapto Xanthine Derivatives in Human mcf7 and k562 Cancer Cell Lines

A series of new 2-methyl-2-[(1,3-Diethyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl)thio]-N- substituted arylacetamides were synthesized. The antitumor activity of these purine based compounds were evaluated on breast cancer (MCF7) and leukemic cancer (K562) cell lines via cell viability assay utilizing the tetrazolium dye 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT). These results were substantiated using computer docking experiments (LigandFit docking engine and PMF scoring function) which predict that the antitumor activity of these new compounds may be attributable to their abilities to effectively bind and block oncogenic tyrosine kinases, particularly bcr/abl.

Synthesis of substituted 1,3-dimethyl-1H-quinoxalin-2-ones from aniline derivatives

Substituted 1,3-dimethyl-1H-quinoxalin-2-ones (7) have been synthesized through the procedures of acylation, nitration, reduction, intramolecular alkylation, oxidation, and N-methylation starting from 3,4-disubstituted aniline.

Novel approach to 3-methyl-1H-quinoxalin-2-ones

A novel approach to the synthesis of 3-methyl-1H-quinoxalin-2-ones has been described. These compounds were regioselectively prepared by starting from substituted phenylamines and α-chloropropionyl chloride through the efficient procedures of acylation, nitration, reduction, intramolecular alkylation, and oxidation. Copyright Taylor & Francis, Inc.

AlCl3-Catalysed trans N-acylation of Acetanilides with α-Chloropropionyl Chloride

trans N-acylation of acetanilides with α-chloropropionyl chloride catalysed by AlCl3 has been shown to occur efficiently, affording 2-chloro-N-phenylpropanamides in preparative yields.

Catalytic Trans N-acylation of Anilides with α-Chloropropionyl Chloride over Zeolites

A mild and effective method of zeolite catalyzed trans N-acylation of anilides in liquid-phase is described.