51736-38-0

Upstream product

• 4584-46-7 (2-chloroethyl)dimethylamine hydrochloride 
• 88-75-5 2-hydroxynitrobenzene 
• 108-01-0 2-(N,N-dimethylamino)ethanol 
• 105-58-8 Diethyl carbonate 
• 1493-27-2 ortho-nitrofluorobenzene 
• 850895-60-2 2-(2-nitrophenoxy)-1-mesyloxyethane 
• 506-59-2 N,N-dimethylammonium chloride 

Downstream Products

• 1409968-66-6 C₂₆H₃₁FN₄O₂ 
• 1202-00-2 2-(2'-aminophenoxy)-1-(N,N-dimethylamino)-ethane 

Relevant academic research and scientific papers

Mustard Carbonate Analogues as Sustainable Reagents for the Aminoalkylation of Phenols

N,N-dialkyl ethylamine moiety can be found in numerous scaffolds of macromolecules, catalysts, and especially pharmaceuticals. Common synthetic procedures for its incorporation in a substrate relies on the use of a nitrogen mustard gas or on multistep syntheses featuring chlorine hazardous/toxic chemistry. Reported herein is a one-pot synthetic approach for the easy introduction of aminoalkyl chain into different phenolic substrates through dialkyl carbonate (β-aminocarbonate) chemistry. This new direct alcohol substitution avoids the use of chlorine chemistry, and it is efficient on numerous pharmacophore scaffolds with good to quantitative yield. The cytotoxicity via MTT of the β-aminocarbonate, key intermediate of this synthetic approach, was also evaluated and compared with its alcohol precursor.

COUMARIN DERIVATIVES AND METHODS OF USE IN TREATING CYSTIC FIBROSIS, CHRONIC OBSTRUCTIVE PULMONARY DISEASE, AND MISFOLDED PROTEIN DISORDERS

Novel CFTR corrector compounds that are effective in rescuing halide efflux, delF508-CFTR protein processing, and apical functional chloride ion transport in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cyst

COUMARIN DERIVATIVES AND METHODS OF USE IN TREATING HYPERPROLIFERATIVE DISEASES

Coumarin derivative compounds and methods for the treatment of hyperproliferative diseases, such as cancer, polycystic kidney disease, and fibrosis of different tissues (e.g., idiopathic pulmonary fibrosis), are provided. The methods include administering

Pyrrolidinyl phenylurea derivatives as novel CCR3 antagonists

Optimization starting with our lead compound 1 (IC50 = 4.9 nM) led to the identification of pyrrolidinyl phenylurea derivatives. Further modification toward improvement of the bioavailability provided (R)-1-(1-((6-fluoronaphthalen-2-yl)methyl)pyrrolidin-3-yl)-3-(2-(2- hydroxyethoxy)phenyl)urea 32 (IC50 = 1.7 nM), a potent and orally active CCR3 antagonist.

Method for arylating aza-heterocycles with activated aromatic compounds in the presence of caesium carbonate

The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of further catalysts at room temperature.

Diphenyl-substituted heterocycles, processes for preparing them and their use as pharmaceutical compositions

The invention relates to new diphenyl-substituted 5-ring heterocycles of general formula (I) wherein A, X and the groups R1, R2, R3, R4and R5are defined as in the claims, processes for preparing them