173991-06-5

Upstream product

• 28611-39-4 4-(dimethylamino)benzene-boronic acid 
• 1122-91-4 4-bromo-benzaldehyde 
• 14047-29-1 4-carboxyphenylboronic acid 
• 586-77-6 4-bromo-N,N-dimethylaniline 
• 87199-17-5 4-formylphenylboronic acid, 
• 171364-78-6 (4-(N,N-dimethylamino)phenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane 
• 15164-44-0 p-(iodophenyl)carboxaldehyde 
• 624-38-4 para-diiodobenzene 
• 179055-26-6 (4-{[methoxy(methyl)amino]carbonyl}phenyl)boronic acid 
• 179055-23-3 N-methoxy-N-methyl-4-(4-dimethylaminophenyl)benzamide 

Relevant academic research and scientific papers

Highly efficient color filter using fluorescent materials, (Z)-3-(4'-(dimethylamino)biphenyl-4-yl)-2-phenylacrylonitrile

The transmittance and color characteristics of color filters are directly related to the energy efficiency and image quality of LCD panels. We tried to investigate the effect of fluorescent dyes, (Z)-3-(4'-(dimethylamino)biphenyl-4- yl)-2-phenylacrylonitr

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, o

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.

Palladium(II) chalcogenolate complexes as catalysts for CC cross-coupling and carbonylative Suzuki coupling reactions

The catalytic activity of palladium chalcogenolate complexes, [PdCl(ECH2CH2NMe2)]3 (E = S or Se), [PdCl(ECH2CH2CH2NMe2)]2 and [PdCl(SeCH2CH2NMe2)(PPh3)] has been investigated in carbonylative Suzuki coupling reactions. The phosphine complex has also been used as a catalyst in CC cross coupling reactions involving an aryl halide and either triaryl bismuth or aryl boronic acid (Suzuki coupling). The catalytic system was also explored for other carbonylation reactions including carbonylative Sonogashira coupling and amino carbonylation reaction. The phosphine complex showed better activity in carbonylative Suzuki coupling reactions than dimeric and trimeric complexes. All the complexes showed comparable activity in Suzuki coupling reactions.

Design of donor-acceptor geometry for tuning excited-state polarization: Fluorescence solvatochromism of push-pull biphenyls with various torsional restrictions on their aryl-aryl bonds

In this work, push-pull biphenyl analogs (4-(N,N-dimethylamino)-4′-formylbiphenyl) with a modulated dihedral angle of the aryl-aryl bond, using a bridged structure or methyl groups, were synthesized. Photophysical measurements of the synthesized compounds revealed the effect of the torsion between N,N-dimethylaniline (donor) and benzaldehyde moieties (acceptor) on their solvatochromic properties. Our data showed that the sensitivity of the fluorescence maxima to solvent polarity gradually increases as the biphenyl chromophore was restricted to a twisted conformation. This finding indicates that changing the torsional restrictions on the donor-acceptor system can be a factor to take into account for the development of novel solvatochromic dyes.

Palladium nanoparticles supported on carbon nanotubes from solventless preparations: Versatile catalysts for ligand-free Suzuki cross coupling reactions

Palladium nanoparticles supported on single- or multi-walled carbon nanotubes (Pd/SWCNT and Pd/MWCNT) were prepared by a rapid, solventless method that does not require reducing agents or electric current. The method involves a straightforward process using dry mixing of a precursor Pd salt (e.g., palladium acetate) with carbon nanotubes at ambient temperature by ball-milling (mechanochemical route) or with subsequent annealing at 300°C (thermal route) in an inert atmosphere. The Pd/MWCNT sample with Pd nanoparticle size of 1-3 nm and uniform dispersion prepared by mechanochemical ball-milling at room temperature [designated as (Pd/MWCNT)M] displayed remarkable catalytic activity towards Suzuki cross coupling reactions with a high turn over number (TON) of 7250 and turn over frequency (TOF) of 217-500 h-1. These nanoparticles were characterized by a variety of techniques including transmission electron microscopy (TEM), X-ray diffraction (XRD) and X-ray photoelectron spectroscopy (XPS). Additionally, the (Pd/MWCNT)M sample was successfully employed in Suzuki cross coupling reactions with a wide variety of functionalized substrates.

N,N′-Dibutylbarbituric acid as an acceptor moiety in push-pull chromophores

Twelve novel D-π-A chromophores with the N,N′-dibutylbarbituric acid acceptor, the N,N-dimethylamino donor and a systematically extended π-linker were synthesized. The extent of intramolecular charge-transfer, structure-property relationships and nonlinear optical properties were further investigated by X-ray analysis, electrochemistry, UV/Vis absorption spectra, calculations and EFISH experiments.

Synthesis, biological evaluation, and molecular modeling studies of methylene imidazole substituted biaryls as inhibitors of human 17α-hydroxylase-17,20-lyase (CYP17)-Part II: Core rigidification and influence of substituents at the methylene bridge

Thirty-five novel substituted imidazolyl methylene biphenyls have been synthesized as CYP17 inhibitors for the potential treatment of prostate cancer. Their activities have been tested with recombinant human CYP17 expressed in Escherichia coli. Promising compounds were tested for selectivity against CYP11B1, CYP11B2, and hepatic CYP enzymes 3A4, 1A2, 2B6 and 2D6. The core rigidified compounds (30-35) were the most active ones, being much more potent than Ketoconazole and reaching the activity of Abiraterone. However, they were not very selective. Another rather potent and more selective inhibitor (compound 23, IC50 = 345 nM) was further examined in rats regarding plasma testosterone levels and pharmacokinetic properties. Compared to the reference Abiraterone, 23 was more active in vivo, showed a longer plasma half-life (10 h) and a higher bioavailability. Using our CYP17 homology protein model, docking studies with selected compounds were performed to study possible interactions between inhibitors and amino acid residues of the active site.

PIPERIDINES USEFUL FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS

The invention relates to compounds which are substituted chiral or achiral derivatives of 3- or 4- aminopiperidine of the general formula (I). The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of general formula I and especially their use as inhibitors of β-secretases.