817618-57-8

Upstream product

• 57598-34-2 3-Bromo-N-tert-butoxycarbonyl-N-methylaniline 
• 73183-34-3 bis(pinacol)diborane 
• 28131-24-0 tert-butyl N-methyl-N-(phenyl)carbamate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 100-61-8 N-methylaniline 
• 330793-09-4 tert-butyl N-[3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolane-2-yl)phenyl]carbamate 
• 74-88-4 methyl iodide 

Downstream Products

• 817618-56-7 tert-butyl [3-(5-formylpyrid-2-yl)phenyl]methylcarbamate 
• 887831-90-5 (3-((tert-butoxycarbonyl)(methyl)amino)phenyl)boronic acid 

Relevant academic research and scientific papers

Improvement of Cell Permeability of Human Neuronal Nitric Oxide Synthase Inhibitors Using Potent and Selective 2-Aminopyridine-Based Scaffolds with a Fluorobenzene Linker

Inhibition of neuronal nitric oxide synthase (nNOS) is a promising therapeutic approach to treat neurodegenerative diseases. Recently, we have achieved considerable progress in improving the potency and isoform selectivity of human nNOS inhibitors bearing a 2-aminopyridine scaffold. However, these inhibitors still suffered from too low cell membrane permeability to enter into CNS drug development. We report herein our studies to improve permeability of nNOS inhibitors as measured by both PAMPA-BBB and Caco-2 assays. The most permeable compound (12) in this study still preserves excellent potency with human nNOS (Ki = 30 nM) and very high selectivity over other NOS isoforms, especially human eNOS (hnNOS/heNOS = 2799, the highest hnNOS/heNOS ratio we have obtained to date). X-ray crystallographic analysis reveals that 12 adopts a similar binding mode in both rat and human nNOS, in which the 2-aminopyridine and the fluorobenzene linker form crucial hydrogen bonds with glutamate and tyrosine residues, respectively.

Amide Effects in C?H Activation: Noncovalent Interactions with L-Shaped Ligand for meta Borylation of Aromatic Amides

A new concept for the meta-selective borylation of aromatic amides is described. It has been demonstrated that while esters gave para borylations, amides lead to meta borylations. For achieving high meta selectivity, an L-shaped bifunctional ligand has been employed and engages in an O???K noncovalent interaction with the oxygen atom of the moderately distorted amide carbonyl group. This interaction provides exceptional control for meta C?H activation/borylation.

NOVEL BIAROMATIC COMPOUNDS THAT MODULATE PPAR-RECEPTORS

Novel biaromatic compounds that modulate peroxisome proliferator-activator receptors, known as PPAR, having the formula (I): are formulated into pharmaceutical compositions useful in human or veterinary medicine, or alternatively, in cosmetic compositions.

NOVEL COMPOUNDS THAT MODULATE PPARγ TYPE RECEPTORS, AND USE THEREOF IN COSMETIC OR PHARMACEUTICAL COMPOSITIONS

The invention relates to novel compounds corresponding to the general formula (I) below: (I) and also to the method for preparing them, and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism),-or alternatively in cosmetic compositions.