877133-54-5

Basic information

• Product Name: 4-Bromo-2,6-diethyl-pyridine
• Synonyms: 4-Bromo-2,6-diethyl-pyridine;Pyridine, 4-bromo-2,6-diethyl-
• CAS NO: 877133-54-5
• Molecular Formula: C9H12BrN
• Molecular Weight: 214.105
• Mol File: 877133-54-5.mol
• Article Data: 5

Chemical Properties

• Boiling Point: 243 °C at 760 mmHg
• Flash Point: 100.8 °C
• Appearance: /
• Density: 1.301g/cm³
• Vapor Pressure: 0.0512mmHg at 25°C
• Refractive Index: 1.534
• Storage Temp.: under inert gas (nitrogen or Argon) at 2-8°C
• CAS DataBase Reference: 4-Bromo-2,6-diethyl-pyridine(CAS DataBase Reference)
• NIST Chemistry Reference: 4-Bromo-2,6-diethyl-pyridine(877133-54-5)
• EPA Substance Registry System: 4-Bromo-2,6-diethyl-pyridine(877133-54-5)

Safety Data

• Hazardous Substances Data: 877133-54-5(Hazardous Substances Data)

Usage

Uses

4-Bromo-2,6-diethylpyridine is a useful reactant for the synthesis of PF-?00868554 (I)?, an HCV polymerase inhibitor.

InChI:InChI=1/C9H12BrN/c1-3-8-5-7(10)6-9(4-2)11-8/h5-6H,3-4H2,1-2H3

Upstream product

• 1115035-61-4 2,6-diethylpyridin-4-ol 
• 1035267-63-0 4-bromo-2,6-diethyIpyridine 1-oxide 
• 542-05-2 acetonedicarboxylic acid 
• 123-62-6 propionic acid anhydride 

Downstream Products

• 1228897-37-7 C₂₆H₃₃NO₃ 
• 1228897-38-8 C₁₇H₂₃NO 
• 37581-44-5 2,6-Diethyl-4-cyanopyridin 

Relevant articles and documents

A New Fluorogenic Small-Molecule Labeling Tool for Surface Diffusion Analysis and Advanced Fluorescence Imaging of β-Site Amyloid Precursor Protein-Cleaving Enzyme 1 Based on Silicone Rhodamine: SiR-BACE1

β-site APP-cleaving enzyme 1 (BACE1) is a major player in the pathogenesis of Alzheimer's disease. Structural and functional fluorescence microscopy offers a powerful approach to learn about the physiology and pathophysiology of this protease. Up to now, however, common labeling techniques require genetic manipulation, use large antibodies, or are not compatible with live cell imaging. Fluorescent small molecules that specifically bind to the protein of interest can overcome these limitations. Herein, we introduce SiR-BACE1, a conjugate of the BACE1 inhibitor S-39 and SiR647, as a novel fluorogenic, tag-free, and antibody-free label for BACE1. We present its chemical development, characterize its photophysical and pharmacologic properties, and evaluate its behavior in solution, in overexpression systems, and in native brain tissue. We demonstrate its applicability in confocal, stimulated emission depletion and dynamic single-molecule microscopy. The first functional studies with SiR-BACE1 on the surface mobility of BACE1 revealed a markedly confined diffusion pattern.

Di-substituted pyridinyl aminohydantoins as potent and highly selective human β-secretase (BACE1) inhibitors

The identification of highly selective small molecule di-substituted pyridinyl aminohydantoins as β-secretase inhibitors is reported. The more potent and selective analogs demonstrate low nanomolar potency for the BACE1 enzyme as measured in a FRET assay, and exhibit comparable activity in a cell-based (ELISA) assay. In addition, these pyridine-aminohydantoins are highly selectivity (>500×) against the other structurally related aspartyl proteases BACE2, cathepsin D, pepsin and renin. Our design strategy followed a traditional SAR approach and was supported by molecular modeling studies based on the previously reported aminohydantoin 3a. We have taken advantage of the amino acid difference between the BACE1 and BACE2 at the S2′ pocket (BACE1 Pro70 changed to BACE2 Lys86) to build ligands with >500-fold selectivity against BACE2. The addition of large substituents on the targeted ligand at the vicinity of this aberration has generated a steric conflict between the ligand and these two proteins, thus impacting the ligand's affinity and selectivity. These ligands have also shown an exceptional selectivity against cathepsin D (>5000-fold) as well as the other aspartyl proteases mentioned. One of the more potent compounds (S)-39 displayed an IC50 value for BACE1 of 10 nM, and exhibited cellular activity with an EC50 value of 130 nM in the ELISA assay.

NOVEL 2-AMINO-5, 5-DIARYL-IMIDAZOL-4-ONES

This invention relates to novel compounds having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.