1214337-82-2

Usage

Uses

Used in Pharmaceutical Industry:
Ethyl 5-bromo-6-methoxypicolinate is used as an intermediate in the synthesis of various pharmaceuticals, contributing to the development of new drugs and improving existing ones.
Used in Agrochemical Industry:
Ethyl 5-bromo-6-methoxypicolinate is used as a building block in the production of insecticides, fungicides, and herbicides, helping to create more effective and safer agrochemicals for agricultural applications.
Used in Organic Synthesis:
Ethyl 5-bromo-6-methoxypicolinate is utilized in organic synthesis for the preparation of various organic compounds, expanding the scope of chemical reactions and syntheses.
Used in Medicinal Chemistry Research:
Ethyl 5-bromo-6-methoxypicolinate is employed in medicinal chemistry research to explore its potential applications and properties, contributing to the advancement of drug discovery and development.

Upstream product

• 1256823-65-0 5-bromo-6-chloropyridine-2-carbonitrile 
• 64-17-5 ethanol 
• 1373126-39-6 3-bromo-2-chloropyridine 1-oxide 
• 52200-48-3 3-bromo-2-chloropyridine 
• 717843-47-5 3-bromo-2-methoxy-6-methylpyridine 
• 185017-72-5 3-bromo-2-chloro-6-methyl pyridine 
• 1214334-70-9 5-bromo-6-methoxypyridine-2-carboxylic acid 

Downstream Products

• 1373126-40-9 ethyl 5-(5,5-dimethyl-1,3,2-dioxaborinan-2-yl)-6-methoxypyridine-2-carboxylate 

Relevant academic research and scientific papers

Novel S1P1 receptor agonists - Part 5: From amino-to alkoxy-pyridines

In a previous communication we reported on the discovery of aminopyridine 1 as a potent, selective and orally active S1P1 receptor agonist. More detailed studies revealed that this compound is phototoxic in vitro. As a result of efforts aiming at eliminating this undesired property, a series of alkoxy substituted pyridine derivatives was discovered. The photo irritancy factor (PIF) of these alkoxy pyridines was significantly lower than the one of aminopyridine 1 and most compounds were not phototoxic. Focused SAR studies showed, that 2-, 3-, and 4-pyridine derivatives delivered highly potent S1P1 receptor agonists. While the 2-pyridines were clearly more selective against S1PR3, the corresponding 3- or 4-pyridine analogues showed significantly longer oral half-lives and as a consequence longer pharmacological duration of action after oral administration. One of the best compounds, cyclopentoxy-pyridine 45b lacked phototoxicity, showed EC50 values of 0.7 and 140 nM on S1PR1 and S1PR3, respectively, and maximally reduced the blood lymphocyte count for at least 24 h after oral administration of 10 mg/kg to Wistar rats.

Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active γ-secretase modulators

We report the discovery and optimization of a novel series of dihydrobenzofuran amides as γ-secretase modulators (GSMs). Strategies for aligning in vitro potency with drug-like physicochemical properties and good microsomal stability while avoiding P-gp mediated efflux are discussed. Lead compounds such as 35 and 43 have moderate to good in vitro potency and excellent selectivity against Notch. Good oral bioavailability was achieved as well as robust brain Aβ42 lowering activity at 100 mg/kg po dose.

NOVEL HETEROARYL IMIDAZOLES AND HETEROARYL TRIAZOLES AS GAMMA-SECRETASE MODULATORS

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I; (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.