1256789-95-3

Usage

Uses

Used in Pharmaceutical Industry:
Methyl 5-bromo-4-methoxypyridine-2-carboxylate is used as a key intermediate in the synthesis of substituted Piperidinylpyridazinamines, which are TRPC6 inhibitors. These inhibitors are valuable for treating various diseases by modulating the activity of TRPC6 channels, which play a crucial role in cellular calcium signaling and are implicated in several pathological conditions.
Used in Agrochemical Industry:
Although not explicitly mentioned in the provided materials, methyl 5-bromo-4-methoxypyridine-2-carboxylate may also find applications in the agrochemical industry as a precursor for the development of new pesticides or other agrochemical products. Its unique structure and reactivity could be harnessed to create novel compounds with potential uses in agriculture, such as pest control or crop protection.

Upstream product

• 29681-43-4 methyl 4-methoxypicolinate 
• 5470-22-4 4-chloropicolinic acid 
• 886372-61-8 5-bromo-4-methoxy-2-methylpyridine 
• 67-56-1 methanol 

Relevant academic research and scientific papers

SUBSTITUTED PHENYLPROPENYL PYRIDINE DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL APPLICATIONS

Disclosed are a substituted phenylpropenylpyridine derivative, a preparation method therefor and the use thereof as a PD-1/PD-L1 inhibitor. In particular, disclosed are a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, a preparation method therefor and the use thereof. The definition of each group in the formula is detailed in the description and claims.

BIARYL DERIVATIVE, PREPARATION METHOD THEREOF AND PHARMACEUTICAL APPLICATION THEREOF

Disclosed are a biaryl derivative having a structure represented by Formula (I) and inhibitory activity against PD-1/PD-L1 interaction, a preparation method thereof, and a pharmaceutical application thereof. The series of compounds of the present inventio

Preparation and application of hydrochlorides of 5-cyano-4-methoxy-2-picolinic acid

The invention provides a preparation method of hydrochlorides of 5-cyano-4-methoxyl-2-picolinic acid. According to the preparation method, 5-bromo-4-methoxy-2-methylpyridin is used as raw materials to form 5-bromo-4-methoxyl-2-methyl picolinate sequentially through oxidation and esterification; under the catalysis effect of tetrakis(triphenylphosphine)palladium, the reaction is taken with nucleophilic reagents to obtain the 5-cyano-4-methoxyl-2-methyl picolinate; hydrolysis is performed to obtain 5-cyano-4-methoxy-2-picolinic acid; obtained 5-cyano-4-methoxy-2-picolinic acid reacts with acid to form salts. A novel synthesis path is provided by the invention; a prepared intermediate product of 5-cyano-4-methoxy-2-picolinic acid (H4) can take a reaction with hydrochloric acid under a conventional condition to obtain the hydrochlorides of the 5-cyano-4-methoxy-2-picolinic acid. The intermediate product of active compounds for preparing uretica, natruresis promoting medicine and valuable medicine for treating cardiovascular diseases and diseases due to retention of excessive salts and hydropexis.

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.