Application examples of 6-bromo-4-methylpyridine-3-carbonitrile_Industrial additives

Background and overview of application examples of 6-bromo-4-methylpyridine-3-carbonitrile

6-Bromo-4-methylpyridine-3-carbonitrile is a pharmaceutical intermediate. There are reports in the literature that it can be used to prepare PDE4 inhibitors and ROMK channel inhibitors from fluorophenylboronic acid.

Application examples of 6-bromo-4-methylpyridine-3-carbonitrile

Application examples of 6-bromo-4-methylpyridine-3-carbonitrile Application 1.

6-Bromo-4-methylpyridine-3-carbonitrile can be used to prepare phenylpyrrolidine compounds with the following structure. This type of compound is a compound that effectively inhibits PDE4. Phosphodiesterase (abbreviated as PDE), also known as 3′,5′-cyclic nucleotide phosphodiesterase, can catalyze the hydrolysis reaction of cAMP (cyclic adenosine monophosphate) to generate 5′-AMP (5′ -adenosine monophosphate), or catalyze the hydrolysis reaction of cGMP (cyclic guanosine monophosphate) di-tert-butyl dicarbonate to generate 5′-GMP (5′-guanosine monophosphate). Eleven phosphodiesterases have been identified so far, among which PDE4, PDE7 and PDE8 are specific for cAMP. PDE4 is the most important regulator of cAMP expressed on immune and inflammatory cells such as neutrophils, macrophages and T-lymphocytes. cAMP is a key second messenger in regulating the inflammatory response, and it has been reported that PDE4 can also regulate the inflammatory response of inflammatory cells by regulating pro-inflammatory cytokines such as TNFα, IL-2, IFN-γ, GM-CSF, and LTB4. By inhibiting PDE4, asthma, chronic obstructive pulmonary disease (COPD), rheumatoid arthritis, atopic dermatitis, inflammatory bowel diseases such as Crohn’s disease, and atopic dermatitis (AD) can be effectively treated. and other inflammatory diseases.

Application examples of 6-bromo-4-methylpyridine-3-carbonitrile Application 2.

6-Bromo-4-methylpyridine-3-carbonitrile can prepare substituted nitrogen-containing heterocyclic compounds used as inhibitors of ROMK channel activity. Several lines of evidence indicate that inhibition of ROMK channel activity causes natriuresis, diuresis, and lowering of blood pressure. Therefore, ROMK inhibition may provide novel mechanisms of blood pressure regulation and diuresis in patients with hypertension, congestive heart failure, or any other edematous disease condition.

References

[1] [Chinese invention] CN201911303362.7 Phenylpyrrolidine compounds and their uses

[2] [Invented in China] CN201880035414.4 Substituted nitrogen-containing compounds