Novel benzimidazole derivatives as phosphodiesterase 10A (PDE10A) inhibitors with improved metabolic stability was written by Chino, Ayaka;Masuda, Naoyuki;Amano, Yasushi;Honbou, Kazuya;Mihara, Takuma;Yamazaki, Mayako;Tomishima, Masaki. And the article was included in Bioorganic & Medicinal Chemistry in 2014.Application In Synthesis of 2-Chloro-4-methoxy-3-nitropyridine This article mentions the following:
In this study, we report the identification of potent benzimidazoles as PDE10A inhibitors. We first identified imidazopyridine 1 as a high-throughput screening hit compound from an inhouse library. Next, optimization of the imidazopyridine moiety to improve inhibitory activity gave imidazopyridinone 10b. Following further structure-activity relationship development by reducing lipophilicity and introducing substituents, we acquired 35, which exhibited both improved metabolic stability and reduced CYP3A4 time-dependent inhibition. In the experiment, the researchers used many compounds, for example, 2-Chloro-4-methoxy-3-nitropyridine (cas: 6980-09-2Application In Synthesis of 2-Chloro-4-methoxy-3-nitropyridine).
2-Chloro-4-methoxy-3-nitropyridine (cas: 6980-09-2) belongs to pyridine derivatives. The ring atoms in the pyridine molecule are sp2-hybridized. The nitrogen is involved in the π-bonding aromatic system using its unhybridized p orbital. The lone pair is in an sp2 orbital, projecting outward from the ring in the same plane as the σ bonds. Reduced pyridines, namely tetrahydropyridines, dihydropyridines and piperidines, are found in numerous natural and synthetic compounds. The synthesis and reactivity of these compounds have often been driven by the fact many of these compounds have interesting and unique pharmacological properties. Application In Synthesis of 2-Chloro-4-methoxy-3-nitropyridine