Synthesis, SAR study, and biological evaluation of novel quinoline derivatives as phosphodiesterase 10A inhibitors with reduced CYP3A4 inhibition was written by Hamaguchi, Wataru;Masuda, Naoyuki;Miyamoto, Satoshi;Shiina, Yasuhiro;Kikuchi, Shigetoshi;Mihara, Takuma;Moriguchi, Hiroyuki;Fushiki, Hiroshi;Murakami, Yoshihiro;Amano, Yasushi;Honbou, Kazuya;Hattori, Kouji. And the article was included in Bioorganic & Medicinal Chemistry in 2015.COA of Formula: C9H16O3 This article mentions the following:
A novel class of phosphodiesterase 10A inhibitors with potent PDE10A inhibitory activity and reduced CYP3A4 inhibition was designed and synthesized starting from I. Replacement of pyridine ring of I with N-Me pyridone ring drastically improved CYP3A4 inhibition, and further optimization of these quinoline analogs identified compound II, which showed potent PDE10A inhibitory activity and a good CYP3A4 inhibition profile. A PET study with 11C-labeled II indicated that II exhibited good brain penetration and specifically accumulated in the rodent striatum. Further, oral administration of II dose-dependently attenuated phencyclidine-induced hyperlocomotion in mice with an ED50 value of 2.0 mg/kg and improved visual-recognition memory impairment at 0.1 and 0.3 mg/kg in mice novel object recognition test. In the experiment, the researchers used many compounds, for example, Ethyl 2-(tetrahydro-2H-pyran-4-yl)acetate (cas: 103260-44-2COA of Formula: C9H16O3).
Ethyl 2-(tetrahydro-2H-pyran-4-yl)acetate (cas: 103260-44-2) belongs to tetrahydropyran derivatives. Tetrahydropyrans are also used as important solvents, as chemical intermediate and as monomer for ring-opening polymerization. One classic procedure for the organic synthesis of tetrahydropyran is by hydrogenation of the 3,4-isomer of dihydropyran with Raney nickel.COA of Formula: C9H16O3
Referemce:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics