On October 4, 2012, Masuda, Naoyuki; Miyamoto, Satoshi; Kikuchi, Shigetoshi; Samizu, Kiyohiro; Sato, Fumie; Shiina, Yasuhiro; Hamaguchi, Wataru; Seo, Ryushi; Mihara, Takuma published a patent.Quality Control of 5-Chloroquinoxaline The title of the patent was Preparation of pyrazole compounds as inhibitors of phosphodiesterase 10A. And the patent contained the following:
The title compounds [I; ring A = (un)substituted aromatic heterocyclyl; B = phenylene, pyridinediyl, thiophenediyl, or CC each optionally substituted by ≥1 group selected from C1-6 alkyl, halo, C1-6 alkyloxy, and each (un)substituted cycloalkyl and nonaromatic heterocyclyl; n = 0, 1; L1 = C1-6 alkylene, C1-6 alkylene-T, T-C1-6 alkylene; provided that when n = 0, L1 = trimethylene-T or tetramethylene-T; T = O, S, NH, N(C1-6 alkyl); X = CR0, N; R0 = H, C1-6 alkyl; R1 = H or C1-6 alkyl optionally substituted by ≥1 group selected from halo, HO, C1-6 alkyloxy, cyano, CO2H, and CO2-C1-6 alkyl; ring E = each (un)substituted cycloalkyl, aryl, aromatic heterocyclyl, or nonaromatic heterocyclyl] or salts thereof were prepared These pyrazole compounds have phosphodiesterase 10A (PDE10A)-inhibitory actions, and can be used for the prevention of and/or as therapeutic agents for schizophrenia, anxiety, Huntington’s disease, drug dependence, and/or Alzheimer’s disease. Thus, amidation of 4-[[[1-methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl]oxy]methyl]benzoic acid with 1,2-phenylenediamine using 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride, 1-hydroxybenzotriazole, and Et4N in DMF at room temperature for 1 h followed by cyclization of the resulting amide under heating at 90° for 12 h and salt formation with HCl in EtOAc gave 2-[4-[[[1-methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl]oxy]methyl]phenyl]-1H-benzimidazole (II) dihydrochloride. II.2HCl and compound (III).2HCl showed IC50 of 17 and 0.4 nM, resp., against human PDE10A. The experimental process involved the reaction of 5-Chloroquinoxaline(cas: 62163-09-1).Quality Control of 5-Chloroquinoxaline
The Article related to pyrazole preparation inhibitor phosphodiesterase 10a pde10a, schizophrenia anxiety huntington disease prevention treatment pyrazole preparation, drug dependence alzheimer disease prevention treatment pyrazole preparation, pyridinylpyrazolyloxymethylphenybenzimidazole preparation inhibitor phosphodiesterase 10a and other aspects.Quality Control of 5-Chloroquinoxaline
Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider