3133-81-1Relevant articles and documents
Direct Carboxylation of Electron-Rich Heteroarenes Promoted by LiO-tBu with CsF and [18]Crown-6
Shigeno, Masanori,Hanasaka, Kazuya,Sasaki, Keita,Nozawa-Kumada, Kanako,Kondo, Yoshinori
supporting information, p. 3235 - 3239 (2019/02/13)
We herein demonstrate that the combination of LiO-tBu, CsF, and [18]crown-6 efficiently promotes the direct C?H carboxylation of electron-rich heteroarenes (benzothiophene, thiophene, benzofuran, and furan derivatives). A variety of functional groups, including methyl, methoxy, halo, cyano, amide, and keto moieties, are compatible with this system. The reaction proceeds via the formation of a tert-butyl carbonate species.
[(4-Hydroxyl-benzo[4,5]thieno[3,2-c]pyridine-3-carbonyl)-amino]-acetic acid derivatives; HIF prolyl 4-hydroxylase inhibitors as oral erythropoietin secretagogues
Hong, Yong Rae,Kim, Hyun Tae,Lee, Seung-Chul,Ro, Seonggu,Cho, Joong Myung,Kim, In Su,Jung, Young Hoon
supporting information, p. 5953 - 5957 (2013/10/22)
A new series of PHD (HIF prolyl 4-hydroxylase) inhibitors was designed based on the X-ray co-crystal structure of FG-2216. Using a lead generation process, a series of [(4-Hydroxyl-benzo[4,5]thieno[3,2-c]pyridine-3-carbonyl)- amino]-acetic acid derivatives was developed as potent PHD2 inhibitors. This class of compounds also showed the ability to stabilize HIF-α, to stimulate EPO secretion in in vitro studies, and to increase hematocrit, red blood cell count, and hemoglobin levels in an animal efficacy study.
ACTIVATOR FOR PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR
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Page/Page column 24, (2011/02/19)
A compound represented by the formula (I) or a pharmacologically acceptable salt thereof is used as an activator of PPAR. wherein each of R1 and R2 is hydrogen, C1-8 alkyl, C1-8 alkyl substituted with halogen, or the like; each of R3, R4, R5, and R6 is h