- Direct Carboxylation of Electron-Rich Heteroarenes Promoted by LiO-tBu with CsF and [18]Crown-6
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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.
- Shigeno, Masanori,Hanasaka, Kazuya,Sasaki, Keita,Nozawa-Kumada, Kanako,Kondo, Yoshinori
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supporting information
p. 3235 - 3239
(2019/02/13)
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- SUBSTITUTED BENZOFURAN, BENZOTHIOPHENE AND INDOLE MCL-1 INHIBITORS
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The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
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Page/Page column 233
(2014/04/04)
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- [(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
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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.
- Hong, Yong Rae,Kim, Hyun Tae,Lee, Seung-Chul,Ro, Seonggu,Cho, Joong Myung,Kim, In Su,Jung, Young Hoon
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supporting information
p. 5953 - 5957
(2013/10/22)
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- PYRIDINE DERIVATIVES AND METHODS OF USE THEREOF
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Disclosed herein are pyridine derivatives, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, pharmaceutical compositions comprising the same, and methods of modulating the level or activity of HIF in a subject, inhibiting hydroxylat
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Page/Page column 24-25
(2011/02/25)
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- ACTIVATOR FOR PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR
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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
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Page/Page column 24
(2011/02/19)
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- PHOTOCYCLIZATION OF METHYL 2-ARYLTHIO- AND 2-ARYLOXY-ACETOACETATES A FACILE SYNTHESIS OF BENZOHETEROCYCLES
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A series of methyl 2-arylthio- (2) and 2-aryloxy-acetoacetates (3) have been prepared and their tautomeric equilibria have been examined by 1H NMR spectroscopy.S-substitution at the α-position results in an increase of enol tautomer over 90percent, while
- Sasaki, Tadashi,Hayakawa, Kenji,Ban, Hiroshi
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- PHOTOCYCLIZATION OF METHYL 2-ARYLTHIOACETOACETATES A FACILE SYNTHESIS OF BENZOTHIOPHENES
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A series of methyl 2-arylthioacetoacetates was irradiated in a benzene-methanol solution to give benzothiophenes in satisfactory yields.
- Sasaki, Tadashi,Hayakawa, Kenji
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p. 1525 - 1526
(2007/10/02)
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