92-89-7Relevant academic research and scientific papers
Organic Solvent-Free, Pd(II)-Salan Complex-Catalyzed Synthesis of Biaryls via Suzuki-Miyaura Cross-Coupling in Water and Air
Bunda, Szilvia,Udvardy, Antal,Voronova, Krisztina,Joó, Ferenc
, p. 15486 - 15492 (2019/01/03)
With use of a Pd(II)-sulfosalan complex as a water-soluble catalyst, we have developed an efficient synthesis of biaryls via Suzuki-Miyaura cross-coupling in water under aerobic conditions. The water-insoluble target molecules were isolated by simple filtration in analytical purity after washing with 0.01 M aqueous HCl (20 examples). In most cases, palladium contamination was below 5 ppm considered acceptable for active pharmaceutical ingredients. The established method is scalable, reproducible, and provides biaryl products in isolated yields up to 91%.
Copper chelators
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Paragraph 0039, (2015/11/09)
The present invention relates to a new class of chemical compounds of structure 6,7-dimethoxy-1,2,3,4-tetra-hydro-isoquinoline having therapeutic action, processes for the synthesis thereof and formulations containing said derivatives. More particularly, the present invention relates to ligand compounds adapted for chelating the free cupric ion in the serum of patients suffering from Alzheimer's and Wilson's diseases.
Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents
Lu, Chenshu,Tang, Ke,Li, Yan,Li, Peng,Lin, Ziyun,Yin, Dali,Chen, Xiaoguang,Huang, Haihong
, p. 351 - 360 (2014/04/17)
A novel series of diaryl ureas containing different linker groups were designed and synthesized. Their in vitro antitumor activity against MX-1, A375, HepG2, Ketr3 and HT-29 was evaluated using the standard MTT assay. Compounds having a rigid linker group such as vinyl, ethynyl and phenyl showed significant inhibitory activity against a variety of cancer cell lines. Specifically, compound 23 with a phenyl linker group demonstrated broad-spectrum antitumor activity with IC50 values of 5.17-6.46 μM against five tested tumor cell lines. Compound 23 is more potent than reference drug sorafenib (8.27-15.2 μM), representing a promising lead for further optimization.
Synthesis and luminescence properties of biphenyl-type firefly luciferin analogs with a new, near-infrared light-emitting bioluminophore
Miura, Chihiro,Kiyama, Masahiro,Iwano, Satoshi,Ito, Kazuto,Obata, Rika,Hirano, Takashi,Maki, Shojiro,Niwa, Haruki
, p. 9726 - 9734 (2013/10/22)
New firefly luciferin analogs of the 4,4′-substituted biphenyl-type were synthesized. One analog with a 4′-dimethylamino group possessed bioluminescence activity, emitting near-infrared biological window light at 675 nm suitable for deep-site bioimaging of living animals. The chemiluminescence light-emission maximum of the corresponding methyl ester of the bioluminescence active analog was 500 nm, implying that biphenyl and thiazolinone rings in the light emitter might be placed in a coplanar conformation at the polar luciferase active site.
Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA)
Venkatraj, Muthusamy,Messagie, Jonas,Joossens, Jurgen,Lambeir, Anne-Marie,Haemers, Achiel,Van Der Veken, Pieter,Augustyns, Koen
supporting information; experimental part, p. 1557 - 1568 (2012/04/17)
Recent drug discovery programs targeting urokinase plasminogen activator (uPA) have resulted in nonpeptidic inhibitors consisting of amidine or guanidine functional groups attached to aromatic or heteroaromatic scaffolds. There is a general problem of poor oral bioavailability of these charged inhibitors. In this paper, we report the synthesis and evaluation of a series of naphthamide and naphthalene sulfonamides as uPA inhibitors containing non-basic groups as substitute for amidine or guanidine groups.
Photoactivatable HNO-releasing compounds using the retro-Diels-Alder reaction
Adachi, Yusuke,Nakagawa, Hidehiko,Matsuo, Kazuya,Suzuki, Takayoshi,Miyata, Naoki
supporting information; experimental part, p. 5149 - 5151 (2009/03/11)
We synthesized hetero-Diels-Alder cycloadducts from acyl nitroso derivatives and 9,10-dimethylanthracene, to be photo-inducible HNO-releasing agents and found that introduction of conjugated nitroaromatic groups effectively enhanced the responsiveness of HNO release to UV-A irradiation; we confirmed photoinduced HNO formation by EPR and GCMS analysis. The Royal Society of Chemistry.
PREPARATION AND USE OF BIPHENYL AMINO ACID DERIVATIVES FOR THE TREATMENT OF OBESITY
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Page/Page column 15, (2010/11/25)
This invention relates to certain biphenyl amino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
Heterobifunctional pan-selectin inhibitors
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Page/Page column 12, (2010/11/26)
Compounds and methods are provided for modulating in vitro and in vivo processes mediated by selectin binding. More specifically, selectin modulators and their use are described, wherein the selectin modulators that modulate (e.g., inhibit or enhance) a selectin-mediated function comprise particular glycomimetics alone or linked to a member of a class of compounds termed BASAs (Benzyl Amino Sulfonic Acids) or a member of a class of compounds termed BACAs (Benzyl Amino Carboxylic Acids).
PREPARATION AND USE OF BIPHENYL-4-YL-CARBONYLAMINO ACID DERIVATIVES FOR THE TREATMENT OF OBESITY
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Page/Page column 47, (2010/11/08)
This invention relates to certain biphenyl-4-yl carbonylamino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
HETEROBIFUNCTIONAL COMPOUNDS FOR SELECTIN INHIBITION
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Page/Page column 25, (2008/06/13)
Compounds and methods are provided for modulating in vitro and in vivo processes mediated by selectin binding. More specifically, selectin modulators and their use are described, wherein the selectin modulators that modulate (e.g., inhibit or enhance) a selectin-mediated function comprise glycomimetics linked to a compound, for example a member of a class of compounds termed BASAs (Benzyl Amino Sulfonic Acids) or a member of a class of compounds termed BACAs (Benzyl Amino Carboxylic Acids).
