32454-16-3Relevant academic research and scientific papers
Intermolecular Reductive Couplings of Arylidene Malonates via Lewis Acid/Photoredox Cooperative Catalysis
McDonald, Benjamin R.,Scheidt, Karl A.
supporting information, p. 6877 - 6881 (2018/11/02)
A cooperative Lewis acid/photocatalytic reduction of arylidene malonates yields a versatile radical anion species. This intermediate preferentially undergoes intermolecular radical-radical coupling reactions, and not the conjugate addition-dimerization reactivity typically observed in the single-electron reduction of conjugate acceptors. Reported here is the development of this open-shell species in intermolecular radical-radical cross couplings, radical dimerizations, and transfer hydrogenations. This reactivity underscores the enabling modularity of cooperative catalysis and demonstrates the utility of stabilized enoate-derived radical anions in intermolecular bond forming reactions.
BIARYL DERIVATIVE AS GPR120 AGONIST
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Paragraph 0341, (2017/11/17)
The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.
Br?nsted Acid-Catalyzed Intramolecular Hydroarylation of β-Benzylstyrenes
Cai, Xiao,Keshavarz, Amir,Omaque, Justin D.,Stokes, Benjamin J.
supporting information, p. 2626 - 2629 (2017/05/24)
Using triphenylmethylium tetrakis(pentafluorophenyl)borate as a convenient Br?nsted acid precatalyst, β-(α,α-dimethylbenzyl)styrenes are shown to cyclize efficiently to afford a variety of new indanes that possess a benzylic quaternary center. The geminal dimethyl-containing quaternary center is proposed to be necessary to arm the substrate for cyclization through steric biasing.
CYCLOALKYLNITRILE PYRAZOLE CARBOXAMIDES AS JANUS KINASE INHIBITORS
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, (2013/04/10)
Cycloalkylnitrile pyrazole carboxamides as JAK inhibitors useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer are provided.
NEPRILYSIN INHIBITORS
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Paragraph 0409, (2013/05/09)
In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
NEPRILYSIN INHIBITORS
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Page/Page column 84, (2012/06/30)
In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
CF3CO2ZnEt-mediated highly regioselective rearrangement of bromohydrins to aldehydes
Wang, Zhihui,Li, Meiyi,Zhang, Wenqin,Jia, Jiangnan,Wang, Fei,Xue, Song
supporting information; experimental part, p. 5968 - 5971 (2011/11/29)
A highly efficient and selective rearrangement reaction of bromohydrins to aldehydes mediated by CF3CO2ZnEt was described. The secondary and tertiary aldehydes were prepared under mild conditions in good to excellent yields (85-99%). The scope and limitations of this rearrangement process were also investigated.
4-AMINO-7,8-DIHYDROPYRIDO[4,3-d]PYRIMIDIN-5(6H)-ONE DERIVATIVES
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Page/Page column 17, (2010/08/08)
The invention provides compounds of the general Formula (I) where R1, R2, and A are defined herein, as well as the preparation, compositions and uses thereof.
A Novel Approach to Dual-Acting Thromboxane Receptor Antagonist/Synthase Inhibitors Based on the Link of 1,3-Dioxane-Thromboxane Receptor Antagonists and -Thromboxane Synthase Inhibitors
Ackerley, Norman,Brewster, Andrew G.,Brown, George R.,Clarke, David S.,Foubister, Alan J.,et al.
, p. 1608 - 1628 (2007/10/02)
A new class of dual-acting racemic thromboxane receptor antagonist/thromboxane synthase inhibitors is reported, based on the novel approach of linking the known thromboxane synthase inhibitors (TXSI) dazoxiben (2) or isbogrel (11) (separately) to thromboxane receptor antagonists (TXRA) from the 1,3-dioxane series, such as ICI 192605 (10).Dual activity was observed in vitro with inhibition of human microsomal thromboxane synthase in the range IC50 = 0.01-1.0 μM and receptor antagonist activity by inhibition of U46619-induced human platelet aggregation in the range pA2 = 5.5-7.0.The in vitro results also showed that very large groups could be tolerated at the selected substitution positions of the TXRA and TXSI components.Oral activity was observed in ex vivo tests in both rats and dogs at a dose of 10 mg/kg.Thus, (E)-7--4-(2-hydroxyphenyl)-1,3-dioxan-2-yl>benzyl>oxy>phenyl>-7-(3-pyridyl)hept-6-enoic acid (110) was both an antagonist (pA2 = 6.7) and a synthase inhibitor (IC50 = 0.02 μM)).On oral dosing (10 mg/kg) to rats and dogs, 110 showed significant TXRA activity 64 (rat, 3 h) and >59 +/- 11.3 (dog, 2 h) vs ex vivo U46619-induced platelet aggregation>.Inhibition of thromboxane synthase at the respective time points in these experiments was 81 +/- 4.4percent (rat) and 69 +/- 4.8percent (dog).
