32017-77-9Relevant academic research and scientific papers
Kinetic resolution ofN-aryl β-amino alcoholsviaasymmetric aminations of anilines
Guo, Zheng,Xie, Jinglei,Hu, Tao,Chen, Yunrong,Tao, Houchao,Yang, Xiaoyu
supporting information, p. 9394 - 9397 (2021/09/22)
An efficient kinetic resolution ofN-aryl β-amino alcohols has been developedviaasymmetricpara-aminations of anilines with azodicarboxylates enabled by chiral phosphoric acid catalysis. Broad substrate scope and high kinetic resolution performances were afforded with this method. Control experiments supported the critical roles of the NH and OH group in these reactions.
The Activation of Carboxylic Acids via Self-Assembly Asymmetric Organocatalysis: A Combined Experimental and Computational Investigation
Monaco, Mattia Riccardo,Fazzi, Daniele,Tsuji, Nobuya,Leutzsch, Markus,Liao, Saihu,Thiel, Walter,List, Benjamin
supporting information, p. 14740 - 14749 (2016/11/18)
The heterodimerizing self-assembly between a phosphoric acid catalyst and a carboxylic acid has recently been established as a new activation mode in Br?nsted acid catalysis. In this article, we present a comprehensive mechanistic investigation on this activation principle, which eventually led to its elucidation. Detailed studies are reported, including computational investigations on the supramolecular heterodimer, kinetic studies on the catalytic cycle, and a thorough analysis of transition states by DFT calculations for the rationalization of the catalyst structure-selectivity relationship. On the basis of these investigations, we developed a kinetic resolution of racemic epoxides, which proceeds with high selectivity (up to s = 93), giving the unreacted epoxides and the corresponding protected 1,2-diols in high enantiopurity. Moreover, this approach could be advanced to an unprecedented stereodivergent resolution of racemic α-chiral carboxylic acids, thus providing access to a variety of enantiopure nonsteroidal anti-inflammatory drugs and to α-amino acid derivatives.
Catalytic Enantioselective Conversion of Epoxides to Thiiranes
Liao, Saihu,Leutzsch, Markus,Monaco, Mattia Riccardo,List, Benjamin
supporting information, p. 5230 - 5233 (2016/05/19)
A highly efficient and enantioselective Br?nsted acid catalyzed conversion of epoxides to thiiranes has been developed. The reaction proceeds in a kinetic resolution, furnishing both epoxide and thiirane in high yields and enantiomeric purity. Heterodimer formation between the catalyst and sulfur donor affords an effective way to prevent catalyst decomposition and enables catalyst loadings as low as 0.01 mol %.
Three powerful dinuclear metal-organic catalysts for converting CO2 into organic carbonates
Zhao, Dan,Liu, Xiao-Hui,Shi, Zhuang-Zhi,Zhu, Chen-Dan,Zhao, Yue,Wang, Peng,Sun, Wei-Yin
, p. 14184 - 14190 (2016/11/05)
Developing efficient catalysts for converting carbon dioxide (CO2) into varied organic carbonates is an important scientific goal. By using the NH2-functionalized tripodal ligand 2-((bis(2-aminoethyl)amino)methyl)phenol (HL), three dinuclear metal-organic complexes [Zn(L)]2·2ClO4 (1), [Cu(L)]2·2ClO4·2H2O (2) and [Cd(L)]2·2ClO4 (3) have been successfully isolated and structurally characterized using single-crystal X-ray diffraction analyses. Considering the dinuclear metal centers and the NH2-functional groups in the structures, 1-3 were investigated as catalysts for converting CO2 into organic carbonates, and the results show that 1-3 exhibit an outstanding ability for converting CO2 into varied organic carbonates at atmospheric pressure (0.1 MPa). The catalytic system also displays a wide substrate scope and high catalytic activity, and the reaction mechanism has been proposed herein.
PPAR-sparing thiazolidinedione salts for the treatment of metabolic diseases
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Page/Page column 108, (2015/09/28)
The present invention relates to novel salts of thiazolidinediones and other pharmaceutical agents that are useful for treating and/or preventing metabolic diseases (e.g., diabetes, or neurodegenerative diseases (e.g., Alzheimer's Disease).
PPAR-SPARING THIAZOLIDINEDIONES AND COMBINATIONS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
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Paragraph 0391; 0392, (2014/07/07)
The present invention relates to PPARy- sparing compounds and pharmaceutical compositions formulated with such compounds that are useful for treating, delaying the onset of, or reducing the symptoms of a neurodegenerative disorder including Huntington's disease, epilepsy, AMS, and MS.
Rhodium-catalyzed transannulation of N-sulfonyl-1,2,3-triazoles and epoxides: Regioselective synthesis of substituted 3,4-dihydro-2 H-1,4-oxazines
Ma, Xueji,Pan, Shanfei,Wang, Hangxiang,Chen, Wanzhi
supporting information, p. 4554 - 4557 (2015/02/19)
Rhodium-catalyzed transannulation of 1,2,3-triazoles and ring-opening reactions of epoxides is described. A number of 3,4-dihydro-2H-1,4-oxazines are obtained in moderate yields probably involving generation of α-imino rhodium(II) carbene species.
Novel Ethanediamone Hepcidine Antagonists
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, (2012/09/05)
The present invention relates to novel hepcidin antagonists of formula (I), pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for treatment of disorders in iron metabolism, such as, in particular, iron deficiency diseases and anaemias, in particular anaemias in connection with chronic inflammatory diseases (ACD: anaemia of chronic disease and AI: anaemia of inflammation).
THIAZOLIDINEDIONE ANALOGUES
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Page/Page column 62, (2010/10/03)
The present invention relates to thiazolidinedione analogues that are useful for treating hypertension, diabetes, and inflammatory diseases. In other aspects, the present invention also presents methods of treating hypertension, diabetes, or other inflamm
Design and synthesis of thiadiazoles and thiazoles targeting the Bcr-Abl T315I mutant: From docking false positives to ATP-noncompetitive inhibitors
Radi, Marco,Crespan, Emmanuele,Falchi, Federico,Bernardo, Vincenzo,Zanoli, Samantha,Manetti, Fabrizio,Schenone, Silvia,Maga, Giovanni,Botta, Maurizio
body text, p. 1226 - 1231 (2011/02/21)
(Figure Presented) Overcoming resistance: In an effort to optimize our previously identified dual Src/Abl hits, a new series of 1,3,4-thiadiazoles and 1,3-thiazoles were designed and synthesized, paying particular attention to the reduction of their lipophilicity and to the improvement of the affinity towards the drug-resistant T315I mutant. Compound 5 was identified as a promising allosteric inhibitor of the T315I mutant.
