90924-54-2Relevant academic research and scientific papers
Oxidize Amines to Nitrile Oxides: One Type of Amine Oxidation and Its Application to Directly Construct Isoxazoles and Isoxazolines
Zhang, Xiao-Wei,He, Xiao-Lin,Yan, Nan,Zheng, Hong-Xing,Hu, Xiang-Guo
, p. 15726 - 15735 (2020/11/30)
A facile oxidative heterocyclization of commercially available amines and tert-butyl nitrite with alkynes or alkenes leading to isoxazoles or isoxazolines is described. The unprecedented strategy of the oxidation of an amine directly to a nitrile oxide was used in this cyclization process. This reaction is highly efficient, regiospecific, operationally simple, mild, and tolerant of a variety of functional groups. Control experiments support a nitrile oxide intermediate mechanism for this novel class of oxidative cyclization reactions. Moreover, synthetic applications toward bioactive molecular skeletons and the late-stage modification of drugs were realized.
Development of a continuous flow photoisomerization reaction converting isoxazoles into diverse oxazole products
Bracken, Cormac,Baumann, Marcus
, p. 2607 - 2617 (2020/03/11)
A continuous flow process is presented, which directly converts isoxazoles into their oxazole counterparts via a photochemical transposition reaction. This results in the first reported exploitation of this transformation to establish its scope and synthe
ISOXAZOLE CARBOXAMIDE COMPOUNDS AND USES THEREOF
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Page/Page column 39-40, (2020/04/25)
A compound of Formula (I) or or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating hearing loss or balance disorder: Formula (I) wherein R1 and Y are as defined herein.
ISOXAZOLE CARBOXAMIDE COMPOUNDS AND USES THEREOF
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Paragraph 0135-0136, (2018/10/19)
A compound of Formula (I)) or or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating hearing loss or balance disorder: wherein R1 through R3, and L are as defined herein.
PYRADAZINONE DERIVATIVES AND THE COMPOSITIONS AND METHODS OF TREATMENT REGARDING THE SAME
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Paragraph 488; 491-492, (2018/01/17)
The present disclosure is directed to pyridazin-3(2H)-one compounds of formula (I), pharmaceutical compositions thereof and methods for modulating or activating a Parkin ligase The present disclosure is also directed to methods of treating and/or reducing the incidence of diseases or conditions related to the activation of Parkin ligase, R21, R22, R23, R24 and R25 are as defined herein.
Synthesis and evaluation as antitubercular agents of 5-arylethenyl and 5-(hetero)aryl-3-isoxazolecarboxylate
Vergelli, Claudia,Cilibrizzi, Agostino,Crocetti, Letizia,Graziano, Alessia,Dal Piaz, Vittorio,Wan, Baojie,Wang, Yuehong,Franzblau, Scott,Giovannoni, Maria Paola
, p. 162 - 172 (2013/05/22)
Preclinical Research A new series of 5-aryl and 5-arylethenylisoxazole carboxylate derivatives was synthesized and evaluated for in vitro activity against Mycobacterium tuberculosis H37Rv. Several compounds exhibited minimum inhibitory concentrations in the low micromolar range (2.3-11.4 μM). A variety of substituents introduced around the isoxazole ring allowed the delineation of preliminary SARs for this new series of compounds.
Molecular recognition at the active site of factor Xa: Cation-π Interactions, stacking on planar peptide surfaces, and replacement of structural water
Salonen, Laura M.,Holland, Mareike C.,Kaib, Philip S. J.,Haap, Wolfgang,Benz, J?rg,Mary, Jean-Luc,Kuster, Olivier,Schweizer, W. Bernd,Banner, David W.,Diederich, Fran?ois
supporting information; experimental part, p. 213 - 222 (2012/03/09)
Factor Xa, a serine protease from the blood coagulation cascade, is an ideal enzyme for molecular recognition studies, as its active site is highly shape-persistent and features distinct, concave sub-pockets. We developed a family of non-peptidic, small-molecule inhibitors with a central tricyclic core orienting a neutral heterocyclic substituent into the S1 pocket and a quaternary ammonium ion into the aromatic box in the S4 pocket. The substituents were systematically varied to investigate cation-π interactions in the S4 pocket, optimal heterocyclic stacking on the flat peptide walls lining the S1 pocket, and potential water replacements in both the S1 and the S4 pockets. Structure-activity relationships were established to reveal and quantify contributions to the binding free enthalpy, resulting from single-atom replacements or positional changes in the ligands. A series of high-affinity ligands with inhibitory constants down to Ki=2nM were obtained and their proposed binding geometries confirmed by X-ray co-crystal structures of protein-ligand complexes. Factor Xa is an ideal enzyme to undertake molecular recognition studies at atomic level resolution as its active site is completely conserved in complexes with designed ligands. Cation-π interactions, water replacements, and stacking interactions with flat peptide fragments were investigated, revealing large changes in binding affinity resulting from single-atom mutations or positional shifts of heteroatoms in the ligands. Copyright
Solid-phase synthesis of isoxazoles using vinyl ethers as chameleon catches
Barrett, Anthony G. M.,Procopiou, Panayiotis A.,Voigtmann, Ulrike
, p. 3165 - 3168 (2007/10/03)
(figure presented) Regioselective 1,3-dipolar cycloadditions of supported vinyl ethers R1C(=CH2)O-CH2-polymer, prepared by the Tebbe olefination of R1CO2-CH2-polymer with ethyl cyanoformate
