6318-76-9Relevant academic research and scientific papers
Synthesis of β-Amino Diaryldienones Using the Mannich Reaction
Elshan, N. G. R. Dayan,Rettig, Matthew B.,Jung, Michael E.
supporting information, (2019/06/13)
The Mannich reaction has been used for decades to prepare many pharmaceutically important molecules. Here, using a "double-Mannich-β-elimination" synthetic sequence, we report the synthesis and the characterization details of a novel class of β-amino diaryldienones with prominent antiprostate cancer activity. Through these studies, we correct an erroneous structure in the current literature, present a discussion of the stereochemical outcome of a new reaction, and probe the mechanism(s) of byproduct formation through isotopic studies.
INHIBITORS OF THE N-TERMINAL DOMAIN OF THE ANDROGEN RECEPTOR
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Page/Page column 53; 54; 114, (2018/08/12)
The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.
Preparation of 1-methyl-3-phenylisoquinoline derivatives from oximes using polyphosphoric esters
Niemczak, Micha?,Czerniak, Kamil,Kopczyński, Tomasz
, p. 1868 - 1873 (2015/03/18)
We show a beneficial new approach to the preparation of 1-methyl-3-phenylisoquinoline derivatives. This method involves heating polyphosphate ester and the appropriate oximes obtained from 3,4-diphenylbut-3-en-2-one derivatives. The isoquinolines were syn
Acid-catalyzed synthesis of α,β-disubstituted conjugated enones by a Meyer-Schuster-type rearrangement in allenols
Alcaide, Benito,Almendros, Pedro,Cembellín, Sara,Martínez Del Campo, Teresa
, p. 1070 - 1078 (2015/03/30)
A novel, direct and simple methodology to gain access to α,β-disubstituted conjugated enones from α-allenols in a sustainable metal catalysis context, considering the inexpensiveness and environmentally friendliness of iron(III) species and protons, has b
Synthesis and antimicrobial evaluation of some pyrazole derivatives
Sharshira, Essam Mohamed,Hamada, Nagwa Mohamed Mahrous
scheme or table, p. 4962 - 4971 (2012/09/22)
Reaction of a series of (E)-3-phenyl-4-(p-substituted phenyl)-3-buten-2- ones with p-sulfamylphenyl hydrazine in glacial acetic acid gave the corresponding hydrazones, subsequent treatment of which with 30% HCl afforded pyrazole-1-sulphonamides. On the ot
Iridium-catalyzed asymmetric hydrogenation of α-substituted α,β-unsaturated acyclic ketones: Enantioselective total synthesis of (-)-mesembrine
Zhang, Qian-Qian,Xie, Jian-Hua,Yang, Xiao-Hui,Xie, Jian-Bo,Zhou, Qi-Lin
supporting information, p. 6158 - 6161 (2013/02/23)
A highly efficient asymmetric hydrogenation of α-substituted α,β-unsaturated acyclic ketones catalyzed by chiral spiro iridium complexes for the preparation of chiral 2-substituted allylic alcohols has been developed (ee up to 99.7%). This method provides a concise route to (-)-mesembrine (34% yield, 12 steps).
Substituted isoxazoles for the treatment of inflammation
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Page 39, (2010/11/30)
A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula (III) wherein R7 is selected from hydroxyl, lower alkyl, carboxyl, halo, lower carboxylalkyl, lower alkoxycarbonylalkyl, lower alkoxyalkyl, lower carboxyalkoxyalkyl, lower haloalkyl, lower haloalkylsulfonyloxy, lower hydroxyalkyl, lower aryl (hydroxylalkyl), lower carboxyaryloxyalkyl, lower alkoxycarbonylaryloxyalkyl, lower cycloalkyl, lower cycloalkylalkyl, and lower aralkyl; and wherein R8 is one or more radicals independently selected from hydrido, lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower hydroxyalkyl, lower haloalkoxy, amino, lower alkylamino, lower arylamino, lower aminoalkyl, nitro, halo, lower alkoxy, aminosulfonyl, and lower alkylthio; or a pharmaceutically-acceptable salt thereof.
Isoxazole compounds as cyclooxygenase inhibitors
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, (2008/06/13)
A class of substituted isoxazolyl compounds is described for use in treating cyclooxygenase-2 related disorders. Compounds of particular interest are defined by Formula I STR1 wherein R1, R2, and R3, are described in the specification.
