59883-07-7Relevant academic research and scientific papers
N-Heterocyclic carbene based catalytic platform for Hauser-Kraus annulations
Sharique, Mohammed,Tambar, Uttam K.
, p. 7239 - 7243 (2020/07/23)
The venerable Hauser-Kraus annulation is an effective and convergent method for generating oxygenated polycyclic aromatic compounds. Despite its application in complex molecule synthesis, the harsh and strongly basic conditions can limit its utility in more functionalized molecular settings. We have developed the first catalytic Hauser-Kraus annulation based on N-heterocyclic carbene catalysis that proceeds under milder conditions. We demonstrate the scope of the transformation in the presence of several functional groups. We also propose a concerted mechanism for the annulation that proceeds through a non-canonical Breslow intermediate. This journal is
Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP4 receptor partial agonist for the treatment of pain
Healy, Mark P.,Allan, Amanda C.,Bailey, Kristin,Billinton, Andy,Chessell, Iain P.,Clayton, Nicholas M.,Giblin, Gerard M.P.,Kay, Melanie A.,Khaznadar, Tarik,Michel, Anton D.,Naylor, Alan,Price, Helen,Spalding, David J.,Stevens, David A.,Swarbrick, Martin E.,Wilson, Alexander W.
, p. 1892 - 1896 (2018/05/17)
A novel series of EP4 agonists and antagonists have been identified, and then used to validate their potential in the treatment of inflammatory pain. This paper describes these novel ligands and their activity within a number of pre-clinical mo
NAPHTHALENE AND QUINOLINE SULFONYLUREA DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS
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Page/Page column 20-21, (2008/12/04)
The invention is directed to naphthalene and quinoline sulfonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.
BENZO (F) ISOINDOL-2-YLPHENYL ACETIC ACID DERIVATIVES AS EP4 RECEPTOR AGONISTS
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Page/Page column 56, (2010/11/28)
A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1 R2 R3, R4, R5, R6, X and Y are as defined in the specification; a process for preparing such compo
An Efficient Synthesis of p-Quinones utilizing a Novel Pummerer-type Rearrangement of p-Sulfinylphenols
Akai, Shuji,Takeda, Yoshifumi,Iio, Kiyosei,Yoshida, Yutaka,Kita, Yasuyuki
, p. 1013 - 1014 (2007/10/02)
Treatment of the p-sulfinylphenol derivatives 1 and 5 with trifluoroacetic anhydride causes a Pummerer-type rearrangement on aromatic rings and concomitant desulfurization to give 1:1 mixtures of the corresponding p-quinones and p-dihydroquinones, which are subjected to mild oxidation to provide high yields of p-quinones 3 and 7.
Synthesis, Conformation, and Complexation Behavior of 2,9,18,25-Tetraoxa(1,4)naphthalenophane
Adams, Steven P.,Whitlock, Howard W.
, p. 3474 - 3478 (2007/10/02)
The synthesis of the title compound is described.Evidence is presented for its preferential "face-edge" conformation.Charge-transfer complexation proves to be a classical ?-? interaction with the "face-edge"conformation.There is no evidence for inclusion complexation.Attempted synthesis of substituted analogues of the title compound is described, including novel transformations in the 1,2,4-trisubstituted and 1,2,3,4-tetrasubstituted naphthalene series.
