40899-68-1Relevant academic research and scientific papers
Regioselective oxidative arylation of indoles bearing N-alkyl protecting groups: Dual c-h functionalization via a concerted metalation-deprotonation mechanism
Potavathri, Shathaverdhan,Pereira, Kyle C.,Gorelsky, Serge I.,Pike, Andrew,Lebris, Alexis P.,Deboef, Brenton
supporting information; experimental part, p. 14676 - 14681 (2010/12/24)
The most direct method for synthesizing 2-arylindoles is oxidative coupling of an arene with an indole. We have shown that both the activity and regioselectivity of this cross-coupling reaction are correlated with the acidity of the medium. This insight has been applied to predict the best conditions for the oxidative cross-coupling of N-alkylindoles, an important class of substrates that has heretofore been incompatible with the harsh conditions required for oxidative cross-coupling. Both experimental and computational data indicate that the mechanism for C-H palladation of both the indoles and simple arenes is best described as concerted metalation-deprotonation, regardless of the substitution on the arene.
2-Aryl-3,3,3-trifluoro-2-hydroxypropionic acids: A new class of protein tyrosine phosphatase 1B inhibitors
Adams, David R.,Abraham, Achamma,Asano, Jun,Breslin, Catherine,Dick, Colin A.J.,Ixkes, Ulrich,Johnston, Blair F.,Johnston, Derek,Kewnay, Justin,Mackay, Simon P.,MacKenzie, Simon J.,McFarlane, Morag,Mitchell, Lee,Spinks, Daniel,Takano, Yasuo
, p. 6579 - 6583 (2008/09/16)
A new series of non-peptidic, mono-acid protein tyrosine phosphatase 1B (PTP1B) inhibitors has been identified by structure-based design. Compounds with 2-(indol-3-yl)- and 2-phenyl-3,3,3-trifluoro-2-hydroxypropionic acid core units targeted at the enzyme's primary site and a hydrophobic chlorophenylthiazole extension in its 2° site exhibit 3-60 μM IC50s for PTP1B inhibition in an Sf9 cell-based assay.
SUBSTITUTED BISINDOLYLMALEIMIDES FOR THE INHIBITION OF CELL PROLIFERATION
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, (2008/06/13)
Certain substituted pyrroles are antiproliferative agents useful in the treatment of cancer.
Substituted pyrroles
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, (2008/06/13)
Certain substituted pyrroles are antiproliferative agents useful in the treatment of cancer.
TETRAHYDRO-BETA-CARBOLINES
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, (2008/06/13)
Tetrahydro-beta-carboline compounds having useful central nervous system activity are enclosed.
INTERMEDIATES TO TETRAHYDRO-BETA-CARBOLINES
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, (2008/06/13)
3-Ethanamine and 3-ethanamine related compounds are provided that are useful intermediates and have beneficial central nervous system activity.
METHOD FOR TREATING 5HT2B RECEPTOR RELATED CONDITIONS
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, (2008/06/13)
The present invention provides methods for binding a 5-HT 2B receptor in mammals using a both known and novel compounds. Further, the invention provides a method for treating or preventing 5-HT 2B related conditions. Finally, the invention provides an article of manufacture.
TETRAHYDRO-PYRIDO-INDOLE
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, (2008/06/13)
The present invention provides pentacyclic pyrido[3,4-b] indoles having useful central nervous system activity.
Tetrahydro-β-carbolines
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, (2008/06/13)
The present invention provides tetrahydro-betacarboline compounds having useful central nervous system activity.
Tetrahydro-pyrido-indole
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, (2008/06/13)
The present invention provides a new Pictet-Spengler process useful for preparing tetrahydro-beta-carboline compounds.
