131880-76-7Relevant articles and documents
Rhodium-catalyzed direct C7 alkynylation of indolines
Jin, Ning,Pan, Changduo,Zhang, Honglin,Xu, Pan,Cheng, Yixiang,Zhu, Chengjian
, p. 1149 - 1153 (2015)
An efficient rhodium(III)-catalyzed direct C7 alkynylation of indoline C-H bonds with the alkynylated hypervalent iodine reagents has been developed. This reaction proceeds smoothly under mild conditions over a wide structural scope with high site-selectivity and excellent functional-group tolerance. N-Acetyl as well as other N-acyls served as effective directing groups (DG). This procedure allows for the synthesis of a variety of 7-alkynyl-substituted indolines in good to excellent yield. More significantly, C7-alkynylated indoles through further transformations have been successfully accessed.
Ruthenium-catalyzed C7 amidation of indoline C-H bonds with sulfonyl azides
Pan, Changduo,Abdukader, Ablimit,Han, Jie,Cheng, Yixiang,Zhu, Chengjian
supporting information, p. 3606 - 3609 (2014/04/03)
A ruthenium-catalyzed direct C7 amidation of indoline C-H bonds with sulfonyl azides was developed. This procedure allows the synthesis of a variety of 7-amino-substituted indolines, which are useful in pharmaceutical. The good functional tolerances, as well as the mild conditions, are prominent feature of this method.
Iridium(I)-catalyzed direct C-H bond alkylation of the C-7 position of indolines with alkenes
Pan, Shiguang,Ryu, Naoto,Shibata, Takanori
supporting information, p. 929 - 933 (2014/04/03)
A cationic iridium-catalyzed C-7 alkylation of N-substituted indoline derivatives with various alkenes has been developed. A variety of 7-alkylindolines were obtained in moderate to high yields. This protocol relies on the use of the carbonyl group on the nitrogen atom of indoline as a directing group and it is potentially applicable to the large-scale synthesis of 7-alkylindoles.
Oxidative palladium(II)-catalyzed dehydrogenative C-H/C-H cross-coupling of 2,3-substituted indolines with arenes at the C7 position
Jiao, Lin-Yu,Oestreich, Martin
supporting information, p. 10845 - 10848 (2013/09/02)
Directed directing group: The C7 position of the indoline nucleus is difficult to address in C-H activation. An oxidative palladium(II) catalysis that allows for cross-dehydrogenative coupling in that position with activation of the C-H bond of the arene component is disclosed here. This C-H/C-H cross-coupling is applicable to various indolines acetylated at the nitrogen atom. Substitution at C2 is crucial for the C-H activation to occur at C7 (see scheme).
Sulfonamides for the Modulation of PKM2
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Page/Page column 43-44, (2012/05/07)
The invention relates to sulfonamide compounds and methods for activating PKM2. The compounds and methods are useful in treating or preventing a disease or disorder selected from cancer, cell proliferative disorder, inflammatory disorder, metabolic disorder, and immune system disorder.
Identification of inhibitors of NOD1-induced nuclear factor-κB activation
Khan, Pasha M.,Correa, Ricardo G.,Divlianska, Daniela B.,Peddibhotla, Satyamaheshwar,Sessions, E. Hampton,Magnuson, Gavin,Brown, Brock,Suyama, Eigo,Yuan, Hongbin,Mangravita-Novo, Arianna,Vicchiarelli, Michael,Su, Ying,Vasile, Stefan,Smith, Layton H.,Diaz, Paul W.,Reed, John C.,Roth, Gregory P.
supporting information; experimental part, p. 780 - 785 (2011/12/02)
NOD1 (nucleotide-binding oligomerization domain 1) protein is a member of the NLR (NACHT and leucine rich repeat domain containing proteins) protein family, which plays a key role in innate immunity as a sensor of specific microbial components derived from bacterial peptidoglycans and induction of inflammatory responses. Mutations in NOD proteins have been associated with various inflammatory diseases that affect NF-κB (nuclear factor κB) activity, a major signaling pathway involved in apoptosis, inflammation, and immune response. A luciferase-based reporter gene assay was utilized in a high-throughput screening program conducted under the NIH-sponsored Molecular Libraries Probe Production Center Network program to identify the active scaffolds. Herein, we report the chemical synthesis, structure-activity relationship studies, downstream counterscreens, secondary assay data, and pharmacological profiling of the 2-aminobenzimidazole lead (compound 1c, ML130) as a potent and selective inhibitor of NOD1-induced NF-κB activation.
Gold(I)-catalyzed intramolecular hydroamination of unactivated alkenes with carboxamides
Bender, Christopher F.,Widenhoefer, Ross A.
, p. 4143 - 4144 (2007/10/03)
N-Alkenyl carboxamides undergo gold-catalyzed intramolecular exo-hydroamination to form nitrogen heterocycles in excellent yield. The Royal Society of Chemistry 2006.
DIAMINOPYRROLOQUINAZOLINES COMPOUNDS AS PROTEIN TYROSINE PHOSPHATASE INHIBITORS
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Page 84, (2010/02/09)
The invention relates to diaminopyrroloquinazoline compounds of formula (I) wherein R1, Ra, Rb, Rc, Rd, Re, Rf and A are as defined in the specification and claims, which are useful for inhibiting protein tyrosine phosphatases, particularly PTP
Novel bicyclic isoxazolinones as antibacterial agents
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, (2008/06/13)
The present invention provides compounds of formula I useful as antimicrobial agents wherein X, Y, R1, and n are as defined in thereof.
Microbiological Transformations Part 13. Microbiological Transformations of Derivatives of Indoline with the Fungus Cunninghamella elegans
Crabb, Trevor A.,Canfield, Lesley M.
, p. 2936 - 2945 (2007/10/03)
The incubation of N-benzoylindoline and N-benzoyl-3-methylindoline with C. elegans resulted in reductive cleavage to produce the corresponding indoline and benzyl alcohol.N-Benzoyl-2-methylindoline and N-acetyl-2-methylindoline were hydroxylated at the benzylic position to produce a mixture of cis- and trans-substituted products.In contrast aromatic ring hydroxylation of N-acetyl-2-methylindoline occurred to give N-acetyl-5-hydroxy-2-methylindoline.Incubation of N-benzoyl-7-methylindoline also resulted in aromatic ring hydroxylation.
