159755-11-0Relevant academic research and scientific papers
Total synthesis of carbazole alkaloids
Bhatthula, Bharath kumar goud,Kanchani, Janardhan reddy,Arava, Veera reddy,Subha
, p. 874 - 887 (2019)
A Suzuki-Miyaura cross coupling, followed by triphenylphosphine mediated Cadogan reductive cyclization sequence provided efficient access to a series of carbazole alkaloids. In the present work, this approach was applied to the total synthesis of mukonine, clauszoline K, koenoline, murrayanine, murrayafoline A, mukoeic acid, glycoborine, glycozolicine, mukolidine, mukoline, glycozoline, 3-methoxy-9H-carbazole-1-carboxylic acid methyl ester, (3-methoxy-9H-carbazol-1-yl)-methanol, 3-methoxy-9H-carbazole-1-carbaldehyde, 3-methoxy-9H-carbazole-1-carboxylic acid, 2-methyl-9H-carbazole and nonsteroidal anti-inflammatory drug (NSAID) carprofen and its derivatives.
BRM TARGETING COMPOUNDS AND ASSOCIATED METHODS OF USE
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Paragraph 0761-0762, (2019/10/23)
The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
In Situ Generated Gold Nanoparticles on Active Carbon as Reusable Highly Efficient Catalysts for a Csp3 ?Csp3 Stille Coupling
Holz, Julia,Pfeffer, Camilla,Zuo, Hualiang,Beierlein, Dennis,Richter, Gunther,Klemm, Elias,Peters, René
supporting information, p. 10330 - 10334 (2019/06/27)
Gold nanoparticle catalysts are important in many industrial production processes. Nevertheless, for traditional Csp2-Csp2 cross-coupling reactions they have been rarely used and Pd catalysts usually give a superior performance. Herein we report that in situ formed gold metal nanoparticles are highly active catalysts for the cross coupling of allylstannanes and activated alkylbromides to form Csp3-Csp3 bonds. Turnover numbers up to 29 000 could be achieved in the presence of active carbon as solid support, which allowed for convenient catalyst recovery and reuse. The present study is a rare case where a gold metal catalyst is superior to Pd catalysts in a cross-coupling reaction of an organic halide and an organometallic reagent.
Synthesis of α-methylstilbenes using an aqueous Wittig methodology and application toward the development of potent human aromatase inhibitors
Nielsen, Alexander J.,Raez-Villanueva, Sergio,Crankshaw, Denis J.,Holloway, Alison C.,McNulty, James
supporting information, p. 1395 - 1398 (2019/04/03)
The development of aqueous Wittig methodology for the synthesis of α-methylstilbenes using tripropylphosphine-derived phosphonium salts is described. The Wittig olefination reaction was high yielding and allowed isolation of stilbenes by simple filtration and washing with water. The novel phosphonium salts employed were accessed via a highly efficient, regioselective addition of hydrogen bromide to styrenes. Application of the α-methylstilbenes toward the synthesis of a collection of stilbenoid-triazoles is reported and their inhibition of CYP450 19A1 (aromatase) investigated. The overall structure-activity profile provided additional evidence on the aryl halide-ketone bioisostere hypothesis and identified 6c as a potent inhibitor of aromatase in vitro (Ki = 8 nM).
THERAPEUTIC COMPOUNDS
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Paragraph 0591; 0592; 0593, (2018/11/21)
The present embodiments relate to substituted heterocyclic derivative therapeutic compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition
JAK kinase inhibitor and application
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Paragraph 0035-0036; 0044-0046, (2018/09/08)
The present invention discloses a compound having the following general formula (I). The present invention also discloses a JAK kinase inhibitor comprising the compound and application of the compoundin preparation of a medicament for treating JAK-associated diseases. The JAK kinase inhibitor can inhibit the biological activities of JAK1, JAK2, JAK3 and TYK2 kinases involved in various kinds of signal transduction, can effectively treat various inflammatory diseases and various JAK-mediated signal transduction-driven diseases, and has a very broad application prospect.
Visible-light-mediated benzylic sp3 C-H bond functionalization to C-Br or C-N bond
Hou, Tianyuan,Lu, Ping,Li, Pixu
supporting information, p. 2273 - 2276 (2016/05/10)
A visible-light-promoted functionalization of unactivated benzylic sp3 C-H bonds was developed. Ethylbenzene derivatives were converted to the corresponding benzyl bromides or afforded benzylamine derivatives in a one-pot manner under visible light photoredox conditions.
11 β-hydroxysteroid dehydrogenase 1 inhibitors
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Paragraph 0198; 0199; 0204-0207, (2016/11/02)
The invention belongs to the technical field of medicines, and concretely relates to a 11[beta]-hydroxysteroid dehydrogenase type 1 inhibitor as shown in a formula (I), pharmaceutically acceptable salts and isomers thereof, wherein X1, X2, R1, R2, R6a, R6
Catalytic Carbocation Generation Enabled by the Mesolytic Cleavage of Alkoxyamine Radical Cations
Zhu, Qilei,Gentry, Emily C.,Knowles, Robert R.
supporting information, p. 9969 - 9973 (2016/08/16)
A new catalytic method is described to access carbocation intermediates via the mesolytic cleavage of alkoxyamine radical cations. In this process, electron transfer between an excited state oxidant and a TEMPO-derived alkoxyamine substrate gives rise to a radical cation with a remarkably weak C?O bond. Spontaneous scission results in the formation of the stable nitroxyl radical TEMPO.as well as a reactive carbocation intermediate that can be intercepted by a wide range of nucleophiles. Notably, this process occurs under neutral conditions and at comparatively mild potentials, enabling catalytic cation generation in the presence of both acid sensitive and easily oxidized nucleophilic partners.
3-ARYL-5-SUBSTITUTED-ISOQUINOLIN-1-ONE COMPOUNDS AND THEIR THERAPEUTIC USE
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Page/Page column 199, (2015/03/28)
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted- 2/-/-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, e
