56540-70-6Relevant articles and documents
Ni-Catalyzed Direct Carboxylation of Aryl C?H Bonds in Benzamides with CO2
Pei, Chunzhe,Zong, Jiarui,Li, Bin,Wang, Baiquan
supporting information, p. 493 - 499 (2021/12/08)
The direct carboxylation of inert aryl C?H bond catalyzed by abundant and cheap nickel is still facing challenge. Herein, we report the Ni-catalyzed direct carboxylation of aryl C?H bonds in benzamides under 1 atm of CO2 to afford various methyl carboxylates or phthalimides, dealing with different post-processing. The reaction displays excellent functional group tolerance and affords moderate to high carboxylation yields under mild conditions. Detail mechanistic studies suggest that a Ni(0)?Ni(II)?Ni(I) catalytic cycle may be involved in this reaction. (Figure presented.).
Palladium-Catalyzed Chlorocarbonylation of Aryl (Pseudo)Halides Through In Situ Generation of Carbon Monoxide
Bismuto, Alessandro,Boehm, Philip,Morandi, Bill,Roediger, Sven
supporting information, p. 17887 - 17896 (2020/08/19)
An efficient palladium-catalyzed chlorocarbonylation of aryl (pseudo)halides that gives access to a wide range of carboxylic acid derivatives has been developed. The use of butyryl chloride as a combined CO and Cl source eludes the need for toxic, gaseous carbon monoxide, thus facilitating the synthesis of high-value products from readily available aryl (pseudo)halides. The combination of palladium(0), Xantphos, and an amine base is essential to promote this broadly applicable catalytic reaction. Overall, this reaction provides access to a great variety of carbonyl-containing products through in situ transformation of the generated aroyl chloride. Combined experimental and computational studies support a reaction mechanism involving in situ generation of CO.
Rational Development of Novel Activity Probes for the Analysis of Human Cytochromes P450
Sellars, Jonathan D.,Skipsey, Mark,Sadr-ul-Shaheed,Gravell, Sebastian,Abumansour, Hamza,Kashtl, Ghasaq,Irfan, Jawaria,Khot, Mohamed,Pors, Klaus,Patterson, Laurence H.,Sutton, Chris W.
, p. 1122 - 1128 (2016/07/12)
The identification and quantification of functional cytochromes P450 (CYPs) in biological samples is proving important for robust analyses of drug efficacy and metabolic disposition. In this study, a novel CYP activity-based probe was rationally designed and synthesised, demonstrating selective binding of CYP isoforms. The dependence of probe binding upon the presence of NADPH permits the selective detection of functionally active CYP. This allows the detection and analysis of these enzymes using biochemical and proteomic methodologies and approaches.
GEMINAL SUBSTITUTED QUINUCLIDINE AMIDE COMPOUNDS AS AGONISTS OF ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTORS
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Paragraph 00905-00906, (2016/07/05)
The present invention relates to novel geminal substituted quinuclidine amide compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of α7- nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
Nickel-Catalyzed Boron Insertion into the C2-O Bond of Benzofurans
Saito, Hayate,Otsuka, Shinya,Nogi, Keisuke,Yorimitsu, Hideki
supporting information, p. 15315 - 15318 (2016/12/09)
Treatment of benzofurans with bis(pinacolato)diboron and Cs2CO3 under nickel-NHC catalysis resulted in the insertion of a boron atom into the C2-O bond of benzofurans to afford the corresponding oxaborins. The scope of benzofuran substrates is wide, and the reactions proceeded without loss of functional groups such as fluoro, methoxy, and ester that are potentially reactive under nickel catalysis. The boron-inserted products proved to be useful building blocks and subsequently underwent a series of transformations, one of which led to the synthesis of fluorescent π-expanded oxaborins.
A convenient synthesis of 2-phenylbenzofuran derivatives with potent testosterone 5α-reductase inhibitory activities
Ishibashi, Koki,Nakajima, Katsuyoshi,Nishi, Takahide
, p. 2669 - 2675 (2007/10/03)
A convenient method for the synthesis of 4-[2-(benzo[b]furan-2-yl)phenyloxy]butyric acid derivatives with a carbamoyl group at the 5 or 6 position of the benzofuran ring showing potent 5α-reductase inhibitory activities was developed. Oxazolin-2-ylbenzofu
Aminoalkylindoles: Structure - Activity Relationships of Novel Cannabinoid Mimetics
Eissenstat, Michael A.,Bell, Malcolm R.,D'Ambra, Thomas E.,Alexander, E. John,Daum, Sol J.,et al.
, p. 3094 - 3105 (2007/10/02)
Aminoalkylindoles (AAIs) are a novel series of cannabinoid receptor ligands.In this report we disclose the structural features of AAIs which are important for binding to this receptor as measured by inhibition of binding of 3H>Win 55212-2 (5).Functional activity in the mouse vas deferens is also noted and used to distinguish agonists from potential antagonists.The key structural features for potent cannabinoid activity in this series are a bicyclic (naphthyl) substituent at the 3-position, a small (H) substituent at the 2-position, and an aminoethyl (morpholinoethyl) substituent at the 1-position.A 6-bromo analog, Win 54461 (31), has been identified as a potential cannabinoid receptor antagonist.Modeling experiments were done to develop a pharmacophore and also to compare AAI structures with those of classical cannabinoids.The fact that the cannabinoid AAIs arose out of work on a series of cyclooxygenase inhibitors makes sense now that an endogenous cannabinoid ligand has been identified which is a derivative of arachidonic acid.Because of their unique structures and physical properties, AAIs provide useful tools to study the structure and function of the cannabinoid receptor(s).
