201607-63-8Relevant academic research and scientific papers
Photo-Induced ortho-C-H Borylation of Arenes through in Situ Generation of Rhodium(II) Ate Complexes
Araujo Dias, Ant?nio Junio,Nagashima, Yuki,Tanaka, Jin,Tanaka, Ken
supporting information, p. 11325 - 11331 (2021/08/03)
Photoinduced in situ "oxidation"of half-sandwich metal complexes to "high-valent"cationic metal complexes has been used to accelerate catalytic reactions. Here, we report the unprecedented photoinduced in situ "reduction"of half-sandwich metal [Rh(III)] complexes to "low-valent"anionic metal [Rh(II)] ate complexes, which facilitate ligand exchange with electron-deficient elements (diboron). This strategy was realized by using a functionalized cyclopentadienyl (CpA3) Rh(III) catalyst we developed, which enabled the basic group-directed room temperature ortho-C-H borylation of arenes.
NITROGENOUS HETEROCYCLIC AROMATIC COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION THEREOF, AND APPLICATION THEREOF
-
Paragraph 0090; 0092, (2019/06/12)
Provided are a nitrogenous heterocyclic aromatic compound, a preparation method therefor, a pharmaceutical composition thereof, and an application thereof. The nitrogenous heterocyclic aromatic compound can be used for treating and/or preventing various diseases mediated by ALK5.
Synthesis of Chemically and Configurationally Stable Monofluoro Acylboronates: Effect of Ligand Structure on their Formation, Properties, and Reactivities
Noda, Hidetoshi,Bode, Jeffrey W.
supporting information, p. 3958 - 3966 (2015/04/14)
The recent disclosures of two classes of acylborons, potassium acyltrifluoroborates (KATs) and N-methyliminodiacetyl (MIDA) acylboronates, demonstrated that certain acylboron species can be both remarkably stable and uniquely reactive. Here we report new classes of ligands for acylboronates that have a significant influence on the formation, properties, and reactivities of acylboronates. Our systematic investigations identified a class of neutral, monofluoroboronates that can be prepared in a one step, gram-scale fashion from readily accessible KATs. These monofluoroboronates are stable to air, moisture, and silica gel chromatography and can be easily handled without any special precautions. X-ray crystallography, NMR spectroscopy, and HPLC studies showed that they are tetravalent, configurationally stable B-chiral acylboronates. Significantly, the ligands on the boronate allow for fine-tuning of the properties and reactivity of acylboronates. In amide-forming ligation with hydroxylamines under aqueous conditions, a considerable difference in reactivity was observed as a function of ligand structure. The solid-state structures suggested that subtle steric and conformational factors modulate the reactivities of the acylboronates.
Direct ortho-Hydroxylation of 2-Phenylpyridines using Palladium(II) Chloride and Hydrogen Peroxide
Yamaguchi, Tomoaki,Yamaguchi, Eiji,Tada, Norihiro,Itoh, Akichika
supporting information, p. 2017 - 2021 (2015/06/23)
Direct functionalization of the ubiquitous C-H bond is receiving much attention because complex structures can be formed from simple precursors. This paper reports a useful method for the direct hydroxylation of 2-phenylpyridines using palladium(II) chloride and aqueous hydrogen peroxide. In this method, hydrogen peroxide, which has high atom efficiency, is employed as the oxidant and phenol derivatives are generated via C-H activation.
Regioselective synthesis of 2-(2-hydroxyaryl)pyridines from the reactions of benzynes with pyridine N-oxides
Shaibu, Balagopal S.,Kawade, Rahul Kisan,Liu, Rai-Shung
, p. 6834 - 6839 (2012/11/07)
By modifying the conditions from those in Larock's reported synthesis of 3-(2-hydroxyaryl)pyridines from benzynes, and pyridine N-oxides, we altered the regioselectivity of the reaction toward an efficient synthesis of 2-substituted pyridines. The presenc
α1-Adrenoceptor agonists: The identification of novel α1A subtype selective 2′-heteroaryl-2-(phenoxymethyl)imidazolines
Bishop, Michael J.,Barvian, Kevin A.,Berman, Judd,Bigham, Eric C.,Garrison, Deanna T.,Gobel, Michael J.,Hodson, Stephen J.,Irving, Paul E.,Liacos, James A.,Navas, Iii, Frank,Saussy Jr., David L.,Speake, Jason D.
, p. 471 - 475 (2007/10/03)
Novel 2′-heteroaryl-2-(phenoxymethyl)imidazolines have been identified as potent agonists of the cloned human α1-adrenoceptors in vitro. The nature of the 2′-heteroaryl group can have significant effects on the potency, efficacy, and subtype selectivity in this series. α1A Subtype selective agonists have been identified.
