1226571-52-3Relevant academic research and scientific papers
Gold-catalyzed 1,2-oxoarylations of nitriles with pyridine-derived oxides
Karad, Somnath Narayan,Liu, Rai-Shung
, p. 5444 - 5448 (2014)
We report the first success in the gold-catalyzed oxoarylations of nitriles with pyridine-derived N-oxides using gold carbenes as initiators. These oxoarylations were also achieved satisfactorily in intermolecular three-component oxidations, including diverse alkenyldiazo esters, nitriles, and pyridine-based oxides. Spill the (car)benes: Reported herein is the first successful gold-catalyzed oxoarylation of nitriles with pyridine-derived N-oxides using gold carbenes as initiators (see scheme; DCE=1,2-dichloroethane, IPr=1,3-bis(diisopropylphenyl)imidazol-2-ylidene). These oxoarylations were also achieved satisfactorily in intermolecular three-component oxidations using a variety of alkenyldiazo esters, nitriles, and pyridine-based N-oxides.
Nickel-Catalyzed C(sp3)-H Functionalization of Benzyl Nitriles: Direct Michael Addition to Terminal Vinyl Ketones
Zhang, Ninghui,Zhang, Chunli,Hu, Xiaoping,Xie, Xin,Liu, Yuanhong
supporting information, p. 6004 - 6009 (2021/07/31)
An efficient nickel(0)-catalyzed addition of benzyl nitriles to terminal vinyl ketones via C(sp3)-H functionalization has been developed. The reaction provides a novel and efficient protocol for the synthesis of α-functionalized benzyl nitriles with a wide range of structural diversity under mild reaction conditions while obviating the use of a strong base. The work might be potentially useful toward the development of an enantioselective variant using chiral nitrogen ligands.
Synthesis of ortho-Diamino-Functionalized 1-Arylnaphthalenes through Nickel-Catalyzed Cyclization of Ynamide-Benzylnitriles with Organoboronic Acids
Hu, Xiaoping,Lv, Peizhuo,Zhang, Ninghui,Liu, Yuanhong
supporting information, p. 7949 - 7954 (2021/10/12)
A nickel-catalyzed highly regioselective addition/cyclization of ynamide-benzylnitriles with organoboronic acids has been developed. The reaction offers an attractive route for the construction of diamino-functionalized 1-arylnaphthalenes, which is difficult to synthesize by other methods. In addition, a wide range of functional groups are tolerated in this reaction.
Palladium(II)-Catalyzed Cascade Reactions of Ene-Ynes Tethered to Cyano/Aldehyde: Access to Naphtho[1,2- b]furans and Benzo[ g]indoles
Jash, Moumita,De, Sukanya,Pramanik, Subhendu,Chowdhury, Chinmay
supporting information, p. 8959 - 8975 (2019/08/12)
An efficient palladium(II)-catalyzed cascade reaction of ene-yne substrates carrying cyano/aldehyde group is described. It involves successive hetero- and benz-annulations in one pot via trans-oxo/aminopalladation onto alkyne, followed by 1,2-addition to
Discovery of Potent and Orally Bioavailable GPR40 Full Agonists Bearing Thiophen-2-ylpropanoic Acid Scaffold
Li, He,Huang, Qi,Chen, Cheng,Xu, Bin,Wang, He-Yao,Long, Ya-Qiu
supporting information, p. 2697 - 2717 (2017/04/21)
The free fatty acid receptor GPR40 is predominantly expressed in pancreatic β-cells and enhances insulin secretion in a glucose dependent manner. Therefore, GPR40 agonists are possible novel insulin secretagogues with reduced or no risk of hypoglycemia for the treatment of type 2 diabetes mellitus (T2DM). Chemically and structurally diverse GPR40 agonists with high safety are pursued for the clinical development of GPR40-based pharmacotherapeutics. Herein we report our design and discovery of a new chemotype of GPR40 agonists free of the typical phenylpropanoic acid scaffold. The thiophen-2-ylpropanoic acid containing GPR40 modulators functioned as full agonists with high-efficacy response (Emax) and reduced lipophilicity. Significantly, the lead compound in this series, (R)-7k, exhibited more potent in vitro glucose-stimulated insulin secretion and in vivo glucose-lowering effects (10 mg/kg, po) than the GPR40 partial agonist TAK-875, which was once in phase III clinical trials, and high selectivity over the relevant receptors GPR120 and PPARγ.
One-pot procedure for the synthesis of unsymmetrical diarylalkynes
Severin, Rene,Reimer, Jessica,Doye, Sven
supporting information; experimental part, p. 3518 - 3521 (2010/07/17)
Unsymmetrical diarylalkynes are accessible by a one-pot procedure from two different aryl halides and (trimethylsilyl)acetylene. The three-component coupling is initialized by a Pd/Cu-catalyzed Sonogashira coupling of an aryl halide with (trimethylsilyl)a
