Pharmacological evaluation of novel bioisosteres of an adamantanyl benzamide P2X7 receptor antagonist [PDF]
Adamantanyl benzamide 1 was identified as a potent P2X7R antagonist but failed to progress further due to poor metabolic stability. We describe the synthesis and SAR of a series of bioisosteres of benzamide 1 to explore improvements in the ...
Barron, Melissa L+13 more
core +3 more sources
Visible‐Light Enabled Synthesis of 1‐Aryl‐3‐Sulfonylmethyl‐1,2,4‐Triazoles by Arylazo Sulfones
Abstract We present a novel and highly efficient method for synthesizing polyfunctionalized 1,2,4‐triazoles. This approach leverages visible light and arylazo sulfones in combination with N‐vinyl amides, in the environmentally friendly solvent ethyl acetate.
Luca Nicchio+5 more
wiley +1 more source
Bifunctional organocatalysts for the asymmetric synthesis of axially chiral benzamides
Bifunctional organocatalysts bearing amino and urea functional groups in a chiral molecular skeleton were applied to the enantioselective synthesis of axially chiral benzamides via aromatic electrophilic bromination.
Ryota Miyaji+4 more
doaj +1 more source
Regioselective Palladaelectro‐Catalyzed Chlorination of Arenes in an Undivided Cell
Abstract Chloroarenes constitute fundamental building blocks in organic synthesis and are widely applied in the synthesis of bioactive compounds, fine chemicals, materials, natural products and pharmaceuticals. Electrochemical chlorination has been recognized as a promising synthetic method for accessing chloroarenes, but it has proved challenging to ...
Sudipta Ponra+3 more
wiley +1 more source
Ab-initio crystal structure analysis and refinement approaches of oligo p-benzamides based on electron diffraction data [PDF]
Ab-initio crystal structure analysis of organic materials from electron diffraction data is presented. The data were collected using the automated electron diffraction tomography (ADT) technique.
Brunklaus, Gunther+4 more
core +1 more source
Mannich Reaction of Secondary Benzylzinc Reagents: Synthesis of α,β‐Disubstituted β‐Arylethylamines
The organometallic Mannich multicomponent reaction (MCR) of secondary benzylzinc reagents is described. The final α,β‐disubstituted β‐arylethylamines are obtained in generally high yields. The reaction is however characterized by a general lack of diastereoselectivity. A possible explanation is provided.
Baptiste Leroux+6 more
wiley +1 more source
The title compound, C20H18N6O5·0.5C3H7NO, crystallized as a dimethylformamide (DMF) solvate. In the main molecule, the dihedral angle between the pyridodipyrimidine fused-ring system and the benzamide substituent is 82.26 (11)°.
Armen Ayvazyan
doaj +1 more source
Synthesis of Quinazoline and Quinazolinone Derivatives via Ligand-Promoted Ruthenium-Catalyzed Dehydrogenative and Deaminative Coupling Reaction of 2-Aminophenyl Ketones and 2-Aminobenzamides with Amines [PDF]
The in situ formed ruthenium catalytic system ([Ru]/L) was found to be highly selective for the dehydrogenative coupling reaction of 2-aminophenyl ketones with amines to form quinazoline products.
Arachchige, Pandula T. Kirinde+1 more
core +3 more sources
Production Of 11C‐Labeled Amides Via “In‐Loop” 11C‐Carbonylation
The current work utilizes carbon‐11 labelled aroyl dimethylaminopyridinium salts in a two‐step in‐loop carbonylative cross‐coupling reaction of aryl halides with [¹¹C]CO yielding a diverse range of carbon‐11 labelled primary benzamides with good to excellent yields.
Tanpreet Kaur+3 more
wiley +1 more source
2-Anilino-N-methyl-N-phenylbenzamide
The title compound, C20H18N2O, is composed of three aromatic rings, the dihedral angles between the phenyl and benzamide rings, and between the benzamide and aniline rings being 59.86 (9) and 46.57 (10)°, respectively.
Da-Bin Qin+2 more
doaj +1 more source