BACKGROUND Azaheterocycles are an important class of compounds because of their highly potent medicinal activities, and the imidazole subcategory is of special interest in regard to drug discovery research. FINDINGS An expeditious synthetic protocol of 2-aryl-4-phenyl-1H-imidazoles has been accomplished by reacting phenylglyoxal monohydrate, ammonium acetate, and aldehyde under sonication. Fo...

A diastereoselective and enantioselective construction of 2,3-disubstituted 1,4-dicarbonyl compounds is reported. Nishiyama's RuPhebox complex (2.0 mol% catalyst loading) serves as a chiral Lewis acid in conjunction with BrCCl3 base for the oxidative homocoupling 2-acyl imidazoles via stereocontrolled reaction intermediate Ru enolates situ brominated imidazoles. Cleavage achiral imidazole auxil...

Two new monobasic tridentate O?N?N donor ligands, HL1 (I) and HL2 (II) have been obtained in two steps by reacting phenylhydrazine salicylaldehyde or 3,5-di-tert-butylsalicylaldehyde then the resulting compounds with 2-chloromethylbenzimidazole presence of triethylamine. The reaction [VIVO(acac)2] these ligands a 1:1 molar ratio dry methanol led to formation homogeneous oxidovanadium(IV) comple...

An efficient palladium-catalyzed asymmetric hydrogenation of fluorinated aromatic pyrazol-5-ols has been developed via capture of the active tautomers. A wide variety of 2,5-disubstituted and 2,4,5-trisubstituted pyrazolidinones have been synthesized with up to 96% and 95% ee, respectively. The hydrogenation pathway includes Brønsted acid promoted tautomerization of pyrazol-5-ols and Pd-catalyz...

A new stereoselective synthesis of trisubstituted alkenes is developed. Hydrophosphoryloxylation of haloalkynes provides Z-alkenyl halophosphates, which undergo Pd-catalyzed consecutive cross-coupling reactions to afford regio- and stereodefined trisubstituted alkenes.