DURING A STUDY on the metabolism of histidine in a child affected with histidinemia (Beauvais, P., and Humbel, R., to be published), we became interested in the chromatography of imidazoles. In this disease the urine contains numerous imidazoles: histidine and its metabolites, imidazole-pyruvic, imidazole-lactic and imidazole-acetic acids and N-acetylhistidine.’I developed a chromatographic met...

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...

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.

The completely N1-selective Pd-catalyzed arylation of unsymmetric imidazoles with aryl halides and triflates is described. This study showed that imidazoles have a strong inhibitory effect on the in situ formation of catalytically-active Pd(0)-ligand complex. The efficacy of the N-arylation reaction was improved drastically by the use of pre-activated solution of Pd2(dba)3 and L1. From these fi...