A simple and efficient TEMPO-mediated system for aerobic oxidative synthesis of 2-aryl benzoxazoles from readily available primary benzylic hetero amines is presented in one pot. The reaction proceeds through the ring-opening followed by condensation with benzylamines. These metal-free, straightforward reactions worked well a wide range substrates, yielding moderate to good yields under mild co...

2-p-substituted phenyl-2-benzimidazolo acetonitriles (1a-5a) were prepared by the reaction of benzimidazole , p-substituted benzaldehydes and Sodium cyanide. A series of 2-(α-p -Substituted phenyl-αbenzimidazolo) methyl benzoxazoles (1b-5b) were synthesized by the reaction of 2-p-substituted phenyl-2benzimidazolo acetonitrile(1a-5a) and o-aminophenol in presence of Conc. HCl. These compounds we...

Asymmetric hydroheteroarylation of alkenes represents a convenient entry to elaborated heterocyclic motifs. While chiral acids are known to mediate asymmetric addition of electron-rich heteroarenes to Michael acceptors, very few methods exploit transition metals to catalyze alkylation of heterocycles with olefins via a C-H activation, migratory insertion sequence. Herein, we describe the develo...

Based on our contemporary studies on the structures of biologically active molecules, we focus our attention on the aliphatic chain and its conformation. That flexible spacer definitely influenced the balanced position of all pharmacophoric points in molecules of biological ligands. The one atomic linker and two or three atomic spacers with one heteroatom X = O, S, CH2, NH have been taken into ...

A series of lipophilic 2-substituted 5,7-di-tert-butylbenzoxazoles was prepared in average yields by the reaction of 3,5-di-tert-butyl-1,2-benzoquinone with amino acids and dipeptides bearing N-terminal glycine. Dipeptides having other N-terminal amino acids undergo oxidative deamination. 5,7-Di-tert-butylbenzoxazoles have shown activity against Mycobacterium tuberculosis and some nontuberculou...