Abstract In the present study, 3- p -methoxybenzyl/ m -chlorobenzyl/phenyl-4-(3-methyl-2-thienylmethyleneamino)-4,5-dihydro-1 H -1,2,4-triazol-5-ones were obtained from reaction between 3-methylthiophene-2-carbaldehyde and three different 4-amino-(3- -chlorobenzyl/phenyl)-4,5-dihydro-1 -1,2,4-triazole-5-ones. order to compare experimental theoretical values, geometric parameter, electronic, non...

This review highlights the biological importance of many polysubstituted nitro-prolines and -pyrrolidines. Their preparation using asymmetric 1,3-dipolar cycloadditions of azomethine ylides with nitroalkenes using diastereoselective and enantioselective strategies is described remarking the scope and main features of each one.

Polysubstituted phenols are efficiently assembled from one aldehyde and two different methyl ketones in a one-pot operation via a newly base-induced regiospecific [4 + 1 + 1] annulation and sequential metal-free oxidative aromatization using molecular oxygen (from air) as the sole oxidant at room temperature.

A systematic investigation on the metal-free, Cope-type hydroamination reactivity of hydrazides and analogues is reported. Optimization of the hydrazide structure resulted in more facile intramolecular reactivity and enabled intermolecular reactions of alkenes, thus providing a direct approach to polysubstituted hydrazides.

In the further research and synthesis of highly bioactive 3-methylrhodanine derivatives, preparation benzylidene rhodanines followed by bicyclization to form pyrazole compounds has been undertaken. Using a convenient simple method, twelve have synthesized including six rhodanine derivatives ranging from good excellent yield, with four phenylhydrazone two at low yield. The structures all were el...

An effective gold-catalyzed intermolecular nitrene transfer by the reaction of 2H-azirines and ynamides is reported, which provides highly substituted pyrroles in a straightforward manner. This transformation proceeds under mild conditions and gives the polysubstituted pyrroles in good-to-excellent yields. Preliminary results indicate that a nongold carbenoid pathway is preferred for current py...

Regioselective synthesis of polysubstituted benzofurans using a copper catalyst and molecular oxygen from phenols and alkynes in a one-pot procedure has been reported. The transformation consists of a sequential nucleophilic addition of phenols to alkynes and oxidative cyclization. A wide variety of phenols and alkynes can be used in the same manner.

The first TiCl(4)-mediated condensation of secondary amides with aldehydes and ketones has been achieved. The reaction proceeds at room temperature and is complete within 5 h in most cases. The optimized procedure used 5 equiv of an amine base hinting that the in situ activation of both the amide and the Lewis acid is required. The reaction affords polysubstituted (E)-enamides.

In the title compound, C(33)H(34)N(6)O(6), the dihydro-benzimidazol-2-one ring system is essentially planar (r.m.s. deviation = 0.021 Å). The cyclo-hexane ring adopts a chair conformation. In the 5-(biphenyl-2-yl)-2H-tetra-zole fragment, the tetra-zole ring is twisted away from the attached benzene ring by 35.73 (11)° and the two benzene rings form a dihedral angle of 68.00 (9)°. An intra-molec...

We report an efficient method to prepare polysubstituted 3-hydroxypyridines from amino acids, propargyl alcohols, and arylboronic acids. The process involves Pd(0)-catalyzed anti-selective arylative cyclizations of N-propargyl-N-tosyl-aminoaldehydes with acids (“anti-Wacker”-type cyclization), oxidation the resulting 5-substituted-3-hydroxy-1,2,3,6-tetrahydropyridines 3-oxo derivatives, elimina...