Employing a green and efficient 2,2,2trifluoroacetophenone-catalyzed oxidation of alkenes, which utilizes H2O2 as the green oxidant, a novel and sustainable synthesis of indolines and pyrrolidines was developed. This constitutes a cheap, general and environmentally-friendly protocol for the synthesis of substituted nitrogen-containing heterocycles. A variety of substitution patterns, both aroma...

The synthesis of novel fused heterocycles is based on reactions proceeding by the mechanism of the tert-amino effect, which generalizes cyclization of certain derivatives of 3-methyl-1-phenyl-2-pyrazolin-5-ones. Using this strategy a variety of fused heterocycles is obtained by the Knoevenagel condensation of 5-tert-amino-3-methyl-1-phenylpyrazolone-4-carboxal-dehyde 3 with active methylene com...

Saturated N-heterocycles are prevalent in biologically active molecules and are increasingly attractive scaffolds in the development of new pharmaceuticals. Unlike their aromatic counterparts, there are limited strategies for facile construction of substituted saturated N-heterocycles by convergent, predictable methods. In this Synopsis, we discuss recent advances in the synthesis of these comp...

While the exploitation of the Sharpless asymmetric dihydroxylation as the source of chirality in the synthesis of acyclic molecules and saturated heterocycles has been tremendous, its synthetic utility toward chiral benzo-annulated heterocycles is relatively limited. Thus, in the search for wider applications of Sharpless asymmetric dihydroxylation-derived diols for the synthesis of benzo-annul...

Readily available natural α-amino acids are one of nature's most attractive and versatile building blocks in synthesis of natural products and biomolecules. Peptides and N-heterocycles exhibit various biological and pharmaceutical functions. Conjugation of amino acids or peptides with N-heterocycles provides boundless potentiality for screening and discovery of diverse biologically active molec...

Cycloaddition reactions of alkynes are elegant, atom-efficient transformations for the synthesis of carbo- and heterocycles, mostly aromatic, involving the construction of challenging skeletons of complex molecules. Therefore significant efforts have recently been devoted to the development of novel methodologies, efficient strategies and different catalytic systems to broaden the scope of thes...

The chemoselective C−H functionalization of unprotected N-heterocycles is a challenging task in organic synthesis. Herein, we report on Brønsted-acid catalyzed reaction aryl/aryl diazoalkanes with to selectively allow for at the C3-position under mild conditions and short time without need protecting groups. general applicability this method was further expanded towards protected indole pyrrole...

N-Alkenyl carboxamides undergo gold-catalyzed intramolecular exo-hydroamination to form nitrogen heterocycles in excellent yield.

Solidphase organic synthesis is a rapidly expanding area of synthetic chemistry which is being widely exploited in the search for new medicinally important compounds by combinatorial techniques. In recent decades, a large number of reports related to solidphase synthesis of heterocycles have appeared owing to a wide variety of their biological activity. In this review, we report the important r...