Pyrazolines and pyrazolidines represent two important classes of five-membered N-heterocycles found in many natural products, agrochemicals and biologically active molecules. Over the past decades, tremendous efforts have been devoted to the development of efficient methods for efficient construction of these scaffolds. However, the catalytic asymmetric synthesis of pyrazolines and pyrazolidine...

Seven-membered heterocyclic [1,2,5]triazepane and [1,2,5]oxadiazepane derivatives were synthesized as candidate structures for application in drug discovery in place of conventional piperazine or morpholine moieties, offering multiple sites for modification with functional groups. We first synthesized the N-protected heterocycles, and then confirmed their utility by synthesizing analogues of th...

The synthesis of a range of fluorinated heterocycles is described via a Lewis acid-mediated Prins-type cyclisation.

The direct arylation of benzo[b]furan, benzo[b]thiophene, and indole has been studied by using aromatic bromides as the aryl source. The protocol employing common reagents and a Pd catalyst has led to the regioselective arylation of these heterocycles at the 2-position. A range of functional groups were tolerated, providing quick access to a variety of arylated benzo-fused heterocycles that wou...

Indole and the related heterocycles have emerged as efficient building blocks for the creation of novel anion receptors. This chapter focuses on the employment of indoles, carbazoles, and indolocarbazoles in the creation of molecular clefts, macrocycles, oligomers, and sensors. The majority of these structures utilize the heterocyclic NH as a hydrogen bond donor in binding to anions of various ...

We report here a practical and efficient synthesis of α-aminophosphonic acid incorporated into 1,2,3,4-tetrahydroquinoline and 1,2,3,4-tetrahydroisoquinoline heterocycles, which could be considered to be conformationally constrained analogues of pipecolic acid. The principal contribution of this synthesis is the introduction of the phosphonate group in the N-acyliminium ion intermediates, obtai...

An efficient one-pot synthesis of 1,2,3-triazole derivatives of dihydropyrimidinones has been developed using two multicomponent reactions. The aldehyde-1,2,3-triazoles were obtained in good yields from in situ-generated organic azides and O-propargylbenzaldehyde. The target heterocycles were synthesized through the Biginelli reaction in which the aldehyde-1,2,3-triazoles reacted with ethyl ace...

This research was done in order to investigate the anticancer activity of boronic acid arylidene heterocycles. Boronic acid, heterocycles, and aryl compounds have all independently exhibited various anti-microbial properties and have shown potential to be used in pharmaceuticals for the treatment of viruses and cancers. Using a one-step protocol developed by Dr. Murray, several different arylhe...