A modular lead-oriented synthesis of diverse piperazine, 1,4-diazepane and 1,5-diazocane scaffolds.

Piperazines are found widely in commercially-available compounds and bioactive molecules (including many drugs). However, in the vast majority of these molecules, the piperazine ring is isolated (i.e.

Modular, gold-catalyzed approach to the synthesis of lead-like piperazine scaffolds.

Ring-opening of cyclic sulfamidates with propargylic sulfonamides yielded substrates for a gold-catalyzed cyclization to yield tetrahydropyrazines. Manipulation of the tetrahydropyrazines, by reduction or using multicomponent reactions, yielded piperazine scaffolds in which substitution of the carbon atoms was varied. Such scaffolds may have value in the synthesis of novel screening compounds with lead-like molecular properties.

Synthesis of iridium and ruthenium complexes with (N,N), (N,O) and (O,O) coordinating bidentate ligands as potential anti-cancer agents.

Several Ru-arene and Ir-Cp* complexes have been prepared incorporating (N,N), (N,O) and (O,O) coordinating bidentate ligands and have been found to be active against both HT-29 and MCF-7 cell lines. By incorporating a biologically active ligand into a metal complex the anti-cancer activity is increased.

Rhodium-catalysed isomerisation/formal 1,3-dipolar cycloaddition cascades to fused-ring heterocycles.

Fused ring heterocycles were synthesised via the rhodium catalysed isomerisation/regio and stereoselective 1,3-dipolar cycloaddition cascades in good yields.

Iridium catalysed chemoselective alkylation of 2'-aminoacetophenone with primary benzyl type alcohols under microwave conditions.

2'-Aminoacetophenone was chemoselectively alkylated with a range of substituted benzyl, heteroaryl alcohols to afford either the corresponding C- or N- alkylated products in good yield.

Regioselective synthesis of N-aminoisoindolones and mono-N- and di-N,N'-substituted phthalazones utilizing hydrazine nucleophiles in a palladium-catalyzed three-component cascade process.

A palladium-catalyzed three-component cascade process for the synthesis of isoindolone and phthalazone derivatives is reported. The cascade process involves carbonylation of an aryl iodide/Michael acceptor to give an acylpalladium species which is intercepted by a hydrazine nucleophile. Intramolecular Michael addition follows to give either N-aminoisoindolones or mono- N- and di-N,N'-phthalazones depending on whether a monosubstituted or 1,2-disubstituted hydrazine nucleophile is used.

Sequential one-pot bimetallic Ir(III)/Pd(0) catalysed mono-/bis-alkylation and spirocyclisation processes of 1,3-dimethylbarbituric acid and allenes.

Microwave assisted indirect functionalization of alcohols with 1,3-dimethylbarbituric acid followed by spirocyclisation employing a sequential one-pot Ir(III)/Pd(0) catalysed process, involving the formation of three new C-C bonds, one spirocyclic ring and one di- or tri-substituted exocyclic alkene, is described.

Novel synthesis of fused isoxazolidines via a palladium catalysed allene insertion-intramoleculer 1,3-dipolar cycloaddition cascade reaction.

A one pot, three component palladium catalysed allenation of aryl iodides, in combination with a nitrone cycloaddition, leads to formation of fused isoxazolidines, creating two rings, two stereocentres and one tetrasubstituted carbon centre.