Microwave-assisted sequential one-pot protocol to benzothiadiazin-3-one-1,1-dioxides via a copper-catalyzed N-arylation strategy

A microwave-assisted, sequential, one-pot protocol has been developed for the synthesis of a variety of benzothiadiazin-3-one-1,1-dioxides. This protocol utilizes a copper-catalyzed N-arylation of α-bromo-benzenesulfonamides with a number of amines to generate the corresponding 2-aminobenzenesulfonamides, which undergo cyclization to the desired sultams using carbonyl diimidazole (CDI). A range of conditions was evaluated for the key C–N bond formation step with tolerance toward functionalized amines

The Hillarys Transect (1): Seasonal and cross-shelf variability of physical and chemical water properties off Perth, Western Australia, 1996-98

A 27-month study of the water properties across the continental shelf off Perth, Western Australia (the Hillarys Transect ) has provided the first systematic inter-disciplinary climatology of the physical, chemical, optical and biological cycles across the shelf. This paper describes the main features of the seasonal and cross-shelf variability of the physical oceanography and chemistry, while companion papers discuss some of the links between the biology and physics of the regio

Reagent based DOS: A "Click, Click, Cyclize" strategy to probe chemical space

The synthesis of small organic molecules as probes for discovering new therapeutic agents has been an important aspect of chemical-biology. Herein we report a reagent-based, diversity-oriented synthetic (DOS) strategy to probe chemical and biological space via a “Click, Click, Cyclize” protocol. In this DOS approach, three sulfonamide linchpins underwent cyclization protocols with a variety of reagents to yield a collection of structurally diverse S-heterocycles. In silico analysis is utilized to evaluate the diversity of the compound collection against chemical space (PC analysis), shape space (PMI) and polar surface area (PSA) calculations