SULFONAMIDES
The Catalytic Synthesis of Sulfonamides
| Coordinatore | THE CHANCELLOR, MASTERS AND SCHOLARS OF THE UNIVERSITY OF OXFORD
Organization address
address: University Offices, Wellington Square contact info |
| Nazionalità Coordinatore | United Kingdom [UK] |
| Totale costo | 209˙033 € |
| EC contributo | 209˙033 € |
| Programma | FP7-PEOPLE
Specific programme "People" implementing the Seventh Framework Programme of the European Community for research, technological development and demonstration activities (2007 to 2013) |
| Code Call | FP7-PEOPLE-2011-IEF |
| Funding Scheme | MC-IEF |
| Anno di inizio | 2012 |
| Periodo (anno-mese-giorno) | 2012-09-17 - 2014-09-16 |
Partecipanti
| # | ||||
|---|---|---|---|---|
| 1 |
THE CHANCELLOR, MASTERS AND SCHOLARS OF THE UNIVERSITY OF OXFORD
Organization address
address: University Offices, Wellington Square contact info |
UK (OXFORD) | coordinator | 209˙033.40 |
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Obiettivo del progetto (Objective)
'Sulfonamides are functional groups that feature in a significant number of pharmaceuticals, with applications in a variety of indications. Conventional syntheses of sulfonamides usually involve two or three synthetic operations, and often feature low-yielding steps. The chemistry involved also limits the substrates that can be converted to sulfonamides. This proposal seeks to develop an alternative synthesis of sulfonamides; the proposed synthesis will be achieved in a single operation, employ readily available reagents and substrates, and be conducted under mild conditions. The key to the proposed synthesis is to employ a three-component synthesis involving the catalytic combination of an aryl halide, an amine and sulfur dioxide. Achieving the synthesis in a single operation will have significant advantages in terms of waste production, energy required, as well as the time needed to prepare the desired sulfonamides. These are important considerations for both small scale discovery synthesis, as well as the large scale synthesis of these materials. The developed methodology should also be applicable to the preparation of related sulfonate esters and sulfones. The latter stages of the project will explore the application of the developed method to the synthesis or selected target structures that are difficult to access using conventional methods, and to the synthesis of heterocycles.'
Introduzione (Teaser)
Organic chemists have investigated several new methods to create sulfonamides, a chemical group important for manufacturing pharmaceutical drugs.
Descrizione progetto (Article)
Sulfonamides are a functional chemical group found in antibiotics, antidiuretics and various other medicines. They are expensive and difficult to produce, prompting researchers to investigate cheaper and simpler methods to create sulphonamides.
The EU-funded project 'The catalytic synthesis of sulfonamides' (SULFONAMIDES) investigated several such methods. Researchers specifically looked to make sulfonamide synthesis less complex, using milder conditions and readily available precursors.
First, researchers designed the overall system, and optimised it by adjusting various parameters like the catalyst, reaction temperature and source of sulphur dioxide. This approach did not, however, yield any sulfonamide product.
SULFONAMIDES then investigated a different set of starting materials; unfortunately, this approach also failed to yield any useful products.
Finally, the project tested another alternative approach, which converted common N-aminosulfonamides into sulfonamides. This approach was a success in that it required only mild reaction conditions and no catalyst, making the process cheaper and more environmentally friendly.
The research carried out by SULFONAMIDES is vital to improve the sustainability and cost effectiveness of sulfonamide synthesis. This work will contribute to cheaper drug manufacture and thus improved well-being in general.