Facile, fast and safe process development of nitration and bromination reactions using continuous flow reactors

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Org. Process Res. Dev., 2009, 13 (4), pp 698–705

  • Jacques Pelleter* and Fabrice Renaud
  • AstraZeneca, Centre de recherches, Z. I. La Pompelle, BP1050, 51689 Reims cedex 2, France

In this OPRD paper, chemists at AstraZeneca used Syrris flow chemistry pumps to perform a pyrazole nitration at 0.82 g/h (88% yield, 100% purity).

Abstract: Chemists working in a pilot plant often face safety issues during scale-up operations. With the help of emerging microfluidic applications and microdevices, running hazardous, highly exothermic or potentially unstable reactions can be easily transposed into a safe continuous flow mode. This paper describes how a potentially hazardous pyrazole nitration and the bromination of a variety of electron-rich heteroaromatic substrates were efficiently performed using a cheap and easily available system for bench chemists. Advantages of the continuous flow mode in organic synthetic chemistry will be exemplified by the large-scale production of raw materials under safe, green and reproducible conditions.

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This paper was published using the Syrris Asia Syringe Pumps.