Accelerated Process Development of Pharmaceuticals: Selective Catalytic Hydrogenations of Nitro Compounds Containing Other Functionalities
Organic Process Research & Development2004Vol. 8(3), pp. 469–476
Citations Over TimeTop 18% of 2004 papers
Marcel Hoogenraad, Johannes B. van der Linden, Alan A. Smith, Bob Hughes, Andrew Derrick, Laurence J. Harris, Paul Higginson, Alan Pettman
Abstract
The hydrogenation of three different pharmaceutical nitro-containing compounds has been studied using high-throughput experimentation (HTE) methods. Significant improvements to the existing reactions were obtained for two of the examples. Each reaction exhibits distinct features regarding activity and chemoselectivity. The best catalyst and reaction conditions found were remarkably different for each of the reactions. For one of the reactions, larger-scale studies are presented, which show that the screening reactions provided a fast and reliable indicator of the most promising reaction conditions.
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