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Accelerated Process Development of Pharmaceuticals:  Selective Catalytic Hydrogenations of Nitro Compounds Containing Other Functionalities

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 a...

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Bibliographic Details
Published in:Organic process research & development 2004-05, Vol.8 (3), p.469-476
Main Authors: Hoogenraad, Marcel, van der Linden, Johannes B., Smith, Alan A., Hughes, Bob, Derrick, Andrew M., Harris, Laurence J., Higginson, Paul D., Pettman, Alan J.
Format: Article
Language:English
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Summary: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.
ISSN:1083-6160
1520-586X
DOI:10.1021/op0341667