Autor: |
Harrie Straatman, Jeroen A. F. Boogers, Laurent Lefort, André H.M. de Vries, Johannes G. de Vries, John Janssen, Robert Jan Vijn, Thijs Kuilman |
Přispěvatelé: |
Stratingh Institute of Chemistry, Synthetic Organic Chemistry |
Jazyk: |
angličtina |
Rok vydání: |
2010 |
Předmět: |
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Zdroj: |
Organic Process Research & Development, 14(3), 568-573. AMER CHEMICAL SOC INC |
Popis: |
High throughput screening was used to find a cost-effective and scalable catalyst for the asymmetric hydrogenation of a sterically demanding enamide as an intermediate towards a new potent melanocortin receptor agonist useful in the treatment of obesity. Lessons drawn from the testing of a first library of 96 chiral monodentate phosphoramidites led to the design of a second focused library of 16 chiral ligands, allowing the discovery of a new efficient catalyst. This catalyst was based on rhodium and a bulky monodentate phosphite ligand. The catalyst was scaled up and used in the kilogram production of the desired bulky chiral amide. |
Databáze: |
OpenAIRE |
Externí odkaz: |
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