Evaluation of logPo/w values of drugs from some molecular structure calculation software
The iridium‐catalyzed asymmetric hydrogenation of several N‐sulfonyl allyl amines is reported. All substrates can be easily obtained by the Ir‐catalyzed isomerization of N‐tosylaziridines reported previously. The commercially available threonine‐derived phosphinite (UbaPHOX) iridium complex has been...
| Autores: | , , , , , |
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| Tipo de recurso: | artículo |
| Estado: | Versión publicada |
| Fecha de publicación: | 2014 |
| País: | España |
| Institución: | Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya) |
| Repositorio: | Recercat. Dipósit de la Recerca de Catalunya |
| OAI Identifier: | oai:recercat.cat:2445/143378 |
| Acceso en línea: | https://hdl.handle.net/2445/143378 |
| Access Level: | acceso abierto |
| Palabra clave: | Lipofília Química farmacèutica Lipophilicity Pharmaceutical chemistry |
| Sumario: | The iridium‐catalyzed asymmetric hydrogenation of several N‐sulfonyl allyl amines is reported. All substrates can be easily obtained by the Ir‐catalyzed isomerization of N‐tosylaziridines reported previously. The commercially available threonine‐derived phosphinite (UbaPHOX) iridium complex has been found to be the best catalyst for this catalytic application, affording β‐methyl amines with good to excellent ee values (up to 94%). The synthetic potential of this novel methodology was demonstrated by the formal synthesis of Lorcaserin and LY‐404187. |
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