Organocatalytic kinetic resolution of 1,5-dicarbonyl compounds through a retro-Michael reaction

The pharmaceutical chemical industry has long used kinetic resolution to obtain high-value compounds. Organocatalysis has recently been added to this strategy, allowing for the resolution of racemic mixtures with low catalyst loadings and mild reaction conditions. This research focuses on the kineti...

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Main Authors: James Guevara-Pulido, Fernando González-Pérez, José M. Andrés, Rafael Pedrosa
Format: Article
Language:English
Published: Beilstein-Institut 2025-03-01
Series:Beilstein Journal of Organic Chemistry
Subjects:
Online Access:https://doi.org/10.3762/bjoc.21.34
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author James Guevara-Pulido
Fernando González-Pérez
José M. Andrés
Rafael Pedrosa
author_facet James Guevara-Pulido
Fernando González-Pérez
José M. Andrés
Rafael Pedrosa
author_sort James Guevara-Pulido
collection DOAJ
description The pharmaceutical chemical industry has long used kinetic resolution to obtain high-value compounds. Organocatalysis has recently been added to this strategy, allowing for the resolution of racemic mixtures with low catalyst loadings and mild reaction conditions. This research focuses on the kinetic resolution of 1,5-dicarbonyl compounds using a retro-Michael reaction, co-catalyzed at room temperature with 20 mol % of the Jørgensen–Hayashi catalyst and PNBA. The study highlights the importance of conducting the kinetic resolution at a concentration of approximately ten millimolar (mM) to prevent the Michael retro-Michael equilibrium from affecting the process.
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publisher Beilstein-Institut
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series Beilstein Journal of Organic Chemistry
spelling doaj-art-b8c9865f14414a2f8a7dcaec32cedbbf2025-08-20T03:09:28ZengBeilstein-InstitutBeilstein Journal of Organic Chemistry1860-53972025-03-0121147348210.3762/bjoc.21.341860-5397-21-34Organocatalytic kinetic resolution of 1,5-dicarbonyl compounds through a retro-Michael reactionJames Guevara-Pulido0Fernando González-Pérez1José M. Andrés2Rafael Pedrosa3Química Farmacéutica, Grupo Investigación en Química Aplicada INQA, Universidad El Bosque, Cra 7b Bis No 132 – 11, Bogotá, Colombia Instituto Universitario CINQUIMA y Departamento de Química Orgánica, Facultad de Ciencias, Universidad de Valladolid, Paseo Belén 7, 47011-Valladolid, Spain Instituto Universitario CINQUIMA y Departamento de Química Orgánica, Facultad de Ciencias, Universidad de Valladolid, Paseo Belén 7, 47011-Valladolid, Spain Instituto Universitario CINQUIMA y Departamento de Química Orgánica, Facultad de Ciencias, Universidad de Valladolid, Paseo Belén 7, 47011-Valladolid, Spain The pharmaceutical chemical industry has long used kinetic resolution to obtain high-value compounds. Organocatalysis has recently been added to this strategy, allowing for the resolution of racemic mixtures with low catalyst loadings and mild reaction conditions. This research focuses on the kinetic resolution of 1,5-dicarbonyl compounds using a retro-Michael reaction, co-catalyzed at room temperature with 20 mol % of the Jørgensen–Hayashi catalyst and PNBA. The study highlights the importance of conducting the kinetic resolution at a concentration of approximately ten millimolar (mM) to prevent the Michael retro-Michael equilibrium from affecting the process.https://doi.org/10.3762/bjoc.21.341,5-dicarbonylequilibriumkinetic resolutionorganocatalysisretro-michael
spellingShingle James Guevara-Pulido
Fernando González-Pérez
José M. Andrés
Rafael Pedrosa
Organocatalytic kinetic resolution of 1,5-dicarbonyl compounds through a retro-Michael reaction
Beilstein Journal of Organic Chemistry
1,5-dicarbonyl
equilibrium
kinetic resolution
organocatalysis
retro-michael
title Organocatalytic kinetic resolution of 1,5-dicarbonyl compounds through a retro-Michael reaction
title_full Organocatalytic kinetic resolution of 1,5-dicarbonyl compounds through a retro-Michael reaction
title_fullStr Organocatalytic kinetic resolution of 1,5-dicarbonyl compounds through a retro-Michael reaction
title_full_unstemmed Organocatalytic kinetic resolution of 1,5-dicarbonyl compounds through a retro-Michael reaction
title_short Organocatalytic kinetic resolution of 1,5-dicarbonyl compounds through a retro-Michael reaction
title_sort organocatalytic kinetic resolution of 1 5 dicarbonyl compounds through a retro michael reaction
topic 1,5-dicarbonyl
equilibrium
kinetic resolution
organocatalysis
retro-michael
url https://doi.org/10.3762/bjoc.21.34
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AT josemandres organocatalytickineticresolutionof15dicarbonylcompoundsthrougharetromichaelreaction
AT rafaelpedrosa organocatalytickineticresolutionof15dicarbonylcompoundsthrougharetromichaelreaction