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Chemoselective C-4 aerobic oxidation of catechin derivatives catalyzed by the trametes villosa laccase/1-hydroxybenzotriazole system: synthetic and mechanistic aspects (Articolo in rivista)
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- Chemoselective C-4 aerobic oxidation of catechin derivatives catalyzed by the trametes villosa laccase/1-hydroxybenzotriazole system: synthetic and mechanistic aspects (Articolo in rivista) (literal)
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- 2011-01-01T00:00:00+01:00 (literal)
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- 10.1021/jo101886s (literal)
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R. Bernini, F. Crisante, P. Gentili, F. Morana, M. Pierini, M. Piras (2011)
Chemoselective C-4 aerobic oxidation of catechin derivatives catalyzed by the trametes villosa laccase/1-hydroxybenzotriazole system: synthetic and mechanistic aspects
in Journal of organic chemistry
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- R. Bernini, F. Crisante, P. Gentili, F. Morana, M. Pierini, M. Piras (literal)
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- Dipartimento di Agrobiologia e Agrochimica, Università degli Studi della Tuscia, Via S. Camillo De Lellis, 01100 Viterbo, Italy,
Dipartimento di Chimica and IMC-CNR Sezione Meccanismi di Reazione,
Universita' degli Studi La Sapienza, P. le A. Moro 5, I-00185 Roma, Italy, and
Dipartimento di Chimica e Tecnologia del Farmaco, Universita' degli Studi La Sapienza,
P. le A. Moro 5, I-00185 Roma, Italy (literal)
- Titolo
- Chemoselective C-4 aerobic oxidation of catechin derivatives catalyzed by the trametes villosa laccase/1-hydroxybenzotriazole system: synthetic and mechanistic aspects (literal)
- Abstract
- J. Org. Chem. 2011, 76, 820-832 Published on Web 01/04/2011 DOI: 10.1021/jo101886s
r2011 American Chemical Society
pubs.acs.org/joc
Chemoselective C-4 Aerobic Oxidation of Catechin Derivatives Catalyzed
by the Trametes villosa Laccase/1-Hydroxybenzotriazole System:
Synthetic and Mechanistic Aspects
Roberta Bernini,+,* Fernanda Crisante,+ Patrizia Gentili,?,* Fabio Morana,?
Marco Pierini,§ and Monica Piras§
+Dipartimento di Agrobiologia e Agrochimica, Università degli Studi della Tuscia, Via S. Camillo De Lellis,
01100 Viterbo, Italy, ?Dipartimento di Chimica and IMC-CNR Sezione Meccanismi di Reazione,
Università degli Studi La Sapienza, P. le A. Moro 5, I-00185 Roma, Italy, and
§Dipartimento di Chimica e Tecnologia del Farmaco, Università degli Studi La Sapienza,
P. le A. Moro 5, I-00185 Roma, Italy
berninir@unitus.it; patrizia.gentili@uniroma1.it
Received October 6, 2010
Catechin derivatives were oxidized in air in the presence of the Trametes villosa laccase/1-hydroxybenzotriazole
(HBT) system in buffered water/1,4-dioxane as reactionmedium. The oxidation products, flavan-
3,4-diols and the corresponding C-4 ketones, are bioactive compounds and useful intermediates for the
hemisynthesis of proanthocyanidins, plant polyphenols which provide beneficial health properties for
humans. Determinations of oxidation potentials excluded that catechin derivatives could be directly
oxidized by laccase Cu(II), while it resulted in the H-abstraction from benzylic positions being promptly
promoted by the enzyme in the presence of the mediator HBT, the parent species producing in situ the
reactive intermediate benzotriazole-N-oxyl (BTNO) radical. A remarkable and unexpected result for the
laccase/HBT oxidative system has been the chemoselective insertion of the oxygen atom into the C-4-H
bond of catechin derivatives.Mechanistic aspects of the oxidation reaction have been investigated in detail
for the first time in order to corroborate these results. Since the collected experimental findings could not
alone provide information useful to clarify the origin of the observed chemoselectivity, these data were
expressly supplemented with information derived by suitable molecular modeling investigations. The
integrated evaluation of the dissociation energies of theC-Hbonds calculated both by semiempirical and
DFT methods and the differential activation energies of the process estimated by a molecular modeling
approach suggested that the observed selective oxidation at the C-4 carbon has a kinetic origin. (literal)
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