Conferencia Plenaria del Prof. J.V. Sinisterra en el 3rd EuCheMS Chemistry Congress

Molecular Life Sciences
(Biostructure, Biopolymers and their Conjugates, Medicinal Chemistry, Biocatalysis and Biomaterials, Impact of Analytical Chemistry in Life/Bio Sciences)

Plenary Speaker: Barbara Imperiali (USA)
Fluorescent Tools for Chemical Biology

Biostructure, Biopolymers and their Conjugates
Convener: Juan Fontecilla-Camps (FR)
Invited Speakers:

Rolf Thauer (DE)

The Structure of the Nickel Enzyme that Catalyzes the Anaerobic Oxidation of Methane in Archaea
Dino Moras (FR)
Allosteric Control of Dimerisation in Nuclear Receptors of Hormones
Eric Westhof (FR)
RNA Modules and the Assembly of RNA Architecture
Rebecca Wade (DE)
Simulation and Design of Dynamic Tunnels in Enzymes
Péter Tompa (HU)
Intrinsically Disordered Proteins in Cellular Function and Disease
Yoshihito Watanabe (JP)
Design of Organometallo-Enzymes

Medicinal Chemistry
Convener: Roberto Pellicciari (IT)
Invited Speakers:

Maria Flocco (UK)

Biophysical Methods in Medicinal Chemistry Design
Tudor I. Oprea (USA)
The Art of Mapping Drug-Target Interactions
Gisbert Schneider (DE)
Molecular Design Patterns
Maurizio Botta (IT)
Design and Synthesis of HIV-1 Inhibitors
Rasmus Clausen (DK)
Development of Specific Glutamate Receptor Ligands
Timothy M. Willson (USA)
Open Access Chemical Probes

Biocatalysis and Biomaterials
Convener: Manfred Reetz (DE)
Invited Speakers:

Alan Berry (UK)

Novel Enzymes Based on an Aldolase Scaffold
Uwe T. Bornscheuer (DE)
Protein Engineering Tools for Enantioselective Biocatalysis
Donald Hilvert (CH)
Designer Enzymes
Dick B. Janssen (NL)
Engineered Dehalogenases in Enantioselective Biocatalysis
José Vicente Sinisterra (ES)
Industrial Biotransformations in Green Solvents
Pierre Monsan (FR)
Molecular Engineering of a Transglucosidase for the Catalysis of Specific Synthesis

Impact of Analytical Chemistry in Life/Bio Sciences
Convener: Jeremy Nicholson (UK)
Invited Speakers:

R. Graham Cooks (USA)

Applications of Desorption Electrospray Ionisation
Paul Thomas (UK)
Breath Analysis for Disease Diagnosis
Frank Breitling (DE)
Applications of High Density Peptide Arrays in Cancer Studies
Fred Regnier (USA)
Protein Biomarkers of Oxidative Stress
Jeremy Nicholson (UK)
Statistical Spectroscopic Approaches in Systems Biology and Medicine

Pace et al, Green Chemistry 2010

2-Methyltetrahydrofuran as a suitable green solvent for phthalimide functionalization promoted by supported KF

Vittorio Pace, Pilar Hoyos, María Fernández, José V. Sinisterra and Andrés R. Alcántara
Green Chem., 2010, 12, 1380-1382

Abstract

An efficient chemoselective nitrogen functionalization of phthalimides by using KF-Alumina in 2-methyltetrahydrofuran, a solvent obtained from renewal sources, is described.

http://dx.doi.org/10.1039/c0gc00113a

Pace et al, Journal Organic Chemistry 2010

Improved Arndt-Eistert Synthesis of alpha-Diazoketones Requiring Minimal Diazomethane in the Presence of Calcium Oxide as Acid Scavenger.

V. PACE, G. VERNIEST, J.V. SINISTERRA, A.R. ALCANTARA, N. DE KIMPE

Abstract

A practical methodology to obtain α-diazoketones through an improved Arndt−Eistert synthesis is described. The method allows the efficient transformation of acid halides using a stoichiometric amount of diazomethane in the presence of calcium oxide, without concomitant ketene or haloketone formation. The obtained α′-brominated-α-diazoketones were employed as suitable substrates for the synthesis of interesting α-arylamino-α′-halomethylketones.

http://dx.doi.org/10.1021/jo101105g

Pace et al, Synthesis 2010

First General Route to Substituted α-Arylamino-α′-chloropropan-2-ones by Oxidation of N-Protected Aminohalohydrins: The Importance of Disrupting Hydrogen Bond Networks

Vittorio Pace, Álvaro Cortés Cabrera, María Fernández, José V. Sinisterra, Andrés R. Alcántara

Abstract

The presence of a network of intra- and intermolecular hydrogen bonds in β-arylamino alcohols, confirmed by both IR spectroscopy and computer modeling, inhibits their oxidation to the corresponding α-amino ketones. A straightforward protocol, including highly regioselective protection (as carbamates) and subsequent oxidation with Dess-Martin periodinane, affords near quantitative yields of the desired N-protected ketones, which upon mild treatment with iodotrimethylsilane leads to a series of differently functionalized α-arylamino-α′-chloro ketones.

http://dx.doi.org/10.1055/s-0030-1257938

A.R. Alcántara, J.M. Sanchez-Montero, An. R. Acad. Nac. Farm., 2010

Hydrolases use in the preparation of drugs and homochiral intermediates

Andrés R. Alcántara León, José María Sánchez Montero

Abstract

The excellent regio and steroselectivity of biocatalysts, combined with their environmental friendly behaviour, make possible to carry out under biocatalytical conditions many processes which, conducted on strictly classical methodologies, would demand expensive and tedious protection and de-protection steps. In this work we review some examples in which hydrolases (the most useful enzymes in the Biotransformations field) catalyse different reactions for synthesizing only the therapeutically essential stereoisomer of different homochiral building blocks for drugs. Thus, processes leading to antiviral, anticancer, antihypertensive or antiinflammatory drugs, along with many others, are described, remarking the versatility and utility of the biocatalysts in the above-mentioned processes.

http://www.analesranf.com/index.php/aranf/article/view/1091