| Viernes
/ Friday / 15 |
| 08:15 |
Recogida
de Acreditaciones / Registration |
| 08:45 |
Bienvenida / Opening and welcome addresses
Porqué este Simposio / Why this Symposium |
| Session 1 |
Moderador/Chairperson: Jesús Ezquerra
Lilly Research Laboratories. Alcobendas, Madrid, Spain |
| 09:00 |
Manfred T Reetz
Director of Department of Synthetic Organic Chemistry, Max-Planck-Institut
fur Kohlenforschung. Mülheim an der Ruhr, Germany |
|
Evolución Dirigida de Enzimas Enantioselectivos
/Directed Evolution of Enantioselective Enzymes
Applying the methods of directed evolution, i.e. the appropriate
combination of gene mutagenesis and expression and high-throughput
ee-assays, the enantioselectivity of enzymes as catalysts in
organic chemistry can be controlled. This fundamentally new
approach to asymmetric catalysis is independent of any knowledge
concerning the enzyme structure, yet important mechanistic lessons
can be learned from directed evolution. |
| 10:00 |
Barbara Imperiali
Department of Chemistry, Massachusetts Institute of Technology.
Cambridge, Massachusetts, USA |
|
Herramientas Químicas para el Estudio
de Sistemas Biológicos Complejos / Chemical Tools
for the Study of Complex Biological Systems
This presentation will discuss the development and application
of new chemical probes for studying complex biological systems.
In the area of signal transduction, new strategies including
the preparation of synthetic and semi-synthetic protein probes
for interrogating the specific function of proteins involved
in directed cell migration and cell cycle control have been
developed. Due to the essential signaling roles played by intracellular
kinase-mediated phosphorylation in key cellular processes, the
focus of these studies is on protein kinases as strategic targets.
Access to chemical probes to monitor phosphorylation events
will enable to define the spatial and temporal characteristics
of protein kinases and phosphoprotein mediators in complex cellular
pathways. These probes include both environment-sensitive and
chelation enhanced fluorophores for interrogating phosphorylation-dependent
protein-protein interactions and caged phosphoamino acids for
examining phosphorylation-mediated cellular functions. |
| 11:00 |
Café/Coffee |
| 11:30 |
Carlos F Barbas III
Professor. The Skaggs Institute for Chemical Biology, The
Scripps Research Institute. California, USA |
|
De los Anticuerpos Catalíticos a la
Organocatálisis / From Catalytic Antibodies to Organocatalysis
One of the ultimate goals in organic chemistry is the catalytic
asymmetric assembly of simple and readily available precursor
molecules into stereochemically complex products. As chemists,
we often turn to nature for inspiration concerning stereochemically
complex, diverse, and functional molecules. Indeed, the directed
asymmetric assembly of simple achiral building blocks into stereochemically
complex molecules like carbohydrates and polyketides has long
been the purview of nature’s enzymes. Our approach to
this problem began in 1997 when we embarked upon studies exploring
the similarity between proline and a novel class of aldolase
antibodies we had developed earlier. Recently, these studies
have allowed us to describe the first direct organocatalytic
asymmetric ketone and aldehyde additions in aldol, Michael,
Mannich, and Diels-Alder reaction manifolds. Significantly,
these studies were originally designed for antibody catalysis
years before. This lecture will summarize the contributions
of this laboratory to creating and converting enzymatic enamines,
and in some cases imines, into a versatile catalytic asymmetric
strategy powered by small organic molecules. |
| 12:30 |
James E Audia
Executive Director, Discovery Chemistry Research & Technologies,
Lilly Research Laboratories. Indianapolis, USA |
|
Hacia una Pharma mas Productiva / Toward
a more ‘Productive’ Pharma
Jim is a native of South Carolina and obtained his
Ph.D. in Organic Chemistry from the University of South Carolina
in 1986 in the laboratories of Jim Marshall. Over the course
of his career, Jim’s scientific endeavors have contributed
to 8 clinical candidates for development at Lilly. He is a
named inventor on more than 80 issued US Patents and has published
extensively in the synthetic and medicinal chemistry of serotonergic
agonists, antagonists and uptake inhibitors, steroid 5 a-reductase
inhibitors, and g secretase inhibitors. |
| 13:30 |
Almuerzo
/ Lunch |
| SESION 2 |
Moderador/Chairperson: Julio Álvarez
Builla
Departamento Química Orgánica, Facultad
de Farmacia, Universidad de Alcalá de Henares. Spain
|
| 15:00 |
Tom Welton
Department of Chemistry, Imperial College London. London,
UK
|
|
Líquidos Iónicos a Temperatura
Ambiente en Síntesis y Catálisis / Room-Temperature
Ionic Liquids in Synthesis and Catalysis
In the last decade there has been an explosion of interest in
the use of room-temperature ionic liquids as solvents for synthesis
and catalysis. Much of the interest has centered on their on
their potential as ‘green’ solvents. This lecture
goes beyond this to see how ionic liquids can be used to change
synthetic and catalytic processes. Examples will be shown of
ionic liquids being used to effect the yields, rates and selectivities
of reactions. |
| 16:00 |
William R Roush
Executive Director of Medicinal Chemistry, The Scripps Research
Institute. Florida, USA |
|
Nuevos Métodos Síntéticos
y Aplicaciones a la Síntesis Total de Productos Naturales
Biológicamente Activos / New Synthetic Methods and
Applications to the Total Synthesis of Biologically Active Natural
Products
Recent studies on the development of new synthetic methodology will
be presented, along with applications towards the total synthesis of
stereochemically complex, biologically active natural products. The
specific examples highlighted will be selected from our recent
efforts on the total synthesis of 13-deoxytedanolide, amphidinol 3,
and amphidinolides C, E and F.
|
| 17:00 |
Miguel A Yus
Profesor. Departamento Química Orgánica, Facultad
de Ciencias, Universidad de Alicante. Spain |
|
Nuevas Metodologías basadas en Litiaciones
Catalizadas por Arenos / New Methodologies based on an Arene-Catalyzed
Lithiation
The arene-catalyzed lithiation is an efficient methodology in
order (1) to prepare organolithium compounds starting from non-halogenated
materials, (2) to reductively open different heterocycles yielding
functionalized organolithium intermediates, (3) to generate
organodilithium synthons by heteroatom-lithium exchange, and
(4) to activate other metals, for instance nickel, able to perform
the reduction of several organic functionalities. |
| 18:00 |
Café
/ Coffee |
18:30
Mesa redonda /
Round table |
Síntesis
de Alto Rendimiento / High Throughput Synthesis
Moderador/Chairperson: Fernando Albericio
Barcelona Biomedical Research Institute, Universidad de Barcelona. Spain |
José Manuel Villalgordo.
VillaPharma Research S.L. Spain (Moléculas pequeñas)
Joaquín Pastor. Janssen-Cilag. Spain (Diversidad
en síntesis)
Rafael Ferritto. Lilly
Research Laboratories. Spain (Automatización en
síntesis)
Antoni Molins. Almirall-Prodesfarma.
Soain (Quimioinformática) |
|
|
| Sábado
/ Saturday / 16 |
| SESSION
3 |
Moderador/Chairperson: Rafael Ferrito
Lilly Research Laboratories. Alcobendas, Madrid, Spain |
| 08:45 |
Takashi Takahashi
Professor. Department Applied Chemistry, Graduate School of
Science and Engineering, Tokyo Institute of Technology. Tokyo,
Japan |
|
Síntesis en Fase Sólida y en
Disolución de Muestrotecas de Productos Naturales / Solid
and Solution-Phase Synthesis of Natural Products Libraries
The combinatorial synthesis of a 122-member macrosphelide library
using a palladium-catalyzed carbonylation on a polymer-support
and a protected oligosaccharide library by one-pot glycosylation
will be presented. |
| 09:40 |
Claudio Palomo Nicolau
Profesor. Departamento Química Orgánica, Facultad
de Química, Universidad del País Vasco. San
Sebastián, Spain |
|
Reacciones Asistidas por Auxiliaries Quirales:
Inspiración para el desarrollo de Procesos Catalíticos
Enantioselectivos /Chiral Auxiliaries-Assisted Reactions:
Inspiration for Developing Catalytic Enantioselective Processes
For effective chirality transfer from covalently bonded chiral
appendages to the reacting centre there is often the need to
implement concepts such as proximity, concavity, conformational
rigidity, and/or high order in transition state. Aimed at these
goals, we have explored the potential of a'-hydroxy ketones
for metal chelation, using the camphor skeleton as the chiral
appendage. Thus far, the application of this principle to aldol,
Mannich, Diels-Alder, and related reactions has been pursued.
From these designing elements, we have subsequently developed
achiral a '-hydroxy enones as advantageous templates in Lewis
acid-catalyzed enantioselective transformations |
| 10:35 |
Café
/ Coffee |
11:00
|
C Oliver Kappe
Professor. Department of Chemistry, University of Graz. Austria |
|
Microondas en Síntesis Orgánica
/ Microwaves in Organic Synthesis
This presentation will describe recent progress in the
application of controlled microwave-assisted synthesis from
our laboratory. The subjects covered will include transition
metal-catalyzed reactions, heterocycle preparation, solid-phase
synthesis, and the use of polymer-supported reagents for automated
library synthesis. |
11:55
Mesa redonda /
Round table
|
Retos para la I+D
en España: el caso de la Química Médica
/ Challenges for R&D in Spain: the case of Medicinal
Chemistry
Moderador/Chairperson: José A Gutiérrez
Fuentes
Fundación Lilly, Spain |
Robert W Armstrong. Lilly Research
Laboratories. Indianapolis, USA
Miquel A Pericàs.
Instituto Catalán de Investigación Química.
Tarragona, Spain
Carlos Martínez Alonso.
Consejo Superior de Investigaciones Científicas,
Spain
Jorge Martín Juárez. Crystal
Pharma / Ragactives, S.A. Valladolid, Spain
Nazario
Martín. Real Sociedad Española de Química,
Spain |
  |
|
| 13:00 |
Closure Address / Conferencia
de Clausura
Moderador/Chairperson: Julio Álvarez Builla |
| |
Javier de Mendoza
Group Leader Institute of Chemical Research of Catalonia (ICIQ).
Tarragona, Spain |
|
Autoensamblaje: una Aproximación a
la Complejidad Química Inspirada en la Biología
/ Self-assembly: a Bio-inspired approach to Chemical Complexity
The spontaneous self-assembly of molecular building blocks into highly structured, discrete supramolecular architectures constitutes a bio-inspired approach to chemical complexity, overcoming some of the problems associated to synthesis based solely on covalent bonds, with the added virtues of economy, cooperativity, self-error-checking, and efficiency, typical for reversible, dynamic processes. We present herein examples of rosette-like and capsular aggregates based on multiple hydrogen bonds, metal coordination, electrostatic and hydrophobic forces built around calixarene and related molecular platforms. |
| 13:50 |
Despedida / Farewell
Julio Alvarez Builla, Fernando Albericio, Jesús Ezquerra,
José A Gutiérrez Fuentes |
| |
La acreditación supondrá la asistencia a todas
las sesiones plenarias y, a las mesas redondas