Total Synthesis of Natural Products and
Chemical Innovation
Our Laboratory is focused on the total synthesis of
naturally complex molecular architectures. Under this basic topic our
group seeks to invent novel general synthetic methods as answers to
longstanding chemical problems.
1.
Divergent Total Synthesis
of Natural Products.
Total synthesis of naturally occurring compounds with complex molecular
architectures, useful biological properties and interesting mechanism of
biological action, becomes an engine for discovery that drives the field
of organic chemistry.
Constant target selection and creative retrosynthetic analyses based on
their biosynthesis is the key of inspiration for their total
synthesis, targeting in revealing missing synthetic pathways to
longstanding chemical problems.
Under this
basic concept we are trying to uncover "common
synthetic scaffolds" that can lead to efficient divergent total
synthesis of natural products.

"A tour de force"
utilizing this method provided a lbrary of furo-sesquiterpenes and
sesquiterpene lactones with more than 60 members. Libraries are
constantly enriched and biologically screened focusing on their
anticancer activity.

Libraries based on
common synthetic scaffolds has also been prepared for:
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Pyridone alkaloids
(22 members)
|
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Pyrrole imidazole
alkaloids (underway)
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2. Discovery
and Development of Novel Reactions for Target-Oriented Synthesis.
New reaction discovery is the most important research activity in the
area of organic chemistry, and target-directed reaction discovery is one
of the best strategies for identifying important transformations to be
developed.
Focus on CH-activation:
Currently, we
are particularly interested in CH-activation-alkylation of heterocycles
and the CH-oxidation of hydrocarbons.
 |
Alkenylation
of 4-hydroxy-2-pyridones:
Development of the first Heck-type reaction on the 4-hydroxy-2-pyridone
core enabling the utilization of both activated and unactivated alkenes |

 |
Arylation of 4-hydroxy-2-pyridones:
Development of the first CH-arylation of 4-hydroxy-2-pyridone core. |

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CH-Oxidations:
Development of methods utilizing molecular oxygen as the sole oxidant
for the CH-oxidation of hydrocarbons. |
Our group is
also proud to be part of the
CHAOS-COST Action (CH-Activation in Organic
Synthesis)

3.
Biological Evaluation.
Although our group is certainly oriented in the fundamental research of
organic synthesis several collaborations are established with field experts for
the biological evaluation of the newly synthesized compounds.
Collaborations are ongoing
with:
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Prof. Ioannis Vizirianakis;
Pharmaceutical Department, Aristotle University of Thessaloniki
(anticancer activity of sesquiterpenoids) |
 |
Prof. Dimitrios Fatouros;
Pharmaceutical Department, Aristotle University of Thessaloniki (sesquiterpenoids
as enhancers) |
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Prof. Dimitrios Georgiadis;
Department of Chemistry, National University of Athens |
 |
Prof.
Enrique Gómez
Bengoa, Facultad de Químicas Donostia - San Sebastián, UPV-EHU
(DFT calculations on cycloisomerization reactions) |
|