synthesis and catalytic functionalization of biologically active indoles

Preface
The search for drugs is an old human dream and constitutes still a real challenge
for scientists. Already alchemists sought for the one drug, the Elixir healing all
human ailments. Today, the growing knowledge in pharmacy and biology makes
the search for novel drugs complex and difficult. Therefore it is not surprising that
organic chemists are interested in the development of easy accessible synthesis
to new potential drugs.
An interesting target for drug design is the serotonin (5-hydroxytryptamine
5-HT) receptor ligand. It is one of the oldest known neurotransmitter in the central
nervous system and responsible for controlling our body temperature, mood,
sexual drive and sleep rhythm. This hormone is implicated in many diseases like
schizophrenia, anxiety, obesity and Alzheimer’s disease. Based on the indole
skeleton it is an interesting building block which is of importance to the
pharmaceutical industry. The application of new 5-HT receptor ligands against
these diseases demanded an easy access to indole derivatives and wide scope of
functionalization.
Metal-catalyzed cross-coupling reactions have profoundly changed the protocols
for the construction of natural products, building blocks of supermolecular
chemistry and lead compounds in medicinal chemistry from simpler entities. The
development of efficient new carbon-carbon bond forming reactions by metalcatalyzed
cross-coupling has continued to progress dramatically and some of the
reactions are finding industrial application on the multipleton scale. Furthermore
new protocols for C-N and C-O couplings have been introduced and find particular
use in the synthesis of biologically active compounds for pharmaceutical
application.
Cross-coupling reactions play an important role in the development of new 5-HTreceptor
ligands as well. Finding the optimized conditions in C-N- or C-O- bond
forming processes is one of the key steps in the synthesis of new indole
derivatives.
VII