Download The Search of a new synthetic route for a SLV compound

The Search of a new synthetic route for a SLV compound
The goal of my research project was to find, develop and scale up a new synthetic
route for a Liver X Receptor ligand which is being developed by Abbott Healthcare for
the treatment of Arthrosclerosis.
Summary
Liver X Receptor (LXR) ligands are very interesting compounds as they influence the
cholesterol levels in the human body. Cholesterol is one of the major risk factors in
Arthrosclerosis and therefore it is thought that LXR ligands are possible drugs for the
treatment of Arthrosclerosis.
Abbott Healthcare BV has found a compound which shows LXR activity being a
potential drug against Arthrosclerosis. A chemical production process is needed to
supply clinical studies with drug substance resulting ultimately in a commercial
production process.
A new synthetic route has been found, developed and a scale up production has been
performed resulting in 32.5 kg drug substance in high quality and high yield. This new
route has a number of advantages compared to the old route:
 Higher atom efficiency (84 compared to 67%)
 Lower cost price
 Lower number of steps (4 compared to 6)
 Higher overall yield (60% compared to 27%)
 No metal are used in the synthesis (old route used Pd)