Metal Free Scalable Synthesis of Fluorinated Indole and Benzofuran Structures

This technology is a novel one step method to generate fluorinated aryl groups for use in various other reactions.

Background:
There are few alternative existing methods to treat arrhythmia. Originally, there were a slew of powerful anti arrhythmic drugs on the market which had the potential to treat the cardiovascular condition. However, the majority of these drugs were revealed to actually increase mortality rates rather than decrease them. This left only two major compounds in the field, dronedarone and amiodarone.

 

Another way to treat arrhythmia is the pacemaker. While a pacemaker can monitor the heart to identify electrical activity while being able to modulate the rhythm of the heart itself, it is only a temporary fix. Unlike its drug counterparts, a pacemaker does not address the core problem of arrhythmia, it only addresses the symptoms.

 

Advantages:

  • No metal involved, making synthesis potentially cheaper
  • Scalable to large quantity synthesis
  • Intermediate compound can be used in other reactions as well

Applications:

  • Anti-arrhythmic compounds
  • New method for the production of benzofuran, a key component in a variety of existing anti-arrhythmic compounds
  • Could be used to enhance the production of existing compounds that use benzofuran as a component
    • Key benzofuran based molecules for enhancement include dronedarone and amiodarone 
Patent Information: