Beyond the technology innovation, we were convinced that there is a need to influence the future of the pharmaceutical industry, by breaking with traditional research paradigm of medicinal chemistry practice and allow chemists to remotely guide chemical syntheses as a virtual extension of their own lab. During assembly of the automated Synthesis  and purification Laboratory (ASPL) at Eli Lilly and Co., we recognized novel opportunities to tap into the creative synthetic talents of chemists from anywhere in the world. This poster highlights our partnership with University of Notre Dame group  for the design and syntheses of imidazopyridines with impressively potent anti-tuberculosis activity and how the inception of this tool coincided well with a renewed focus on the collaborative research model through the Fully Integrated Pharmaceutical network (FIPNet) model.  While preliminary SAR studies were carried out using traditional manual synthetic techniques, the chemistry was readily adapted to the ASPL and allowed further expansion of SAR.  Collaborative efforts, including high throughput screening (University of Illinois, Chicago), development and utilization of separate sensitive assays (IDRI) and determination of in vivo pharmacokinetics at Lilly, have accelerated studies.  The combined results indicate that imidazo[1,2-a]pyridine-3-carboxamides are an exciting new class of potent, selective anti-TB agents that merit additional development opportunities

Synthesis of an imidazopyridine library using the automated synthesis laboratory (ASL)

246th National Meeting (2013)

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