BILN 2061, a HCV protease inhibitor, is the first small molecule that was clinically validated for the treatment of Hepatitis C infection in human. Its large scale synthesis presented significant synthetic challenge for process chemists. This lecture will highlight the challenges and opportunities for scaling the ring-closing metathesis reaction, and provide an account of our process research that led to the first highly practical application of ring-closing metathesis in the pharmaceutical industry and that allowed for large-scale synthesis of BILN 2061 and closely-related analogs.  

Challenges and opportunities for scaling the ring-closing metathesis reaction: Development of a highly practical process for macrocyclic HCV protease inhibitors

246th National Meeting (2013)

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