Process Safety Considerations for the Supply of a High-Energy Oxadiazole IDO1-Selective Inhibitor
Theodore A. Martinot, Michael J. Ardolino, Lu Chen, Yu‐hong Lam, Chaomin Li, Matthew L. Maddess, Daniel J. Muzzio, Ji Qi, Josep Saurí, Zhiguo J. Song, Lushi Tan, Thomas P. Vickery, Jingjun Yin, Ralph Zhao · Organic Process Research & Development · 2019
The development of a stereospecific synthesis of a IDO1-selective inhibitor is described. The synthetic strategy toward enabling early discovery efforts along with additional findings pertaining to process safety that limited scalability are outlined. A convergent approach that supported the synthesis of material suitable for early preclinical and/or good laboratory practice toxicology studies and avoided the formation of key high-energy intermediates is summarized.