Multistep automated synthesis of pharmaceuticals

Multistep automated pharmaceutical syntheses have been a long-term industrial goal. Automation not only enables the rapid and highly efficient preparation of organic compounds by eliminating the physical barriers, but also endow chemists with more time for critical thinking by relieving them from laborious work. With the growing demand for fast and efficient synthesis of active pharmaceutical ingredients (APIs) for drug development, several efforts have been made in various subfields to improve the universality and capability of automation in multistep synthesis. This review highlights the recent development of automated iterative synthesis, automated digitalized batch synthesis, automated solid-phase synthesis (SPS)-flow synthesis, automated radial synthesis, as well as automated multistep continuous-flow synthesis and how they complement each other in the automated synthesis of pharmaceuticals.

Automated summary

The automation of pharmaceutical synthesis has been a long-term goal in the industry, as it allows for rapid and efficient preparation of organic compounds and frees chemists from laborious work. Efforts have been made to improve the universality and capability of automation in multistep synthesis, with a focus on automated iterative synthesis, automated digitalized batch synthesis, automated SPS-flow synthesis, automated radial synthesis, and automated multistep continuous-flow synthesis. This review highlights the recent development of these methods and their complementarity in the automated synthesis of pharmaceuticals.