How small is big enough? Accelerating Innovation in Multi-Catalysis with High Throughput Experimentation (HTE)
High Throughput Experimentation (HTE) has emerged as an important tool to assist and accelerate the productivity of the synthetic chemist. This iterative process of design, execution, data analysis, and hit identification enables rapid exploration of conditions for reaction discovery and optimization. In this article, we highlight the powerful use of HTE within the fields of multi-catalysis and new route synthesis, with a particular focus on late-stage functionalization.
Traditional chemical research is characterized by a paradigm in which chemists explore and refine reaction conditions through a process of trial and error. However, emerging research paradigms are profoundly impacting organic chemistry by accelerating scientific discovery, reshaping interdisciplinary collaboration and optimizing the use of resources.
HTE allows the execution of large numbers of experiments to be conducted in parallel reducing the effort per experiment compared to traditional methods. These tools and techniques originated in the field of biology in the 1950s[1] and have since matured to the point where high-throughput experimentation has become standard practice in biology laboratories worldwide. In contrast, the state of chemical HTE is far less developed, and the techniques much less frequently employed. Continuous efforts are needed to reduce scale and increase the density of chemical experiments[2]. In addition, only a selection of few industrial laboratories routinely practices chemical HTE, and the technique is extremely rare in academic settings. This disparity in HTE adoption between biology and chemistry is largely due to engineering challenges. Unlike biology and biochemistry experiments, which are typically conducted in aqueous media at or near room temperature, chemical experiments often required a wide range of solvents and temperatures, and frequently involve heterogeneous mixtures that are difficult to array and agitate in a well plate format. The use of volatile organic solvents also introduces additional challenges of material compatibility and evaporative solvent loss. However, in the last decade, significant progress, much progress has been made to adapt equipment for synthetic chemistry use[3].
