High throughput electrosynthesis for enhanced drug discovery via light-powered smart microelectronics

Abstract OWiC Technologies' Fast Track project aims to introduce an innovative, user-friendly platform for high- throughput electrosynthesis to accelerate the discovery of novel small-molecule drugs. Traditional synthetic methods used in drug discovery are limited in the scope of reactions they can promote and the types of bioactive compounds they can prepare. Moreover, many complex medicinal agents require resource-intensive, multi-step synthesis with hazardous chemicals, making them economically and environmentally inefficient. In recent years, electrosynthesis has gained recognition as an enabling synthetic technology with the potential to substantially enhance researchers' ability to access novel compounds and accelerate drug discovery efforts. However, its adoption in the pharmaceutical industry remains limited due to the complexity of existing reactors and the specialized expertise required to operate them. Additionally, these setups are incompatible with high-throughput synthesis and screening. To address these challenges, OWiC Technologies will develop Smart Photoelectronics for Electrochemical Synthesis (SPECS)—a cutting-edge technology designed to enable nonspecialists in medicinal chemistry to seamlessly adopt electrochemical reactions in their R&D efforts. SPECS are miniature microelectronic chips that can be easily integrated into commercial 96- and 384-well plates containing microliter volumes of reactant solutions. These devices use small silicon photodiodes to generate electric currents upon visible light exposure, powering on-chip electrodes to drive electrosynthesis in a wireless fashion and eliminating the need for traditional wired equipment. This breakthrough will enable high throughput electrosynthesis with unparalleled efficiency and flexibility, allowing researchers to control redox reactions through precisely programmed current or voltage inputs. Since SPECS can seamlessly integrate into existing workflows for high- throughput experimentation, drug developers can effortlessly adopt electrosynthesis for rapid preparation of new compound libraries, streamlining drug discovery. OWiC has received positive feedback from potential customers, highlighting the technology’s potential to dramatically improve the scalability and user-friendliness of electrochemistry, while enabling the creation of previously unattainable drug molecules. Specific Phase I objectives include: 1) Developing SPECS with voltage and current control, 2) Integrating systems to record and report reaction conditions, and 3) Demonstrating the synthesis of known compounds using SPECS-enabled electrochemistry. Phase II goals focus on: 1) Scaling the technology for high-throughput screening with enhanced consistency and robustness, 2) Developing software for direct output control, 3) Incorporating diverse electrode materials to expand reactivity and selectivity, and 4) Piloting SPECS in academic research laboratories for validation and further improvement. By the project's conclusion, OWiC Technologies expects to commercialize SPECS as a transformative tool for drug discovery.