SynCar: an approach to automated synthesis

Area of Science:

• Organic Chemistry
• Drug Discovery
• Automation Engineering

Background:

• Automating manual solution-phase synthesis presents a significant challenge in organic chemistry.
• Modern drug discovery requires high-purity compound libraries (50-250 compounds, 10-100 mg scale) with short cycle times and high capacity.
• Existing systems often lack the flexibility and throughput needed for efficient library generation.

Purpose of the Study:

• To design and develop a novel, integrated, and automated system for solution-phase synthesis.
• To meet the demands of modern drug discovery for high-purity compound libraries with enhanced efficiency and throughput.
• To create a flexible and scalable platform for parallel chemical synthesis.

Main Methods:

• Development of a novel system comprising independent modular workstations connected by a shuttle transfer system.
• Integration of synthesis (temperature control, liquid handling), filtration, extraction, evaporation, weighing, solid-phase extraction, and HPLC/MS analysis capabilities.
• Implementation of parallel processing of four reactions per shuttle, enabling continuous loading and customizable workflows.

Main Results:

• The developed system successfully integrates multiple solution-phase synthesis steps into a single automated platform.
• Achieved high flexibility and high throughput, enabling efficient production of compound libraries.
• Demonstrated the capability for parallel processing and continuous operation, significantly reducing cycle times.

Conclusions:

• The novel automated system effectively addresses the unmet challenge of automating solution-phase synthesis.
• The integrated platform offers a flexible, scalable, and high-throughput solution for drug discovery library production.
• This advancement in automation is critical for accelerating lead optimization and target class library development.