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An Integrated Console for Capsule-Based, Fully Automated Organic Synthesis

preprint
submitted on 22.03.2019 and posted on 25.03.2019 by Tuo Jiang, Samuele Bordi, Angus E. McMillan, Kuang-Yen Chen, Fumito Saito, Paula Nichols, Benedikt Wanner, Jeffrey Bode
The current laboratory-based practice of organic synthesis renders automation difficult, suffers from safety and environmental hazards, and hampers the implementation of artificial intelligence guided drug discovery. Using a combination of innovative reagent design, hardware engineering, and a simple operating system we provide an instrument capable of executing complex organic reactions with prepacked capsules in a fully automated fashion. The machine conducts coupling reactions and delivers the purified products with minimal user involvement. Two of the most desirable reaction classes – the synthesis of saturated N-heterocycles and reductive amination – were implemented, along with multi-step sequences that provide drug-like organic molecules in a fully automated manner. We envision that this system will serve as a console for developers to provide synthetic methods as integrated, user-friendly packages for conducting organic synthesis in a safe and convenient fashion.

Funding

ERC-2012-StG_20111012

ERC-2015-PoC - Hetspresso

ETH Pioneer Fellowship

Innosuisse 27406.1 PFLS-LS

History

Email Address of Submitting Author

bode@org.chem.ethz.ch

Institution

ETH Zurich

Country

Switzerland

ORCID For Submitting Author

0000000183948910

Declaration of Conflict of Interest

B.M.W., P.L.N, T.J, and J.W.B. are co-founders and shareholders of Synple Chem AG. ETH Zürich has filed a patent related to the technology; B.M.W.; P.L.N.; K.Y.C. and J.W.B. are listed as inventors.

Exports