Synthesis of Many Different Types of Organic Small Molecules Using One Automated Process

Overview

Journal Science

Specialty Science

Date 2015 Mar 14

PMID 25766227

Citations 122

Authors

Junqi Li

Steven G Ballmer

Eric P Gillis

Seiko Fujii

Michael J Schmidt

Andrea M E Palazzolo

Jonathan W Lehmann

Greg F Morehouse

Martin D Burke

Affiliations

Soon will be listed here.

Abstract

Small-molecule synthesis usually relies on procedures that are highly customized for each target. A broadly applicable automated process could greatly increase the accessibility of this class of compounds to enable investigations of their practical potential. Here we report the synthesis of 14 distinct classes of small molecules using the same fully automated process. This was achieved by strategically expanding the scope of a building block-based synthesis platform to include even C(sp3)-rich polycyclic natural product frameworks and discovering a catch-and-release chromatographic purification protocol applicable to all of the corresponding intermediates. With thousands of compatible building blocks already commercially available, many small molecules are now accessible with this platform. More broadly, these findings illuminate an actionable roadmap to a more general and automated approach for small-molecule synthesis.

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