Synthesis of many different types of organic small molecules using one automated process

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

Research output: Contribution to journalArticlepeer-review

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 Csp3-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.

Original languageEnglish (US)
Pages (from-to)1221-1226
Number of pages6
JournalScience
Volume347
Issue number6227
DOIs
StatePublished - Mar 13 2015

ASJC Scopus subject areas

  • General

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