Acoustic Droplet Ejection Enabled Automated Reaction Scouting.
Journal
ACS central science
ISSN: 2374-7943
Titre abrégé: ACS Cent Sci
Pays: United States
ID NLM: 101660035
Informations de publication
Date de publication:
27 Mar 2019
27 Mar 2019
Historique:
received:
26
10
2018
entrez:
3
4
2019
pubmed:
3
4
2019
medline:
3
4
2019
Statut:
ppublish
Résumé
Miniaturization and acceleration of synthetic chemistry are critically important for rapid property optimization in pharmaceutical, agrochemical, and materials research and development. However, in most laboratories organic synthesis is still performed on a slow, sequential, and material-consuming scale and not validated for multiple substrate combinations. Herein, we introduce fast and touchless acoustic droplet ejection (ADE) technology into small-molecule chemistry to transfer building blocks by nL droplets and to scout a newly designed isoquinoline synthesis. With each compound in a discrete well, 384 random derivatives were synthesized in an automated fashion, and their quality was monitored by SFC-MS and TLC-UV-MS analysis. We exemplify a pipeline of fast and efficient nmol scouting to mmol- and mol-scale synthesis for the discovery of a useful novel reaction with great scope.
Identifiants
pubmed: 30937372
doi: 10.1021/acscentsci.8b00782
pmc: PMC6439453
doi:
Types de publication
Journal Article
Langues
eng
Pagination
451-457Subventions
Organisme : NIGMS NIH HHS
ID : R01 GM097082
Pays : United States
Déclaration de conflit d'intérêts
The authors declare no competing financial interest.
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