Applications of high throughput chemistry to medicinal chemistry

Alexander Buitrago Santanilla, Gemma Cook

Research output: Chapter in Book/Report/Conference proceedingChapter


Rapid exploration of chemical space in Medicinal Chemistry projects is a demanding exercise that requires a steadfast approach and commitment to synthetic strategies that increase the success rate for desired compounds to answer a hypothesis. High-Throughput Experimentation (HTE) has proven to increase this success rate by directly evaluating project intermediates with pharmaceutically relevant building blocks in microscale quantities across a diverse chemical reaction space in parallel. This approach enables both the synthesis route and a blueprint for the scalability of the successful reactions. Herein, we present examples of the application of High-Throughput Chemistry (HTC) to Medicinal Chemistry projects spanning route scouting, parallel synthesis, and HTE coupled with other technologies such as flow and automation.
Original languageEnglish
Title of host publicationThe Power of High-Throughput Experimentation
Subtitle of host publicationCase Studies from Drug Discovery, Drug Development, and Catalyst Discovery
Place of PublicationWashington, DC
PublisherAmerican Chemical Society
Number of pages19
ISBN (Electronic)9780841297548
ISBN (Print)9780841297555
Publication statusE-pub ahead of print - 15 Nov 2022

Publication series

NameACS Symposium Series
PublisherAmerican Chemical Society
ISSN (Print)0097-6156


  • chemical synthesis
  • coupling reactions
  • medicinal chemistry
  • photochemical reactions
  • solvents


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