The Evolution of High-Throughput Experimentation in Pharmaceutical Development and Perspectives on the Future

Steven M. Mennen, Carolina Alhambra, C. Liana Allen, Mario Barberis, Simon Berritt, Thomas A. Brandt, Andrew D. Campbell, Jesús Castañón, Alan H. Cherney, Melodie Christensen, David B. Damon, J. Eugenio De Diego, Susana García-Cerrada, Pablo García-Losada, Rubén Haro, Jacob Janey, David C. Leitch, Ling Li, Fangfang Liu, Paul C. LobbenDavid W.C. Macmillan, Javier Magano, Emma McInturff, Sebastien Monfette, Ronald J. Post, Danielle Schultz, Barbara J. Sitter, Jason M. Stevens, Iulia I. Strambeanu, Jack Twilton, Ke Wang, Matthew A. Zajac

Research output: Contribution to journalArticlepeer-review

282 Scopus citations


High-throughput experimentation (HTE) has revolutionized the pharmaceutical industry, most notably allowing for rapid screening of compound libraries against therapeutic targets. The past decade has also witnessed the extension of HTE principles toward the realm of small-molecule process chemistry. Today, most major pharmaceutical companies have created dedicated HTE groups within their process development teams, invested in automation technology to accelerate screening, or both. The industry's commitment to accelerating process development has led to rapid innovations in the HTE space. This review will deliver an overview of the latest best practices currently taking place within our teams in process chemistry by sharing frequently studied transformations, our perspective for the next several years in the field, and manual and automated tools to enable experimentation. A series of case studies are presented to exemplify state-of-the-art workflows developed within our laboratories.

Original languageEnglish (US)
Pages (from-to)1213-1242
Number of pages30
JournalOrganic Process Research and Development
Issue number6
StatePublished - Jun 21 2019

All Science Journal Classification (ASJC) codes

  • Physical and Theoretical Chemistry
  • Organic Chemistry


  • automation
  • catalysis
  • high-throughput experimentation
  • screening


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