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Cited by 537

The DOI matches its Crossref record; 60 of the 60 references it cites were found in a registry or an index.

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

Open access
Mennen, Steven M., Alhambra, Carolina, Allen, C. Liana, Barberis, Mario, Berritt, Simon, Brandt, Thomas A., Campbell, Andrew D., Castañón, Jesús, Cherney, Alan H., Christensen, Melodie, Damon, David B., Eugenio de Diego, J., García-Cerrada, Susana, García-Losada, Pablo, Haro, Rubén, Janey, Jacob, Leitch, David C., Li, Ling, Liu, Fangfang, Lobben, Paul C., MacMillan, David W. C., Magano, Javier, McInturff, Emma, Monfette, Sebastien, Post, Ronald J., Schultz, Danielle, Sitter, Barbara J., Stevens, Jason M., Strambeanu, Iulia I., Twilton, Jack, Wang, Ke, Zajac, Matthew A.·2019·Organic Process Research & Development

Abstract

Abstract 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.

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Crossref · 10.1021/acs.oprd.9b00140

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Metadata

Authors
Mennen, S. M., Alhambra, C., Allen, C. L., Barberis, M., Berritt, S., Brandt, T. A., Campbell, A. D., Castañón, J., Cherney, A. H., Christensen, M., Damon, D. B., Eugenio de Diego, J., García-Cerrada, S., García-Losada, P., Haro, R., Janey, J., Leitch, D. C., Li, L., Liu, F., Lobben, P. C., MacMillan, D. W. C., Magano, J., McInturff, E., Monfette, S., Post, R. J., Schultz, D., Sitter, B. J., Stevens, J. M., Strambeanu, I. I., Twilton, J., Wang, K., & Zajac, M. A.
Venue
Organic Process Research & Development
Published
2019-05-07
Volume
23
Issue
6
Pages
1213-1242
ISSN
  • 1083-6160 (ISSN-L)
  • 1520-586X
OpenAlex
W2944148756
Cited by
537
References
60
FWCI
14.59
Type
journal article
Language
en
Open access
hybrid

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CoChat. (2026). Citation check: The Evolution of High-Throughput Experimentation in Pharmaceutical Development and Perspectives on the Future. https://app.cochat.ai/papers/10.1021/acs.oprd.9b00140
The paper
Mennen, S. M., Alhambra, C., Allen, C. L., Barberis, M., Berritt, S., Brandt, T. A., Campbell, A. D., Castañón, J., Cherney, A. H., Christensen, M., Damon, D. B., Eugenio de Diego, J., García-Cerrada, S., García-Losada, P., Haro, R., Janey, J., Leitch, D. C., Li, L., Liu, F., . . . Zajac, M. A. (2019). The Evolution of High-Throughput Experimentation in Pharmaceutical Development and Perspectives on the Future. Organic Process Research & Development. https://doi.org/10.1021/acs.oprd.9b00140

Data sources

Bibliographic data: Semantic Scholar, OpenAlex, Crossref.

Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.