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The medicinal chemist's toolbox for late stage functionalization of drug-like molecules
Abstract
The advent of modern C–H functionalization chemistries has enabled medicinal chemists to consider a synthetic strategy, late stage functionalization (LSF), which utilizes the C–H bonds of drug leads as points of diversification for generating new analogs.
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Cited by
Late-stage C–H functionalization offers new opportunities in drug discovery
Guillemard, L., Kaplaneris, N., Ackermann, L., & Johansson, M. J. (2021) · Nature Reviews Chemistry · doi:10.1038/s41570-021-00300-6 · Cited by 837
The importance of synthetic chemistry in the pharmaceutical industry
Campos, K. R., Coleman, P. J., Alvarez, J. C., Dreher, S. D., Garbaccio, R. M., Terrett, N. K., Tillyer, R. D., Truppo, M. D., & Parmee, E. R. (2019) · Science · doi:10.1126/science.aat0805 · Cited by 668
Douglas, J. J., Sevrin, M. J., & Stephenson, C. R. J. (2016) · Organic Process Research & Development · doi:10.1021/acs.oprd.6b00125 · Cited by 361
Shrivastava, A. D., & Kell, D. B. (2021) · Molecules · doi:10.3390/molecules26072065 · Cited by 25
Focused Libraries for Epigenetic Drug Discovery: The Importance of Isosteres: Miniperspective
Green, A. I., & Burslem, G. M. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c00592 · Cited by 21
Metadata
- Authors
- Cernak, T., Dykstra, K. D., Tyagarajan, S., Vachal, P., & Krska, S. W.
- Venue
- Chemical Society Reviews
- Publisher
- Royal Society of Chemistry (RSC)
- Published
- 2016
- Volume
- 45
- Issue
- 3
- Pages
- 546-576
- ISSN
- 0306-0012 (ISSN-L)
- 1460-4744
- OpenAlex
- W1956858148
- Cited by
- 1,743
- References
- 0
- FWCI
- 2.67
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: The medicinal chemist's toolbox for late stage functionalization of drug-like molecules. https://app.cochat.ai/papers/10.1039/c5cs00628g
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- Cernak, T., Dykstra, K. D., Tyagarajan, S., Vachal, P., & Krska, S. W. (2016). The medicinal chemist's toolbox for late stage functionalization of drug-like molecules. Chemical Society Reviews. https://doi.org/10.1039/c5cs00628g
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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.
