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Embarking on a Chemical Space Odyssey.
1School of Chemistry and Astbury Centre for Structural Molecular Biology, University of Leeds , Leeds, LS2 9JT, U.K.
Journal of Medicinal Chemistry
|March 25, 2017
Summary
Drug discovery faces limitations from a restricted reaction toolkit. High-throughput reaction optimization is expanding synthetic chemistry capabilities, driving innovation in medicinal chemistry.
Area of Science:
- Medicinal Chemistry
- Synthetic Chemistry
- Drug Discovery
Background:
- The chemical space accessible in drug discovery is limited by a narrow reaction toolkit.
- Existing reactions often fail with polar and functionalized substrates, further restricting exploration.
- Innovation in medicinal chemistry is hampered by these synthetic limitations.
Purpose of the Study:
- To highlight the impact of high-throughput reaction optimization on drug discovery workflows.
- To discuss the potential of high-throughput experimentation in expanding synthetic chemistry.
- To emphasize the role of enhanced synthetic capabilities in driving medicinal chemistry innovation.
Main Methods:
- Integration of high-throughput reaction optimization into discovery workflows.
- Application of high-throughput experimentation to explore new reaction classes.
- Analysis of the impact of optimized reactions on substrate scope.
Main Results:
- High-throughput reaction optimization increases the utility of specific reaction classes.
- The value of existing reaction toolkits is enhanced through optimization.
- Successful optimization broadens the applicability of reactions to challenging substrates.
Conclusions:
- High-throughput experimentation is poised to expand the scope of synthetic chemistry in drug discovery.
- This expansion is expected to foster greater innovation in medicinal chemistry.
- Overcoming synthetic limitations through advanced techniques is crucial for future drug development.