C-H chlorination of (hetero)anilines via photo/organo co-catalysis.

doi:10.1039/d2ob00834c

Paper

C-H chlorination of (hetero)anilines via photo/organo co-catalysis.

Published Jun 22, 2022 · Wuchen Xie, Meng Wang, Siyu Yang

Organic & biomolecular chemistry

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Abstract

Chlorinated (hetero)anilines are a class of important structural motifs that are widely present in synthetic building blocks and pharmaceuticals. Despite recent advancements, direct aniline chlorination still suffers from ortho/para and mono/poly chlorination selectivity problems. Herein, we disclose a photo-redox and organo co-catalyzed chlorination method for anilines. This method has great substrate generality and excellent mono-chlorination selectivity. Another merit of this method is the late-stage modification of drug molecules, which would be useful in medicinal chemistry.

Study Snapshot

This photo-redox and organo co-catalyzed chlorination method for anilines offers excellent substrate generality and mono-chlorination selectivity, making it useful for late-stage modification of drug molecules in medicinal chemistry.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

C-H chlorination of (hetero)anilines via photo/organo co-catalysis.

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References

Citations

Late-stage modification of bioactive compounds: Improving druggability through efficient molecular editing

Late-stage modification of bioactive compounds can improve their potency and druggability, with increased cooperation between chemists and pharmacists potentially leading to new drug discovery ideas.