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Photo-Fries Rearrangement in Flow: Ways to Access 2-Acylphenols and Opportunities for Reaction Development

Yen-Ku Wu

Department of Applied Chemistry, National Yang Ming Chiao Tung University

Hsinchu, Taiwan

E-mail: yenkuwu@nycu.edu.tw

The Photo-Fries rearrangement was first discovered by Anderson and Reese over fifty years ago.1a Mechanistically, when a phenolic ester is photoexcited, it undergoes homolytic cleavage, forming a transient radical pair (phenoxyl and carbonyl).1b The productive combination of these radicals initially offers dearomatized intermediates, which then tautomerize into the corresponding ortho- or para-acylated products. Besides the possible formation of mixtures, the reaction can be further complicated by internal light filtering of 2-

acylphenol,1c by which the effective light absorbance gradually diminishes as the reaction proceeds (i.e. the concentration of the rearranged product increases). To address these challenges, a flow edition of photo-Fries rearrangement for the synthesis of 2-acylphenols in an aqueous micellar medium was developed.2a We take advantage of a narrow channel reactor and micelle-induced confinement effect to refine both the efficiency and selectivity of the parent photoreaction. Furthermore, I would like to discuss our recent efforts to exploit photoflow-Fries processes for the synthesis of fine chemicals and for the exploration of new reaction manifolds.2b,c

References

1. (a) Anderson, J. C.; Reese, C. B. Proc. Chem. Soc., London 1960, 217. (b) Toldo, J.

M.; Barbatti, M.; Goncalves, P. F. B. Phys. Chem. Chem. Phys. 2017, 19, 19103. (c)

Primo, J.; Tormo, R.; Miranda, M. A. Heterocycles 1982, 19, 1819.

2. (a) Chien, C.-C.; Kao, S.-C.; Chen, C.-J.; Wu, Y.-K. Chem. Commun. 2020, 56,

15470. (b) Chang, C.-Y.; Chen, C.-J.; Huang, S.-H.; Kao, S.-C.; Wu, Y.-K. Asian J. Org.

Chem. 2022, 11, e202100721. (c) Lin, X.-J.; Wang, C.-L.; Peng, C.-H.; Liu, H.-J.; Wu,

Y.-K. Chem. Asian J. 2024, 19, e202400269.

 

Keywords: organic synthesis; rearrangement; polyphenols; photoirradiation

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