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Rhodium(III)-Catalyzed C-H Activation: Annulation of Petrochemical Feedstocks for the Construction of Isoquinolone Scaffolds

Joyann S. Barber, Dehuan Kong, Wei Li, Indrawan J. McAlpine, Sajiv K. Nair, Sylvie K. Sakata, Nicole Sun, Ryan L. Patman*

*Pfizer Oncology Medicinal Chemistry, 10770 Science Center Drive, San Diego, California 92121, USA, Email:

J. S. Barber, D. Kong, W. Li, I. J. McAlpine, S. K. Nair, S. K Sakata, N. Sun, R. L. Patman, Synlett, 2021, 32, 202-206.

DOI: 10.1055/s-0040-1706548

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A simple and robust procedure for the Rh(III)-catalyzed [4+2] cycloaddition of feedstock gases enabled through C-H activation provides a diverse set of 3,4-dihydroisoquinolones and 3-methylisoquinolones in very good yields. The effects of using ethylene and propyne as coupling partners on C-H site selectivity have been explored with a representative set of substrates.

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Key Words

rhodium catalysis, C-H activation, C-C bond formation, isoquinolones, 3,4-dihydroisoquinolones, annulation

ID: J72-Y2021