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Synthesis of Arylethylamines via C(sp3)-C(sp3) Palladium-Catalyzed Cross-Coupling

Rhys A. Lippa, David J. Battersby, John A. Murphy* and Tim N. Barrett*

*University of Strathclyde, 295 Cathedral Street, Glasgow G1 1XL, U.K.; GlaxoSmithKline, Gunnels Wood Road, Stevenage SG1 2NY, U.K. Email:;

R. A. Lippa, D. J. Battersby, J. A. Murphy, T. N. Barrett, J. Org. Chem., 2021, 86, 3583-3604.

DOI: 10.1021/acs.joc.0c02958

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A palladium-catalyzed C(sp3)-C(sp3) coupling between benzyl chlorides and air-/moisture-stable N,N-dialkylaminomethyltrifluoroborate salts provides substituted arylethylamines in good yields.

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Key Words

benzylation, amines

ID: J42-Y2021