Reductive sp³–sp² Coupling Reactions Enable Late-Stage Modification of Pharmaceuticals
2020
Mennie, Katrina M. | Vara, Brandon A. | Levi, Samuel M.
Late-stage derivatization of pharmaceutically relevant scaffolds relies on the availability of highly functional-group tolerant reactions. Reactions that increase the sp³ character of molecules enable the pursuit of more selective and well-tolerated pharmaceuticals. Herein, we report the use of sp³–sp² cross-electrophile reductive couplings to modify a generic ATP-competitive kinase inhibitor with a broad range of primary and secondary alkyl halide coupling partners.
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