Reductive sp 3 -sp 2 Coupling Reactions Enable Late-Stage Modification of Pharmaceuticals

Late-stage derivatization of pharmaceutically relevant scaffolds relies on the availability of highly functional-group tolerant reactions. Reactions that increase the sp character of molecules enable the pursuit of more selective and well-tolerated pharmaceuticals. Herein, we report the use of sp -s...

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Bibliographic Details
Published inOrganic letters Vol. 22; no. 2; pp. 556 - 559
Main Authors Mennie, Katrina M, Vara, Brandon A, Levi, Samuel M
Format Journal Article
LanguageEnglish
Published United States 17.01.2020
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Summary:Late-stage derivatization of pharmaceutically relevant scaffolds relies on the availability of highly functional-group tolerant reactions. Reactions that increase the sp character of molecules enable the pursuit of more selective and well-tolerated pharmaceuticals. Herein, we report the use of sp -sp cross-electrophile reductive couplings to modify a generic ATP-competitive kinase inhibitor with a broad range of primary and secondary alkyl halide coupling partners.
ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.9b04320