A General Strategy for the Nickel‐Catalyzed C−H Alkylation of Anilines | Zendy

Ruan Zhixiong | Zendy; Lackner Sebastian | Zendy; Ackermann Lutz | Zendy

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A General Strategy for the Nickel‐Catalyzed C−H Alkylation of Anilines

Author(s) -

Ruan Zhixiong,

Lackner Sebastian,

Ackermann Lutz

Publication year - 2016

Publication title -

angewandte chemie

Language(s) - English

Resource type - Journals

eISSN - 1521-3757

pISSN - 0044-8249

DOI - 10.1002/ange.201510743

Subject(s) - alkylation , chemistry , aniline , catalysis , denticity , nickel , halide , combinatorial chemistry , bond cleavage , vicinal , alkyl , primary (astronomy) , medicinal chemistry , organic chemistry , metal , physics , astronomy

The C−H alkylation of aniline derivatives with both primary and secondary alkyl halides was achieved with a versatile nickel catalyst of a vicinal diamine ligand. Step‐economic access to functionalized 2‐pyrimidyl anilines, key structural motifs in anticancer drugs, is thus provided. The C−H functionalization proceeded through facile C−H activation and SET‐type C−X bond cleavage with the assistance of a monodentate directing group, which could be removed in a traceless fashion.

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