Cobalt-catalyzed conformationally restricted alkylarylation enables divergent access to Csp³-rich N-heterocycles.

ABSTRACT: Due to the intrinsic spatial orientation and structural novelty, Csp³-rich N-heterocycles have been recognized as increasingly sought-after scaffolds as compared to the aromatic ring-based moieties, which have generated considerable recent attention in drug discovery. Hence, we disclose a modular cobalt-catalyzed conformationally restricted alkylarylation strategy for the divergent access to Csp³-rich N-hetero(spiro)cycles. Herein, multiple effects, including radical rebound and conformational restriction, play critical roles in the stabilization of the stereospecific alkyl-cobalt-aryl intermediate. Under simple and mild reaction conditions, cobalt catalyst combines a range of polyfunctionalized cyclenyl bromides and organozinc pivalates to rapidly and reliably forge

SUBMITTER: Chen K 

PROVIDER: S-EPMC11406614 | biostudies-literature | 2024 Sep

REPOSITORIES: biostudies-literature