Molecular editing of aza-arene C-H bonds by distance, geometry and chirality.

ABSTRACT: Direct molecular editing of heteroarene carbon-hydrogen (C-H) bonds through consecutive selective C-H functionalization has the potential to grant rapid access into diverse chemical spaces, which is a valuable but often challenging venture to achieve in medicinal chemistry¹. In contrast to electronically biased heterocyclic C-H bonds^2-9, remote benzocyclic C-H bonds on bicyclic aza-arenes are especially difficult to differentiate because of the lack of intrinsic steric/electronic biases^10-12. Here we report two conceptually distinct directing templates that enable the modular differentiation and functionalization of adjacent remote (C6 versus C7) and positionally similar (C3 versus C7) positions on bicyclic aza-arenes through careful modulation of distance,

SUBMITTER: Fan Z 

PROVIDER: S-EPMC10292866 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature