Aryl Annulation: A Powerful Simplifying Retrosynthetic Disconnection.

ABSTRACT: Retrosynthetic deconstruction of a core aromatic ring is an especially simplifying retrosynthetic step, reducing the complexity of the precursor synthetic target. Moreover, when implemented to provide a penultimate intermediate, it enables late-stage divergent aryl introductions, permitting deep-seated core aryl modifications ordinarily accessible only by independent synthesis. Herein, we highlight the use of a ketone carbonyl group as the functionality to direct such late-stage divergent aryl introductions onto a penultimate intermediate with a projected application in the total synthesis of vinblastine and its presently inaccessible analogs containing indole replacements. Although the studies highlight this presently unconventional strategy with an especially challenging target in mind,

SUBMITTER: Gillard RM 

PROVIDER: S-EPMC10745204 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature