Bicyclo[1.1.1]pentane Ketones via Friedel-Crafts Acylation.

ABSTRACT: Bicyclo[1.1.1]pentane (BCP) is a rigid aliphatic hydrocarbon with a three-dimensional (3D), propeller-like shape and a molecular size that makes it a targeted bioisosteric replacement for phenylene and acetylene groups in medicinal chemistry. For the pharmaceutical application of BCP, simple, efficient, and cost-effective synthetic tools are required to enable the exploration of BCP's potential as a bioisostere across a broad chemical space. With numerous sophisticated protocols for C(sp³) functionalization of rigid aliphatic hydrocarbons reported in the literature, the synthesis of BCP mono- and diketones remains a challenging task, limited by both substrate scope and expensive photocatalysts. Here, we present a protocol for Friedel-Crafts acylation of (hetero)aromatic hydrocar

SUBMITTER: Urbanska K 

PROVIDER: S-EPMC12797227 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature