Late-Stage Borylation Strategy for the Development of New Boron-Based Retinoids

Herein, we describe the design and synthesis of boron-based bexarotene analogues as potential new retinoid X receptor (RXR) agonists. The synthetic strategy utilized a common intermediate to access different classes of bexarotene analogues, and subsequently these novel retinoids were borylated. The strategy accomplished synthesis of new classes of borotenoids (boron-based retinoids) via late-stage palladium-catalyzed borylation which could be useful for the development of new therapeutic agents and probes to study retinoic acid signaling pathways.

Automated summary

Here, we present the design and synthesis of boron-based bexarotene analogues as potential RXR agonists. A common intermediate was used to access different classes of analogues, which were then borylated to create novel borotenoids. This strategy enables the synthesis of new therapeutic agents and probes for studying retinoic acid signaling pathways.