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.