Late‐Stage Borylation Strategy for the Development of New Boron‐Based Retinoids. Issue 5 (1st February 2023)

• Record Type: Journal Article
• Authors: Das, Bhaskar C.; Yadav, Pratik; Das, Sasmita; Saito, Mariko; Evans, Todd
• Is Part Of: ChemistrySelect. Volume 8:Issue 5(2023)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2023-02-01
• Subjects: Boratinoids -- Borylation -- Pyrazoles -- Pyrimidines -- Retinoids; Chemistry -- Periodicals; 540.5
• DOI: 10.1002/slct.202205003
• Languages: English
• ISSNs: 2365-6549

Abstract

Abstract: 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. Abstract : 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.