A novel procedure for the synthesis of borylated quinolines and its application in the development of potential boron-based homeodomain interacting protein kinase 2 (HIPK2) inhibitors. Issue 37 (25th August 2022)

• Record Type: Journal Article
• Authors: Das, Bhaskar C.; Yadav, Pratik; Das, Sasmita; He, John Cijiang
• Is Part Of: RSC advances. Volume 12:Issue 37(2022)
• Page Start: 24187
• Page End: 24191
• Publication Date: 2022-08-25
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/d2ra05063c
• Languages: English
• ISSNs: 2046-2069

Abstract

Abstract : This report reveals a Pd catalyzed C-4 borylation of structurally complex chloroquinolines with B2 (pin)2 without the use of any external ligand for the synthesis of potential boron-based homeodomain interacting protein kinase 2 inhibitors. Abstract : Herein, we demonstrate a Pd catalyzed C-4 borylation of structurally complex chloroquinolines with bis(pinacolato)diboron under relatively simple and efficient conditions. Moreover, the borylated quinolines were converted into oxaborole, trifluoroborate salt and boronic acid and also rendered in the Suzuki reaction successfully. The method was also applied for the synthesis of potential boron-based homeodomain interacting protein kinase 2 (HIPK2) inhibitors. The strategy opens up new avenues for the functionalization of quinolines as potential probes and pharmacological agents for future biomedical research.