Convergent synthesis of bicyclic boronates a cascade regioselective Suzuki-Miyaura/cyclisation protocol.

Bicyclic boronates have recently emerged as promising candidates to invoke targeted biomolecular interactions, given their selectivity for specific functionalities. Despite this, the general stability of the C-B bond , for such heterocycles, remains an intractable challenge that can often preclude their utility in drug discovery. To address this challenge, strategies that allow expedient access to strategically substituted boronates, that enable modulation of the C-B bond are urgently required.