<p>[2,1]-Azaboranaphthalenes belong to an important class of compounds that display enhanced therapeutic activities courtesy of their unique boron–nitrogen (BN) bonds which are an isostere of naphthalene-based systems. Recently, Ravindra and co-workers^{<CitationRef CitationID="CR1">1</CitationRef>} reported a three-component synthesis of ring fused BN-isosteres with BN-2,1-azaboranaphthalenes that subsequently undergoes a ring expansion of unstrained cyclic ketones via a Wolff-type rearrangement. This commentary emphasizes the efficient and scalable preparation of these potentially high value azaborine analogues.</p> Graphical abstract <p>The boron-nitrogen (BN) isosteres, including BN-azaboranaphthalenes, represent an important class of compounds due to their enhanced therapeutic potential; however, their synthesis often demands harsh reaction conditions. In this news story, we highlight recent work by Ravindra and co-workers demonstrating the facile one-pot synthesis of azaborine congeners via a Wolff-type rearrangement.</p>