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Benzannulation strategies that attach a planar arene ring to cyclic, saturated, three-dimensional bridged motifs are becoming valuable for drug discovery. Herein, a Lewis acid-catalyzed 4+3 annulation of in situ -generated o -QMs with bicyclo1.1.0butanes is developed. Reaction modulation further leveraged a telescoped 4+2 annulation of o -QMs with the in situ -formed cyclobutanes, leading to diversified sp 3 -rich oxabicyclic architectures. Overall, this study expands the scope for a new bioisosteric space for medicinal chemistry.
Mondal et al. (Fri,) studied this question.