Molecular Editing of Bilobalide: Regioselective C-Ring Lactam Formation
Wenjing Wang1,2, Stephan Scheeff1,2, Sam Chun-Kit Hau3
1School of Pharmacy, Faculty of Medicine, The Chinese University of Hong Kong, Hong Kong.
None:
Late-stage diversification of complex natural products enables rapid access to analogues for structure-activity relationship studies. Herein, we report a regioselective lactone-to-lactam editing strategy for bilobalide, affording previously inaccessible C-ring lactam analogues. The transformation proceeds through in situ activation of a benzoylated intermediate followed by cyclization, delivering fused bilobalide lactam scaffolds. This work expands the accessible chemical space of bilobalide for future biological exploration.
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