Molecular editing of bilobalide: Regioselective C-ring lactam formation
May 15, 2026·
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Wenjing Wang
contributed equally
Stephan Scheeff
contributed equally
,Sam Chun-Kit Hau
Yao Qin
Chanin Sillapachaiyaporn
Billy Wai-Lung Ng
Abstract
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.
Type
Publication
Org. Lett. 2026, 28, 19, 6027–6031
Authors
Research Associate (Medicinal Chemistry)
Medicinal chemist designing novel antiviral and anticancer compounds. Researched nucleoside analogues at CUHK under Prof. Billy Ng since 2021, awarded Hong Kong Postdoctoral Fellowship 2022/2023. Enjoys exploring Hong Kong’s countryside and culture through photography.