Total Syntheses of Ring Intact Limonoids:1,2-Dihydroazadirone, Azadirone, Azadiradione and Epoxyazadiradione

30 April 2025, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

Intact limonoids are an important class of limonoids with diverse biological activities. Herein, we report a concise and convergent route for the synthesis of four intact limonoids from readily available sclareolide in 12 to 15 steps. Key transformations include: 1) a selective oxidation of sclareolide at the C3 position via a C-H oxidation; 2) an intermolecular Mukaiyama-type aldol reaction for the convergent formation of the C12-C13 bond with an all-carbon quaternary center at C13; 3) a Pd-catalyzed Heck reaction for construction of the central six-membered C-ring in a stereocontrolled manner.

Keywords

ring intact limonoids
heck reaction
total synthesis

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