This synthesis study demonstrates a stereoselective approach to form a tricyclic core in tetrapetalones, implying efficient assembly for future modifications.
We describe a stereoselective approach to the ACD-ring tricyclic core of tetrapetalones, featuring a highly functionalized 6/7/5fused framework. The synthesis is enabled by two key transformations: an aryne-mediated three-component assembly that connects the A- and D-ring fragments while installing a synthetically versatile bromide handle, and a ring-closing olefin metathesis to forge the nitrogencontaining seven-membered C-ring. This sequence efficiently provided the fully assembled ACD-ring tricyclic framework bearing the requisite side chains for subsequent B-ring construction in 18 steps.
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LIU et al. (2026) studied this question.
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