Protecting-Group Free Total Synthesis of β-Levantenolide through Late Stage Bromo-Spirocyclization

Org Lett. 2024 Nov 28. doi: 10.1021/acs.orglett.4c03542. Online ahead of print.

Abstract

We describe a concise asymmetric total synthesis of naturally occurring [5,5]-oxaspirolactone β-levantenolide through an adventitious bromo-spirocyclization reaction of a trans-decalin appended γ-alkylidenebutenolide. The γ-alkylidenebutenolide core was constructed through "Pd-Cu" bimetallic cascade lactonization reaction of properly functionalized enantiopure alkyne. (+)-Sclareolide was used as a chiral pool starting material to access the desired alkyne.