Scalable Total Synthesis of (−)-Vinigrol

Vinigrol is a structurally
and stereochemically complex natural
product that displays various potent pharmacological activities, including
the capability to modulate TNF-α. A new and efficient synthetic
route toward this natural product has been developed to complete the
asymmetric synthesis of (−)-vinigrol and provide over 600 mg
of material, manifesting the power of macrocyclic stereocontrol and
transannular Diels–Alder reaction.

Vinigrol是一种结构复杂且立体化学性质多样的天然产物，其展现出多种显著的药理活性，其中包括调节TNF-α的能力。针对该天然产物，已开发出一种新颖且高效的合成路径，以完成（-）-vinigrol的不对称合成，并提供了超过600毫克的物质，这一成就彰显了宏观环立体控制和跨环狄尔斯-阿尔德反应的强大力量。