The present invention provides a novel 11-step enantioselective approach to the natural product hyperforin which enables access to a wide variety of hyperforin analogs. The present invention also provides pharmaceutical compositions comprising inventive hyperforin analogs. Hyperforin analogs synthesized using the present synthetic method are envisionsed useful in the treatment of various conditions including but not limited to depression and conditions characterized by depression inflammatory skin conditions diabetes asthma chronic obstructive pulmonary disease (COPD) kidney disorders and ischemic brain damage.
