The first synthesis of the marine HIF-1 inhibitor furospongolide has been achieved in eight linear steps from geranyl acetate. Key steps include Schlosser sp ³ -sp ³ cross-coupling and Sonogashira alkynylation of β-bromobutenolide. ... So far, little is known about the SAR profile of 1. It appears, however, that the intact butenolide ring is essential for HIF-1 inhibition since both its open lactone derivative 2 and the related furanolipid 3 were found to be inactive [4] [6] ( ...
