[摘要]：A convergent route to the synthesis of manassantins A (I) and B (II), potent inhibitors of HIF-1, is described. Central to the synthesis is a stereoselective addn. of an organozinc reagent to a 2-benzenesulfonyl cyclic ether to achieve the 2,3-cis-3,4-trans-4,5-cis-tetrahydrofuran of the natural products. Preliminary structure-activity relationships suggested that the (R)-configuration at C-7 and C-7''' is not crit. for HIF-1 inhibition. In addn., the hydroxyl group at C-7 and C-7''' can be replaced with a carbonyl group without loss of activity.
