A new nucleophilic isoprenoid C-5 reagent is introduced which allowed synth
esis of an advanced and optically active forskolin intermediate in a very e
fficient way. In addition, docking experiments that are based on X-ray resu
lts indicate that there might exist forskolin analogues with improved prope
rties as far as binding to adenylyl cyclases and synthetic accessibility ar
e concerned. (C) 2000 Elsevier Science Ltd. All rights reserved.