Facile and Highly Efficient Synthesis of Canrenone

OBJECTIVE To improve the synthetic procedure of canrenone. METHODS Canrenone was conveniently and high effectively synthesized from dehydroepiandrosterone acetate via epoxidation with sulfur ylide, carbolactonization with NaCH(COOEt)2, and regioselective dehydrogenation with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone, in sequence. RESULTS The total yield of canrenone was up to 69.8%. The chemical structures of target product were characterized by UV, IR, 1H-NMR, MS, and element analysis. CONCLUSION The improved procedure avoids the use of expensive reagents and canrenone was synthesized in a convenient way, which is facile for scale production.