Synthesis Of The Intermediate Of Eplerenone

Eplerenon, a derivative of spironolactone, is the first selective aldosterone receptor antagonist. It has been proved to be a successful drug that targets the renin-angiotensin-aldosterone system. So it can be used for the treatment of hypertension and has no side effects such as menstrual irregularity and gynecomastia.17-hydroxy-7α-methoxycarbonyl-3 -oxo-17α-pregn-4ene-21 -carboxylic acid γ-lactone, the intermediate of eplerenone, was synthesized from dehydroepiandrosterone in the process of oxidation, enol etherification, oxirane formation, cyclocondensation, decarboxylation, dehydrogenation, addition, hydrolysis, ring-opening. Eplerenon can be convenient synthesized from this intermediate. And compared with the reported process, the improved process is safe, convenient and higher-yield. All products were indentified by IR, ~1H-NMR spectra.