The methylenation of androsta-1,4-dien-17beta-ol-3-one (I) with paraformaldehyde and dimethylamine hydrochloride in isopentanol, at a temperature of at least 130 C, gives 6-methylenandrosta-1,4-diene-17beta-ol-3-one (II). Subsequent oxidation with Jones reagent in acetone, at approx. -10 C, yields exemestane.